Sumatriptan

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Identification

Summary

Sumatriptan is a serotonin receptor agonist used to treat migraines and cluster headaches.

Brand Names

Imitrex, Onzetra, Sumavel, Tosymra, Treximet, Zembrace

Generic Name

Sumatriptan

DrugBank Accession Number

DB00669

Background

Sumatriptan is a serotonin receptor agonist commonly used to treat migraines and sometimes cluster headaches.^5,6,7,8,9,10 Sumatriptan is the first of the triptans and was made available in Europe in 1991 to treat migraines.⁴ Sumatriptan was granted FDA approval on 28 December 1992.⁸

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Sumatriptan (DB00669)

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Weight

Average: 295.4
Monoisotopic: 295.135447621

Chemical Formula

C₁₄H₂₁N₃O₂S

Synonyms

• (3-[2-(dimethylamino)ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamide
• 1-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-methyl-methanesulfonamide
• 3-(2-(dimethylamino)ethyl)-N-methyl-1H-indole-5-methanesulfonamide
• 3-[2-(dimethylamino)ethyl]-N-methylindole-5-methanesulfonamide
• Sumatriptan
• Sumatriptán
• Sumatriptanum

External IDs

• GR 43175 A
• GR 43175 C
• GR 43175 X
• NP101
• SN 308

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Pharmacology

Indication

A combination sumatriptan and naproxen tablet is indicated for the treatment of migraines with or without auras in patients 12 years of age and older.⁵ Sumatriptan nasal powder, nasal spray, subcutaneous injection, and tablets are indicated to treat migraines with or without auras in adults.^6,7,8,9,10 One of the subcutaneous formulations of sumatriptan is also indicated to treat cluster headaches in adults⁸, while the other subcutaneous formulation is not.⁹

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Acute migraine		••••••••••••	•••••
Treatment of	Acute migraine		••• •••••	•••••••••
Treatment of	Acute migraine		••• •••••	••••••••••
Used in combination to treat	Acute migraine	Combination Product in combination with: Naproxen (DB00788)	••••••••••••	•••••
Treatment of	Acute cluster headache		••••••••••••	•••••

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Pharmacodynamics

Sumatriptan constricts cranial blood vessels and prevents the release of vasoactive peptides.² The dose of sumatriptan varies widely by route of administration and in most cases, no more than 2 doses should be given daily.^5,6,7,8,9,10 Medication overuse headaches may occur in patients who use sumatriptan frequently.^5,6,7,8,9,10

Mechanism of action

Sumatriptan is an agonist of 5-HT_1B and 5-HT_1D.^5,6,7,8,9,10 This agonism leads to constriction of cranial blood vessels and inhibits the release of pro-inflammatory neuropeptides.^5,6,7,8,9,10 Sumatriptan decreases carotid arterial blood flow, but increases blood flow velocity in the internal carotid artery and middle cerebral artery.^2,2,2

Target	Actions	Organism
A5-hydroxytryptamine receptor 1A	agonist	Humans
A5-hydroxytryptamine receptor 1D	agonist	Humans
A5-hydroxytryptamine receptor 1B	agonist	Humans
A5-hydroxytryptamine receptor 1F	agonist	Humans

Absorption

A 6mg subcutaneous injection of sumatriptan reaches a C_max of 69.5ng/mL (95% CI of 62.8-76.9ng/mL) with a T_max of 0.17h (95% CI of 0.08-0.33h), an AUC of 9.0h*ng/mL (95% CI of 7.5-10.9h*ng/mL), and a bioavailability of 100%.³

A 25mg oral dose of sumatriptan reaches a C_max of 16.5ng/mL (95% CI of 13.5-20.1ng/mL) with a T_max of 1.50h (95% CI of 0.50-2.00h), an AUC of 8.7h*ng/mL (95% CI of 6.1-12.5h*ng/mL), and a bioavailability of 14.3% (95% CI of 11.4-17.9%).³

A 20mg intranasal dose of sumatriptan reaches a C_max of 12.9ng/mL (95% CI of 10.5-15.9ng/mL) with a T_max of 1.50h (95% CI of 0.25-3.00h), an AUC of 7.4h*ng/mL (95% CI of 5.0-10.8h*ng/mL), and a bioavailability of 15.8% (95% CI of 12.6-19.8%).³

A 25mg rectal dose of sumatriptan reaches a C_max of 22.9ng/mL (95% CI of 18.4-28.6ng/mL) with a T_max of 1.00h (95% CI of 0.75-3.00h), an AUC of 14.6h*ng/mL (95% CI of 11.3-18.8h*ng/mL), and a bioavailability of 19.2% (95% CI of 15.3-24.1%).³

Volume of distribution

Sumatriptan has a volume of distribution of 50±8L for a 6mg subcutaneous dose⁷, or 2.7L/kg.¹⁰

Protein binding

Sumatriptan is 14%-21% bound to protein in circulation.^5,6,7,8,9,10

Metabolism

Sumatriptan is predominantly metabolized by monoamine oxidase A^{7,10,8,10,5,9}. The main metabolites are the inactive indole acetic acid and indole acetic acid glucuronide.^{7,10,8,10,5,9}

Hover over products below to view reaction partners

• Sumatriptan
  • Sumatriptan Metabolite GR49336
    • Sumatriptan Metabolite Ester Glucuronide of GR49336
  • Sumatriptan Metabolite GR34633

Route of elimination

22±4% is excreted in the urine as unchanged sumatriptan and 38±7% in urine as indole acetic acid^7,8 approximately 40% is excreted in the feces^10,5.

Half-life

Subcutaneous sumatriptan has a half life of 1.9h (95% CI of 1.7-2.0h).³ Oral sumatriptan has a half life of 1.7h (95% CI of 1.4-1.9h).³ Rectal sumatriptan has a half life of 1.8h (95% CI of 1.6-2.2h).³ Intrsnasal sumatriptan has a half life of 1.8h (95% CI of 1.7-2.0h).³

Clearance

Subcutaneous sumatriptan has a clearance of 0.22L/min (95% CI of 0.19-0.25L/min).³ Oral sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min).³ Rectal sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min).³ Intrsnasal sumatriptan has a clearance of 0.21L/min (95% CI of 0.18-0.25L/min).³ Total plasma clearance of sumatriptan is approximately 1200mL/min.⁶

Adverse Effects

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Toxicity

Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.^5,6,7,8,9,10 Overdoses may be fatal and patients should be monitored for 3-5 half lives or while symptoms persist.^5,6,7,8,9,10

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3	---	(T;T) / (C;T)	T Allele	Effect Directly Studied	Patients with this genotype have an increased likelihood of responding to sumatriptan when treating (condition: cluster headache).	Details

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of CNS depression can be increased when Sumatriptan is combined with 1,2-Benzodiazepine.
Abacavir	Sumatriptan may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abemaciclib	Abemaciclib may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Acarbose	The therapeutic efficacy of Acarbose can be increased when used in combination with Sumatriptan.
Acebutolol	Sumatriptan may decrease the antihypertensive activities of Acebutolol.

Food Interactions

• Avoid excessive or chronic alcohol consumption. Alcohol increased the risk of GI bleeding, ulcer, and perforation when taken with sumatriptan.
• Take with or without food.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Sumatriptan hemisulfate	7T9PTJ824O	143675-45-0	ZPBKNEYMSRHSSI-UHFFFAOYSA-N
Sumatriptan succinate	J8BDZ68989	103628-48-4	PORMUFZNYQJOEI-UHFFFAOYSA-N

Product Images

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International/Other Brands

Adracon (Inti) / Altaxa (Alapis Pharma) / Apigrane (Advanced Pharmaceutical) / Boots Pharmacy Migraine Relief (Boots) / Cinie (Zentiva) / Frimig (Orion) / Illument (Pliva) / Imigen (Mylan) / Imigran (GlaxoSmithKline) / Imigran mite (GlaxoSmithKline) / Imigran Radis (GlaxoSmithKline) / Imigrane (GlaxoSmithKline) / Imitrex Oral (GlaxoSmithKline) / Migralgin (GMP) / Migraneitor (Driburg) / Nazdav (Dr. Reddy's) / Sapphirex (Hemofarm) / Sumatran (Rowex) / Sumax (Libbs) / Suminat (Sun) / Youshu (Simcere)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Act Sumatriptan	Tablet	25 mg	Oral	Actavis Pharma Company	2005-08-24	2018-06-19
Act Sumatriptan	Tablet	100 mg	Oral	TEVA Canada Limited	2005-08-24	2021-07-30
Act Sumatriptan	Tablet	50 mg	Oral	Actavis Pharma Company	2005-08-24	2018-06-19
Alsuma	Injection, solution	6 mg/0.5mL	Subcutaneous	Us World Meds, Llc	2010-10-15	2013-08-31
Alsuma	Injection, solution	6 mg/0.5mL	Subcutaneous	Pfizer Laboratories Div Pfizer Inc.	2009-08-31	2015-08-31

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Ag-sumatriptan	Tablet	100 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-sumatriptan	Tablet	50 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-sumatriptan	Tablet	25 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Apo-sumatriptan	Tablet	100 mg	Oral	Apotex Corporation	2005-08-24	Not applicable
Apo-sumatriptan	Spray	5 mg / dose	Nasal	Apotex Corporation	Not applicable	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
SUAXINA® TABLETA RECUBIERTA	Sumatriptan succinate (85 mg) + Naproxen sodium (500 mg)	Tablet, coated	Oral	LABORATORIO FRANCO COLOMBIANO LAFRANCOL S.A.S.	2015-09-09	2021-10-01
Sumatriptan and Naproxen Sodium	Sumatriptan succinate (85 mg/1) + Naproxen sodium (500 mg/1)	Tablet, film coated	Oral	Aurobindo Pharma Limited	2018-02-15	Not applicable
Sumatriptan and Naproxen Sodium	Sumatriptan succinate (85 mg/1) + Naproxen sodium (500 mg/1)	Tablet, film coated	Oral	Northstar RxLLC	2018-11-27	Not applicable
Sumatriptan and Naproxen Sodium	Sumatriptan succinate (85 mg/1) + Naproxen sodium (500 mg/1)	Tablet, film coated	Oral	Mylan Pharmaceuticals Inc.	2018-09-04	2021-12-31
Sumatriptan and Naproxen Sodium	Sumatriptan succinate (85 mg/1) + Naproxen sodium (500 mg/1)	Tablet, film coated	Oral	Innovida Phamaceutique Corporation	2020-12-09	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Migranow	Sumatriptan succinate (50 mg/1) + Menthol (10 g/100g) + Synthetic camphor (4 g/100g)	Gel; Kit; Tablet	Oral; Topical	PureTek Corporation	2016-04-18	Not applicable
SumaChip	Sumatriptan succinate (100 mg/1) + Capsaicin (0.0375 g/100g) + Menthol (5 g/100g)	Kit	Oral; Topical	Basiem	2015-11-29	2016-03-04
Sumansetron	Sumatriptan succinate (50 mg/1) + Ondansetron hydrochloride dihydrate (4 mg/1)	Kit; Tablet; Tablet, film coated	Oral	PureTek Corporation	2021-01-01	Not applicable

Categories

ATC Codes

N02CC01 — Sumatriptan

• N02CC — Selective serotonin (5HT1) agonists
• N02C — ANTIMIGRAINE PREPARATIONS
• N02 — ANALGESICS
• N — NERVOUS SYSTEM

G01AE10 — Combinations of sulfonamides

• G01AE — Sulfonamides
• G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
• G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
• G — GENITO URINARY SYSTEM AND SEX HORMONES

N02CC51 — Sumatriptan and naproxen

• N02CC — Selective serotonin (5HT1) agonists
• N02C — ANTIMIGRAINE PREPARATIONS
• N02 — ANALGESICS
• N — NERVOUS SYSTEM

Drug Categories

• Agents that produce hypertension
• Amides
• Amines
• Analgesics
• Antidepressive Agents
• Antimigraine Preparations
• BCRP/ABCG2 Substrates
• Biogenic Amines
• Biogenic Monoamines
• Cardiovascular Agents
• Central Nervous System Depressants
• Drugs that are Mainly Renally Excreted
• Genito Urinary System and Sex Hormones
• Heterocyclic Compounds, Fused-Ring
• Indoles
• Monoamine Oxidase A Substrates
• Nervous System
• Neurotransmitter Agents
• OATP1B1/SLCO1B1 Substrates
• P-glycoprotein substrates
• Selective Serotonin 5-HT1 Receptor Agonists
• Selective Serotonin Agonists
• Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
• Serotonin 1b Receptor Agonists
• Serotonin 1d Receptor Agonists
• Serotonin 5-HT1 Receptor Agonists
• Serotonin Agents
• Serotonin Modulators
• Serotonin Receptor Agonists
• Serotonin-1b and Serotonin-1d Receptor Agonist
• Sulfonamides
• Sulfones
• Sulfur Compounds
• Triptans
• Tryptamines
• Vasoconstrictor Agents

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring substituted at the 3-position by an ethanamine.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Indoles and derivatives

Sub Class

Tryptamines and derivatives

Direct Parent

Tryptamines and derivatives

Alternative Parents

3-alkylindoles / Aralkylamines / Substituted pyrroles / Organosulfonamides / Organic sulfonamides / Benzenoids / Heteroaromatic compounds / Aminosulfonyl compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives

show 3 more

Substituents

3-alkylindole / Amine / Aminosulfonyl compound / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / Indole / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organic sulfonic acid amide / Organic sulfonic acid or derivatives / Organonitrogen compound / Organopnictogen compound / Organosulfonic acid amide / Organosulfonic acid or derivatives / Organosulfur compound / Pyrrole / Substituted pyrrole / Sulfonyl / Tertiary aliphatic amine / Tertiary amine / Tryptamine

show 16 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

sulfonamide, tryptamines (CHEBI:10650)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

8R78F6L9VO

CAS number

103628-46-2

InChI Key

KQKPFRSPSRPDEB-UHFFFAOYSA-N

InChI

InChI=1S/C14H21N3O2S/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3/h4-5,8-9,15-16H,6-7,10H2,1-3H3

IUPAC Name

1-{3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}-N-methylmethanesulfonamide

SMILES

CNS(=O)(=O)CC1=CC=C2NC=C(CCN(C)C)C2=C1

References

Synthesis Reference

Rajeev Mathur, T. Kumar, Sunilendu Roy, Rajiv Malik, "Taste masked sumatriptan tablets and processes for their preparation." U.S. Patent US20060233875, issued October 19, 2006.

US20060233875

General References

1. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. doi: 10.1016/j.pain.2008.06.002. Epub 2008 Aug 23. [Article]
2. Ferrari MD, Saxena PR: Clinical effects and mechanism of action of sumatriptan in migraine. Clin Neurol Neurosurg. 1992;94 Suppl:S73-7. [Article]
3. Duquesnoy C, Mamet JP, Sumner D, Fuseau E: Comparative clinical pharmacokinetics of single doses of sumatriptan following subcutaneous, oral, rectal and intranasal administration. Eur J Pharm Sci. 1998 Apr;6(2):99-104. [Article]
4. Humphrey PP: The discovery and development of the triptans, a major therapeutic breakthrough. Headache. 2008 May;48(5):685-7. doi: 10.1111/j.1526-4610.2008.01097.x. [Article]
5. FDA Approved Drug Products: Sumatriptan and Naproxen Oral Tablets [Link]
6. FDA Approved Drug Products: Sumatriptan Nasal Powder [Link]
7. FDA Approved Drug Products: Sumatriptan Nasal Spray [Link]
8. FDA Approved Drug Products: Sumatriptan Subcutaneous Injection [Link]
9. FDA Approved Drug Products: Sumatriptan Subcutaneous Solution [Link]
10. FDA Approved Drug Products: Sumatriptan Oral Tablets [Link]
11. Sumatriptan Tablets, USP monograph [Link]

External Links

Human Metabolome Database

HMDB0005037

KEGG Drug

D00451

KEGG Compound

C07319

PubChem Compound

5358

PubChem Substance

46506520

ChemSpider

5165

BindingDB

50005835

RxNav

37418

ChEBI

10650

ChEMBL

CHEMBL128

ZINC

ZINC000000014360

Therapeutic Targets Database

DNC001649

PharmGKB

PA451566

Guide to Pharmacology

GtP Drug Page

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Sumatriptan

MSDS

Download (49.9 KB)

Clinical Trials

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
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Not Available	Completed	Not Available	Arthritis / Gout Flares / Headache / Migraine / Muscle Spasms / Radicular syndrome / Synovitis / Tendonitis	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Healthy Volunteers (HV)	2	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Healthy Volunteers (HV) / Migraine	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Migraine	7	somestatus	stop reason	just information to hide
Not Available	Completed	Basic Science	Migraine	1	somestatus	stop reason	just information to hide

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Pharmacoeconomics

Manufacturers

• Glaxosmithkline
• King pharmaceuticals inc
• App pharmaceuticals llc
• Bedford laboratories div ben venue laboratories inc
• Bedford laboratories
• Jhp pharmaceuticals llc
• Par pharmaceutical inc
• Sagent strides llc
• Sandoz canada inc
• Teva parenteral medicines inc
• Wockhardt ltd
• Zogenix inc
• Aurobindo pharma ltd
• Dr reddys laboratories inc
• Mylan pharmaceuticals inc
• Orchid healthcare
• Ranbaxy laboratories ltd
• Roxane laboratories inc
• Sandoz inc
• Sun pharmaceutical industries ltd
• Teva pharmaceuticals usa inc
• Watson laboratories inc

Packagers

• 3M Health Care
• Advanced Pharmaceutical Services Inc.
• Amerisource Health Services Corp.
• Apotheca Inc.
• APP Pharmaceuticals
• A-S Medication Solutions LLC
• Ascend Therapeutics
• Aurobindo Pharma Ltd.
• AzurPharma Inc.
• Barr Pharmaceuticals
• Bayer Healthcare
• Bedford Labs
• Ben Venue Laboratories Inc.
• Bradley Pharmaceuticals Inc.
• Bristol-Myers Squibb Co.
• Cardinal Health
• Caremark LLC
• Cobalt Pharmaceuticals Inc.
• Contract Pharm
• Cura Pharmaceutical Co. Inc.
• Direct Dispensing Inc.
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• Doctor Reddys Laboratories Ltd.
• DPT Laboratories Ltd.
• Duramed
• Esprit Pharma Inc.
• Fielding Pharmaceutical Co.
• GlaxoSmithKline Inc.
• Greenstone LLC
• Innovative Manufacturing and Distribution Services Inc.
• JHP Pharmaceuticals LLC
• Kaiser Foundation Hospital
• Laboratoires Besins International
• Lake Erie Medical and Surgical Supply
• Major Pharmaceuticals
• Murfreesboro Pharmaceutical Nursing Supply
• Mylan
• Novartis AG
• Novavax Inc.
• Noven Pharmaceuticals Inc.
• Novo Nordisk Inc.
• Nucare Pharmaceuticals Inc.
• Ohm Laboratories Inc.
• Orion Corporation
• Palmetto Pharmaceuticals Inc.
• Par Pharmaceuticals
• PD-Rx Pharmaceuticals Inc.
• Penn Labs
• Pharmaceutical Utilization Management Program VA Inc.
• Pharmaceutics International Inc.
• Pharmacia Inc.
• Pharmpak Inc.
• Physicians Total Care Inc.
• Preferred Pharmaceuticals Inc.
• Prepackage Specialists
• QPharm Inc.
• Qualitest
• Ranbaxy Laboratories
• Rebel Distributors Corp.
• Redpharm Drug
• Resource Optimization and Innovation LLC
• Sandoz
• Southwood Pharmaceuticals
• Stat Rx Usa
• Sun Pharmaceutical Industries Ltd.
• Teva Pharmaceutical Industries Ltd.
• Unimed Pharmaceuticals Inc.
• Upsher Smith Laboratories
• Warner Chilcott Co. Inc.
• Watson Pharmaceuticals
• Wockhardt Ltd.
• Zogenix Inc.

Dosage Forms

Form	Route	Strength
Spray	Nasal	20 mg / dose
Spray	Nasal	5 mg / dose
Injection, solution	Subcutaneous	6 mg
Solution	Nasal	20.000 mg
Spray	Nasal	10 MG
Spray	Nasal	20 MG
Suppository		25 MG
Tablet	Oral	100.000 mg
Spray	Nasal
Tablet, film coated	Oral	100 MG
Tablet, film coated	Oral
Injection	Parenteral	6 mg/0.5ml
Tablet	Oral	50.000 mg
Tablet, orally disintegrating	Oral	50 mg
Aerosol	Respiratory (inhalation)	10 mg
Aerosol	Respiratory (inhalation)	20 mg
Injection, solution		6 mg/0.5ml
Spray	Nasal	20 mg / act
Spray	Nasal	20 mg/1
Spray	Nasal	5 mg/1
Spray	Nasal	5 mg / act
Tablet	Oral	50 mg
Liquid	Subcutaneous	12 mg / mL
Gel; kit; tablet	Oral; Topical
Kit	Nasal	11 mg/1
Capsule	Nasal	11 mg/1
Tablet	Oral	25 mg
Solution	Parenteral	6 mg
Solution	Subcutaneous	6 mg
Tablet	Oral	100 mg
Solution	Nasal; Respiratory (inhalation)	10 mg
Kit	Oral; Topical
Injection, solution	Subcutaneous
Kit; tablet; tablet, film coated	Oral
Spray	Nasal	20 mg/100uL
Spray	Nasal	20 mg/0.1mL
Spray	Nasal	5 mg/0.1mL
Spray	Nasal	5 mg/100uL
Tablet, coated	Oral	100 mg/1
Tablet, coated	Oral	50 mg/1
Tablet, delayed release	Oral	50 mg
Injection, solution		6 MG
Tablet	Oral
Solution	Subcutaneous	12 mg / mL
Injection	Subcutaneous	4 mg/0.5mL
Injection	Subcutaneous	6 mg/0.5mL
Injection, solution	Subcutaneous	4 mg/0.5mL
Injection, solution	Subcutaneous	6 mg/0.5mL
Tablet	Oral	100 mg/1
Tablet	Oral	25 mg/1
Tablet	Oral	50 mg/1
Tablet, coated	Oral	25 mg/1
Tablet, film coated	Oral	100 mg/1
Tablet, film coated	Oral	25 mg/1
Tablet, film coated	Oral	50 mg/1
Tablet	Oral
Injection, solution	Parenteral	6 MG/0.5ML
Injection, solution		3 MG/0.5ML
Tablet, coated	Oral	100 mg
Solution	Subcutaneous	6 mg / 0.5 mL
Spray	Nasal	10 mg/1
Spray	Nasal	10 mg/0.1mL
Tablet, coated	Oral
Tablet, film coated	Oral
Patch, extended release, electrically controlled	Transdermal	6.5 mg/4h
Injection, solution	Subcutaneous	3 mg/1
Solution	Subcutaneous	3 mg/0.5mL
Tablet, film coated	Oral	50 mg
Tablet, coated	Oral	50 mg

Prices

Unit description	Cost	Unit
Imitrex 4 mg/0.5 ml syringe kit	229.02USD	kit
Imitrex 6 mg/0.5 ml syringe kit	229.02USD	kit
Imitrex STATdose Refill 1 Ea = 2 unit Refill Box	217.16USD	box
Imitrex 4 mg/0.5 ml kit refill	216.92USD	kit
Imitrex 6 mg/0.5 ml kit refill	216.92USD	kit
SUMAtriptan Succinate Refill 6 mg/0.5ml Kit Box	191.84USD	box
Sumatriptan 6 mg/0.5 ml refill	184.46USD	each
Sumatriptan 4 mg/0.5 ml refill	184.44USD	each
Imitrex 6 mg/0.5 ml vial	106.84USD	vial
Imitrex 6 mg/0.5ml Solution 0.5ml Vial	98.93USD	vial
Imitrex 5 mg/act Solution Nasal Inhaler	55.49USD	inhaler
Imitrex 20 mg nasal spray	45.73USD	each
Imitrex 5 mg nasal spray	45.73USD	each
Imitrex 20 mg/act Solution Nasal Inhaler	43.44USD	inhaler
Sumatriptan 20 mg nasal spray	38.89USD	each
Sumatriptan 5 mg nasal spray	38.89USD	each
Imitrex 25 mg tablet	32.45USD	tablet
Imitrex 100 mg tablet	30.16USD	tablet
Imitrex 50 mg tablet	30.16USD	tablet
Sumatriptan Succinate 25 mg tablet	28.14USD	tablet
Sumatriptan succ 25 mg tablet	27.06USD	tablet
Sumatriptan Succinate 100 mg tablet	26.15USD	tablet
Sumatriptan Succinate 50 mg tablet	26.15USD	tablet
Sumatriptan succ 100 mg tablet	25.14USD	tablet
Sumatriptan succ 50 mg tablet	25.14USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US5705520	No	1998-01-06	2011-12-10
CA2469019	No	2005-09-13	2022-12-04
CA2098302	No	2001-10-16	2011-12-10
US6060499	Yes	2000-05-09	2018-02-14
US7332183	Yes	2008-02-19	2026-04-02
US6586458	Yes	2003-07-01	2018-02-14
US5872145	Yes	1999-02-16	2018-02-14
US8022095	Yes	2011-09-20	2018-02-14
US8491524	No	2013-07-23	2022-11-21
US6681810	No	2004-01-27	2015-12-13
US8287489	No	2012-10-16	2024-12-06
US6135979	No	2000-10-24	2017-03-21
US6280410	No	2001-08-28	2017-03-27
US6174304	No	2001-01-16	2015-12-13
US8343130	No	2013-01-01	2022-10-18
US8241243	No	2012-08-14	2023-08-10
US8241244	No	2012-08-14	2022-11-21
US5957886	No	1999-09-28	2016-03-08
US8267903	No	2012-09-18	2023-03-18
US7901385	No	2011-03-08	2026-07-31
US6251091	No	2001-06-26	2016-12-09
US8118771	No	2012-02-21	2023-08-10
US7776007	No	2010-08-17	2026-11-22
US7811254	No	2010-10-12	2027-08-26
US7973058	No	2011-07-05	2027-04-12
US8155737	No	2012-04-10	2027-04-12
US8366600	No	2013-02-05	2029-04-21
US8470853	No	2013-06-25	2027-04-12
US8983594	No	2015-03-17	2030-11-19
US6745071	No	2004-06-01	2023-02-21
US8597272	No	2013-12-03	2027-04-12
US9272137	No	2016-03-01	2027-09-07
US8875704	No	2014-11-04	2028-04-07
US8590530	No	2013-11-26	2025-09-15
US8327844	No	2012-12-11	2023-10-03
US7975690	No	2011-07-12	2025-08-18
US8899229	No	2014-12-02	2030-08-18
US9108015	No	2015-08-18	2025-09-15
US6715485	No	2004-04-06	2020-03-03
US8555877	No	2013-10-15	2020-03-03
US8550073	No	2013-10-08	2029-10-22
US8978647	No	2015-03-17	2030-12-06
US8047202	No	2011-11-01	2023-07-02
US9119932	No	2015-09-01	2024-04-23
US9327114	No	2016-05-03	2032-10-08
US9427578	No	2016-08-30	2027-04-12
US9649456	No	2017-05-16	2030-10-21
US10076615	No	2018-09-18	2029-07-30
US10076614	No	2018-09-18	2034-10-20
US10124132	No	2018-11-13	2027-03-06
US9211282	No	2015-12-15	2031-07-19
US9974770	No	2018-05-22	2030-06-16
US8440631	No	2013-05-14	2026-05-09
US9610280	No	2017-04-04	2030-06-16
US9283280	No	2016-03-15	2025-07-01
US8268791	No	2012-09-18	2026-05-09
US10478574	No	2019-11-19	2033-11-04
US10398859	No	2019-09-03	2027-12-19
US10537554	No	2020-01-21	2036-01-29
US10603305	No	2020-03-31	2030-06-16
US10722667	No	2020-07-28	2028-12-30
US11337962	No	2010-06-16	2030-06-16
US11364224	No	2016-01-29	2036-01-29
US11571531	No	2006-02-23	2026-02-23

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	169-170	http://www.chemspider.com/Chemical-Structure.5165.html
water solubility	54mg/mL	Sumatriptan Tablets, USP monograph
logP	0.93	ADLARD,M ET AL. (1995)
pKa	4.9	Sumatriptan Tablets, USP monograph

Predicted Properties

Property	Value	Source
Water Solubility	0.127 mg/mL	ALOGPS
logP	1.17	ALOGPS
logP	0.74	Chemaxon
logS	-3.4	ALOGPS
pKa (Strongest Acidic)	11.24	Chemaxon
pKa (Strongest Basic)	9.54	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	3	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	65.2 Å2	Chemaxon
Rotatable Bond Count	5	Chemaxon
Refractivity	82.08 m3·mol-1	Chemaxon
Polarizability	32.31 Å3	Chemaxon
Number of Rings	2	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.9626
Caco-2 permeable	-	0.8957
P-glycoprotein substrate	Substrate	0.5914
P-glycoprotein inhibitor I	Non-inhibitor	0.8782
P-glycoprotein inhibitor II	Non-inhibitor	0.9081
Renal organic cation transporter	Non-inhibitor	0.7344
CYP450 2C9 substrate	Non-substrate	0.8014
CYP450 2D6 substrate	Non-substrate	0.5913
CYP450 3A4 substrate	Substrate	0.6029
CYP450 1A2 substrate	Non-inhibitor	0.5603
CYP450 2C9 inhibitor	Non-inhibitor	0.7898
CYP450 2D6 inhibitor	Non-inhibitor	0.7422
CYP450 2C19 inhibitor	Non-inhibitor	0.7428
CYP450 3A4 inhibitor	Non-inhibitor	0.8309
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.6974
Ames test	Non AMES toxic	0.649
Carcinogenicity	Non-carcinogens	0.8134
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.5404 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.5668
hERG inhibition (predictor II)	Non-inhibitor	0.7046

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-0zfr-7390000000-5809ad2270f77ffcec79
Mass Spectrum (Electron Ionization)	MS	splash10-0a4i-9400000000-93cc7dc7e521f98aa292
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-03di-0190000000-c12ee3ac5f29c3420996
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-0a4i-2910000000-8769dc29dcac8fede7d1
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0002-0390000000-cdddf05865e6d570c337
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0a4i-2910000000-8769dc29dcac8fede7d1
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-052b-3090000000-33546513371e68e2fa08
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03di-9000000000-4a11fcb73b077f8c0dc9
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0a4i-9130000000-0504f559193daf7a0ad6
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01ox-9070000000-1c17c455eff68a79522f
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0a4i-9100000000-20e601df46e07eb8b56d
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-06tf-7940000000-83b4ba5bdf98816b6df2
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	183.9224126	predicted	DarkChem Lite v0.1.0
[M-H]-	184.4840126	predicted	DarkChem Lite v0.1.0
[M-H]-	161.67427	predicted	DeepCCS 1.0 (2019)
[M+H]+	183.7482126	predicted	DarkChem Lite v0.1.0
[M+H]+	184.7080126	predicted	DarkChem Lite v0.1.0
[M+H]+	164.06984	predicted	DeepCCS 1.0 (2019)
[M+Na]+	183.0707126	predicted	DarkChem Lite v0.1.0
[M+Na]+	184.3173126	predicted	DarkChem Lite v0.1.0
[M+Na]+	170.11028	predicted	DeepCCS 1.0 (2019)

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	501.19	N/A	N/A	A28734
IC 50 (nM)	398.11	N/A	N/A	A28734
Ki (nM)	440	N/A	N/A	A27734 / A28739
Ki (nM)	1023.29	N/A	N/A	A27484
Ki (nM)	257.03	N/A	N/A	A27484
Ki (nM)	330	N/A	N/A	A28735 / A28737
Ki (nM)	255	N/A	N/A	A28736
Ki (nM)	341	N/A	N/A	A28738 / A28740
Ki (nM)	407.1	N/A	N/A	A27735
Ki (nM)	230	N/A	N/A	A28741

Details

Binding Properties1. 5-hydroxytryptamine receptor 1A

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli

Specific Function

G protein-coupled serotonin receptor activity

Gene Name

HTR1A

Uniprot ID

P08908

Uniprot Name

5-hydroxytryptamine receptor 1A

Molecular Weight

46106.335 Da

References

1. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	16	N/A	N/A	A28746 / A28742
EC 50 (nM)	220	N/A	N/A	A28747
EC 50 (nM)	4.3	N/A	N/A	A28741
EC 50 (nM)	14	N/A	N/A	A28748 / A28749
EC 50 (nM)	12	N/A	N/A	A28750
EC 50 (nM)	5.3	N/A	N/A	A28754
IC 50 (nM)	39.81	N/A	N/A	A28734
IC 50 (nM)	5	N/A	N/A	A28746 / A28742
IC 50 (nM)	2400	N/A	N/A	A28742
IC 50 (nM)	6.7	N/A	N/A	A28748 / A28749
IC 50 (nM)	6.8	N/A	N/A	A28750
Ki (nM)	7.7	N/A	N/A	A27491
Ki (nM)	3.7	N/A	N/A	A28744
Ki (nM)	8.5	N/A	N/A	A27734 / A28739
Ki (nM)	3.71	N/A	N/A	A27484
Ki (nM)	3.38	N/A	N/A	A27484
Ki (nM)	1.7	N/A	N/A	A13000
Ki (nM)	30	N/A	N/A	A28738
Ki (nM)	5.7	N/A	N/A	A28738
Ki (nM)	8.4	N/A	N/A	A28745
Ki (nM)	2	N/A	N/A	A28740
Ki (nM)	8.6	N/A	N/A	A27735
Ki (nM)	4.4	N/A	N/A	A28741
Ki (nM)	1.99	N/A	N/A	A11525
Ki (nM)	11	N/A	N/A	A28751
Ki (nM)	5.5	N/A	N/A	A28752
Ki (nM)	3.4	N/A	N/A	A28753 / A28755
Ki (nM)	1.2	N/A	N/A	A28756

Details

Binding Properties2. 5-hydroxytryptamine receptor 1D

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction

Specific Function

G protein-coupled serotonin receptor activity

Gene Name

HTR1D

Uniprot ID

P28221

Uniprot Name

5-hydroxytryptamine receptor 1D

Molecular Weight

41906.38 Da

References

1. Koran LM, Pallanti S, Quercioli L: Sumatriptan, 5-HT(1D) receptors and obsessive-compulsive disorder. Eur Neuropsychopharmacol. 2001 Apr;11(2):169-72. [Article]
2. Baxter LR Jr: Brain mediation of Anolis social dominance displays. III. Differential forebrain 3H-sumatriptan binding in dominant vs. submissive males. Brain Behav Evol. 2001 Apr;57(4):202-13. [Article]
3. Razzaque Z, Pickard JD, Ma QP, Shaw D, Morrison K, Wang T, Longmore J: 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan. Br J Clin Pharmacol. 2002 Mar;53(3):266-74. [Article]
4. Akin D, Gurdal H: Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):177-82. [Article]
5. Zohar J, Kennedy JL, Hollander E, Koran LM: Serotonin-1D hypothesis of obsessive-compulsive disorder: an update. J Clin Psychiatry. 2004;65 Suppl 14:18-21. [Article]
6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
7. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. [Article]
8. Cohen ML, Schenck KW, Hemrick-Luecke SH: 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):1195-201. [Article]
9. Roy A, Brand NJ, Yacoub MH: Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves. J Heart Valve Dis. 2000 Mar;9(2):256-60; discussion 260-1. [Article]
10. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. doi: 10.1016/j.pain.2008.06.002. Epub 2008 Aug 23. [Article]
11. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. [Article]
12. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	77	N/A	N/A	A28739
EC 50 (nM)	38.3	N/A	N/A	A27735
IC 50 (nM)	16	N/A	N/A	A28746 / A28742
IC 50 (nM)	27	N/A	N/A	A28742
IC 50 (nM)	11	N/A	N/A	A28748 / A28749
IC 50 (nM)	10	N/A	N/A	A28750
Ki (nM)	2	N/A	N/A	A28613
Ki (nM)	3.4	N/A	N/A	A27491
Ki (nM)	23	N/A	N/A	A27734
Ki (nM)	7.76	N/A	N/A	A27484
Ki (nM)	9.33	N/A	N/A	A27484
Ki (nM)	10.96	N/A	N/A	A27484
Ki (nM)	1.99	N/A	N/A	A27484
Ki (nM)	61.65	N/A	N/A	A27484
Ki (nM)	5.5	N/A	N/A	A28735
Ki (nM)	10	N/A	N/A	A28737
Ki (nM)	1.2	N/A	N/A	A13000
Ki (nM)	22	N/A	N/A	A28738
Ki (nM)	24	N/A	N/A	A28738
Ki (nM)	23.1	N/A	N/A	A28739
Ki (nM)	60	N/A	N/A	A28745
Ki (nM)	28	N/A	N/A	A28745
Ki (nM)	6.4	N/A	N/A	A28740
Ki (nM)	19.1	N/A	N/A	A27735
Ki (nM)	9.6	N/A	N/A	A28741
Ki (nM)	25.11	N/A	N/A	A11525
Ki (nM)	36	N/A	N/A	A28751
Ki (nM)	47.9	N/A	N/A	A28752
Ki (nM)	7.7	N/A	N/A	A28753 / A28755
Ki (nM)	9.1	N/A	N/A	A28756

Details

Binding Properties3. 5-hydroxytryptamine receptor 1B

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries

Specific Function

G protein-coupled serotonin receptor activity

Gene Name

HTR1B

Uniprot ID

P28222

Uniprot Name

5-hydroxytryptamine receptor 1B

Molecular Weight

43567.535 Da

References

1. Dupuis DS, Perez M, Halazy S, Colpaert FC, Pauwels PJ: Magnitude of 5-HT1B and 5-HT1A receptor activation in guinea-pig and rat brain: evidence from sumatriptan dimer-mediated [35S]GTPgammaS binding responses. Brain Res Mol Brain Res. 1999 Apr 6;67(1):107-23. [Article]
2. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. [Article]
3. Cohen ML, Schenck KW, Hemrick-Luecke SH: 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):1195-201. [Article]
4. Cohen Z, Bouchelet I, Olivier A, Villemure JG, Ball R, Stanimirovic DB, Hamel E: Multiple microvascular and astroglial 5-hydroxytryptamine receptor subtypes in human brain: molecular and pharmacologic characterization. J Cereb Blood Flow Metab. 1999 Aug;19(8):908-17. [Article]
5. Granas C, Larhammar D: Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor. Eur J Pharmacol. 1999 Sep 10;380(2-3):171-81. [Article]
6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
7. Razzaque Z, Pickard JD, Ma QP, Shaw D, Morrison K, Wang T, Longmore J: 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan. Br J Clin Pharmacol. 2002 Mar;53(3):266-74. [Article]
8. Akin D, Gurdal H: Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):177-82. [Article]
9. Roy A, Brand NJ, Yacoub MH: Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves. J Heart Valve Dis. 2000 Mar;9(2):256-60; discussion 260-1. [Article]
10. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. doi: 10.1016/j.pain.2008.06.002. Epub 2008 Aug 23. [Article]
11. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	35	N/A	N/A	A28743
IC 50 (nM)	>1000	N/A	N/A	A28742
Ki (nM)	22.9	N/A	N/A	A27484
Ki (nM)	23	N/A	N/A	A18238
Ki (nM)	25.7	N/A	N/A	A28743

Details

Binding Properties4. 5-hydroxytryptamine receptor 1F

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity

Specific Function

G protein-coupled serotonin receptor activity

Gene Name

HTR1F

Uniprot ID

P30939

Uniprot Name

5-hydroxytryptamine receptor 1F

Molecular Weight

41708.505 Da

References

1. Razzaque Z, Heald MA, Pickard JD, Maskell L, Beer MS, Hill RG, Longmore J: Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999 Jan;47(1):75-82. [Article]
2. Pauwels PJ, John GW: Present and future of 5-HT receptor agonists as antimigraine drugs. Clin Neuropharmacol. 1999 May-Jun;22(3):123-36. [Article]
3. Cohen ML, Schenck K: Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT(1F) receptor agonists and PGF(2alpha). Br J Pharmacol. 2000 Oct;131(3):562-8. [Article]
4. Janssen P, Tack J, Sifrim D, Meulemans AL, Lefebvre RA: Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67. [Article]
5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
6. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. [Article]
7. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. doi: 10.1016/j.pain.2008.06.002. Epub 2008 Aug 23. [Article]
8. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. [Article]

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Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 17:56