Identification

Summary

Dihydroergotamine is an ergot alkaloid used in the acute treatment of migraine headache and cluster headache.

Brand Names
Dhe-45, Migranal, Trudhesa
Generic Name
Dihydroergotamine
DrugBank Accession Number
DB00320
Background

A 9,10alpha-dihydro derivative of ergotamine. Dihydroergotamine is used as an abortive therapy for migraines.10 Its use has largely been supplanted by triptans in current therapy due to the class's greater selectivity and more favourable side effect profile.

Recent improvements have been made in the design of intranasal delivery devices allowing for greater delivery of dihydroergotamine solution to the vasculature-rich upper nasal cavity.7 The recently approved Precision Olfactory Delivery technology developed by Impel Neuropharma technology has correlated with an increase of 3-fold in Cmax and 4-fold in AUC despite the solution formulated at 75% of the strength of the existing intranasal product.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 583.6774
Monoisotopic: 583.279469319
Chemical Formula
C33H37N5O5
Synonyms
  • (2R,4R,7R)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.02,7.012,16]hexadeca-1(16),9,12,14-tetraene-4-carboxamide
  • 5'-benzyl-12'-hydroxy-2'-methyl-3',6',18-trioxo-9,10-dihydroergotaman
  • 9,10-dihydro-12'-hydroxy-2'-methyl-5'-(phenylmethyl)ergotoman-3',6',18-trione
  • 9,10-dihydroergotamine
  • Dihidroergotamina
  • Dihydroergotamin
  • Dihydroergotamine
  • Dihydroergotaminum
  • Diidroergotamina
External IDs
  • MAP-0004
  • MAP0004

Pharmacology

Indication

Dihydroergotamine (DHE) in all formulations is indicated for the acute treatment of migraine with or without aura in adults.8,9,10 As an injection, DHE is also indicated for the acute treatment of cluster headache episodes.8

DHE is not indicated for migraine prevention or the management of hemiplegic or basilar migraine.8,9,10

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

DHE is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes.8,9,10 It is thought to exert its therapeutic effect through both neurological and vascular mechanisms.3 Its serotonin agonist activity may contribute to decreasing glutamatergic activity of the trigeminal system and subsequent cortical depolarization which is thought to participate in the neurological pathophysiology of migraine.2 The same serotonin agonist activity also contributes to vasoconstriction, producing both the characteristic side effect of chest tightness and potentially contributing to a therapeutic effect by counteracting the vasodilation due to calcitonin gene-related peptide (CGRP) release in migraine attacks.3

Mechanism of action

DHE has several proposed mechanisms which may contribute to its therapeutic efficacy as an abortive therapy in migraines. Firstly, DHE's s agonist action on 5-hydroxytryptamine (5HT) 1b receptors in the smooth muscle of the cranial vasculature may provide relief via vasoconstriction of the blood vessels which typically become dilated due to the release of CGRP during migraine attacks. 3,4 DHE's off-target action at alpha-adrenergic receptors may further contribute via this mechanism. The remaining mechanisms are thought to provide relief through the effects on the neurogenic causes of migraine symptoms. Agonist action by DHE on 5-HT1b and 5-HT1d receptors inhibits nociceptive signalling through the ventroposteromedial thalamus to the trigeminal sensory neurons. Further action on 5-HT1b and 5-HT1d receptors with the addition of agonist activity on 5-HT1f in the trigeminal nucleus caudalis decreases afferent signalling to trigeminal sensory neurons which contributes to central sensitization. The success of experimental compounds selectively targetting the 5-HT1f receptor lends support to this mechanism. Lastly, action at 5-HT1d receptors on trigeminal nerve terminals inhibits the release of vasoactive neuropeptides thought to contribute to pain and inflammation during a migraine attack. DHE is known to have 10-fold less potency at the 5-HT1b receptor than its predecessor ergotamine which reduces the incidence of vascular side effects.5 Notably, DHE slowly diffuses from receptors resulting in unreliable prediction of effects from plasma concentration. 4

TargetActionsOrganism
A5-hydroxytryptamine receptor 1B
agonist
Humans
A5-hydroxytryptamine receptor 1D
agonist
Humans
A5-hydroxytryptamine receptor 1F
agonist
Humans
UAlpha-2A adrenergic receptor
agonist
Humans
U5-hydroxytryptamine receptor 1A
agonist
Humans
U5-hydroxytryptamine receptor 1E
agonist
Humans
U5-hydroxytryptamine receptor 2A
agonist
Humans
U5-hydroxytryptamine receptor 2B
agonist
Humans
U5-hydroxytryptamine receptor 2C
agonist
Humans
UAlpha-1 adrenergic receptors
agonist
Humans
UAlpha-2 adrenergic receptors
agonist
Humans
UDopamine D2 receptor
agonist
Humans
UDopamine D3 receptor
agonist
Humans
UDopamine D4 receptor
agonist
Humans
U5-hydroxytryptamine receptor 4
agonist
Humans
UBeta-3 adrenergic receptor
agonist
Humans
Absorption

When delivered intranasally, DHE has a bioavailability of approximately 40% with a tmax of 30-60 min.10,4. Oral formulations have largely been unsuccessful due to a 1% bioavailability owing to a high degree of first-pass metabolism. 4 Both intramuscular and intravenous administration produces 100% bioavailability with a tmax of 1-2 min and 24-34 min respectively.4,6

Volume of distribution

DHE has a steady-state volume of distribution of 800 L.10,8

Protein binding

DHE is 93% bound to plasma proteins 10,8

Metabolism

DHE is metabolized in the liver to four identified metabolites. 8'-β-hydroxy dihydroergotamine is the primary metabolite and an active one with equipotency for adrenergic and 5-HT receptors.10 8'-β-hydroxy dihydroergotamine is present at plasma concentrations 5-7 times that of DHE. 4 The remaining metabolites are Dihydrolysergic acid, dihydrolysergic amide, and a fourth metabolite formed through oxidative opening of the proline ring are considered minor metabolites. After intranasal administration, it has been found that metabolites represent 20-30% of plasma AUC.10,4

Route of elimination

DHE is primarily eliminated through hepatic metabolism followed by biliary excretion. 10,4 6-7% of a single intramuscular dose is excreted in the urine.4

Half-life

DHE exhibits a biphasic elimination with half lives of 0.7-1 h and 10-13 h. 4

Clearance

The total clearance of DHE is 1.5 L/h with renal clearance contributing 0.1 L/h.10

Adverse Effects
Adverseeffects
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Toxicity

Symptoms of overdose include numbness, tingling, pain, and cyanosis of the extremities associated with diminished or absent peripheral pulses; respiratory depression; an increase and/or decrease in blood pressure, usually in that order; confusion, delirium, convulsions, and coma; and/or some degree of nausea, vomiting, and abdominal pain.10 In case of overdose, warmth should be applied to affected areas and vasodilators administered. Local poison control centres should be contacted for detailed information on care in cases of ergot overdose.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Dihydroergotamine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Dihydroergotamine can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Dihydroergotamine.
AbirateroneThe metabolism of Dihydroergotamine can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Dihydroergotamine can be decreased when combined with Acalabrutinib.
AcebutololAcebutolol may increase the vasoconstricting activities of Dihydroergotamine.
AceclofenacThe risk or severity of hypertension can be increased when Dihydroergotamine is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Dihydroergotamine is combined with Acemetacin.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Dihydroergotamine.
Interactions
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Food Interactions
  • Avoid grapefruit products. Grapefruit inhibits the metabolism of dihydroergotamine through the CYP3A4 pathway and, therefore, may increase serum levels of dihydroergotamine. Use caution if co-administering.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Dihydroergotamine mesylate81AXN7R2QT6190-39-2ADYPXRFPBQGGAH-UMYZUSPBSA-N
Dihydroergotamine tartrate76F2R89O7X5989-77-5FXDJFTCVYTUARH-YZPGULDNSA-N
International/Other Brands
Dihydergot (Sandoz) / Ergont (Sigmapharm) / Ergotonin / Ikaran (Pierre Fabre) / Orstanorm (Amdipharm) / Trudhesa (Impel NeuroPharma, Inc.) / Verladyn (Verla)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
D.H.E. 45Injection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousNovartis2001-10-032017-09-07US flag
D.H.E. 45Injection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousBausch Health US, LLC2001-10-03Not applicableUS flag
Dihydroergotamine (dhe), 1mg/mlLiquid1 mg / mLIntramuscular; Intravenous; SubcutaneousSterimax Inc1946-12-31Not applicableCanada flag
Dihydroergotamine Mesylate Injection USPLiquid1 mg / mLIntramuscular; Intravenous; SubcutaneousSandoz Canada Incorporated1999-12-232017-08-01Canada flag
MigranalSpray4 mg/1mLNasalBausch Health US, LLC1997-12-08Not applicableUS flag
Migranal Nasal Spray 4mg/mlLiquid0.5 mg / actNasalSterimax Inc1996-11-05Not applicableCanada flag
TrudhesaSpray, metered4 mg/1mLNasalImpel NeuroPharma, Inc.2021-09-24Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Dihydroergotamine MesylateInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousSagent Pharmaceuticals2018-09-15Not applicableUS flag
Dihydroergotamine MesylateInjection1 mg/1mLIntramuscular; Intravenous; SubcutaneousWest-Ward Pharmaceuticals Corp2017-09-15Not applicableUS flag
Dihydroergotamine MesylateSpray4 mg/1mLNasalLeucadia Pharmaceuticals2020-04-14Not applicableUS flag
Dihydroergotamine MesylateInjection1 mg/1mLIntramuscular; Intravenous; SubcutaneousBedford Pharmaceuticals2003-09-042011-08-31US flag
Dihydroergotamine MesylateInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousPaddock Laboratories, LLC.2003-04-29Not applicableUS flag
Dihydroergotamine MesylateSpray4 mg/1mLNasalOceanside Pharmaceuticals2013-03-18Not applicableUS flag
Dihydroergotamine MesylateInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousProvepharm Inc.2021-09-30Not applicableUS flag
Dihydroergotamine MesylateInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousPaddock Laboratories, LLC.2020-05-182021-09-30US flag
Dihydroergotamine MesylateInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousApollo Pharmaceuticals Inc.2020-04-14Not applicableUS flag
Dihydroergotamine Mesylate NasalSpray, metered4 mg/1mLNasalExelan Pharmaceuticals, Inc.2020-12-11Not applicableUS flag

Categories

ATC Codes
N02CA51 — Dihydroergotamine, combinationsN02CA01 — Dihydroergotamine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as ergotamines, dihydroergotamines, and derivatives. These are organic compounds containing an ergotamine moiety, which is structurally characterized by a benzyl substituent attached to the piperazine ring of the ergopeptine backbone.
Kingdom
Organic compounds
Super Class
Alkaloids and derivatives
Class
Ergoline and derivatives
Sub Class
Lysergic acids and derivatives
Direct Parent
Ergotamines, dihydroergotamines, and derivatives
Alternative Parents
Hybrid peptides / Dipeptides / Lysergamides / Indoloquinolines / Benzoquinolines / Quinoline-3-carboxamides / Pyrroloquinolines / N-acyl-alpha amino acids and derivatives / 3-alkylindoles / Piperidinecarboxamides
show 20 more
Substituents
1,4-diazinane / 3-alkylindole / 3-piperidinecarboxamide / Alkanolamine / Alpha-amino acid or derivatives / Alpha-dipeptide / Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound
show 43 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
ergot alkaloid (CHEBI:4562)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
436O5HM03C
CAS number
511-12-6
InChI Key
LUZRJRNZXALNLM-JGRZULCMSA-N
InChI
InChI=1S/C33H37N5O5/c1-32(35-29(39)21-15-23-22-10-6-11-24-28(22)20(17-34-24)16-25(23)36(2)18-21)31(41)38-26(14-19-8-4-3-5-9-19)30(40)37-13-7-12-27(37)33(38,42)43-32/h3-6,8-11,17,21,23,25-27,34,42H,7,12-16,18H2,1-2H3,(H,35,39)/t21-,23-,25-,26+,27+,32-,33+/m1/s1
IUPAC Name
(2R,4R,7R)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),9,12,14-tetraene-4-carboxamide
SMILES
[H][C@@]12CCCN1C(=O)[C@H](CC1=CC=CC=C1)N1C(=O)[C@](C)(NC(=O)[C@H]3CN(C)[C@]4([H])CC5=CNC6=CC=CC(=C56)[C@@]4([H])C3)O[C@@]21O

References

General References
  1. Shrewsbury SB, Cook RO, Taylor G, Edwards C, Ramadan NM: Safety and pharmacokinetics of dihydroergotamine mesylate administered via a Novel (Tempo) inhaler. Headache. 2008 Mar;48(3):355-67. doi: 10.1111/j.1526-4610.2007.01006.x. Epub 2007 Dec 28. [Article]
  2. Charles A: The pathophysiology of migraine: implications for clinical management. Lancet Neurol. 2018 Feb;17(2):174-182. doi: 10.1016/S1474-4422(17)30435-0. Epub 2017 Dec 8. [Article]
  3. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  4. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  5. Sullivan HJ, Tursi A, Moore K, Campbell A, Floyd C, Wu C: Binding Interactions of Ergotamine and Dihydroergotamine to 5-Hydroxytryptamine Receptor 1B (5-HT1b) Using Molecular Dynamics Simulations and Dynamic Network Analysis. J Chem Inf Model. 2020 Mar 23;60(3):1749-1765. doi: 10.1021/acs.jcim.9b01082. Epub 2020 Mar 2. [Article]
  6. Silberstein SD, Kori SH: Dihydroergotamine: a review of formulation approaches for the acute treatment of migraine. CNS Drugs. 2013 May;27(5):385-94. doi: 10.1007/s40263-013-0061-2. [Article]
  7. Silberstein SD, Shrewsbury SB, Hoekman J: Dihydroergotamine (DHE) - Then and Now: A Narrative Review. Headache. 2020 Jan;60(1):40-57. doi: 10.1111/head.13700. Epub 2019 Nov 17. [Article]
  8. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
  9. FDA Approved Drug Products: Migranal (dihydroergotamine mesylate) nasal spray [Link]
  10. FDA Approved Drug Products: TRUDHESA (dihydroergotamine mesylate) nasal spray [Link]
Human Metabolome Database
HMDB0014465
KEGG Drug
D07837
KEGG Compound
C07798
PubChem Compound
10531
PubChem Substance
46507711
ChemSpider
10091
BindingDB
50295557
RxNav
3418
ChEBI
4562
ChEMBL
CHEMBL1732
ZINC
ZINC000003978005
Therapeutic Targets Database
DAP000078
PharmGKB
PA164743028
PDBe Ligand
2GM
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Dihydroergotamine
PDB Entries
4iaq
FDA label
Download (412 KB)
MSDS
Download (53.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMigraine1
3CompletedTreatmentMigraine2
3CompletedTreatmentMigraine / Migraine With Aura / Migraine Without Aura1
3RecruitingTreatmentMigraine / Migraine With Aura / Migraine Without Aura2
3SuspendedTreatmentMigraine1
2TerminatedTreatmentMigraine in Children1
1CompletedTreatmentHealthy Subjects (HS)3
1CompletedTreatmentMigraine1
1CompletedTreatmentMigraine / Migraine With Aura / Migraine Without Aura1
1, 2CompletedTreatmentHealthy Subjects (HS)1

Pharmacoeconomics

Manufacturers
  • Valeant pharmaceuticals international
  • Bedford laboratories
  • Paddock laboratories inc
Packagers
  • Bedford Labs
  • Draxis Specialty Pharmaceuticals Inc.
  • Mipharm S.P.A.
  • Novartis AG
  • Paddock Labs
  • Prescript Pharmaceuticals
  • Valeant Ltd.
Dosage Forms
FormRouteStrength
Injection, solutionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Tablet
LiquidIntramuscular; Intravenous; Subcutaneous1 mg / mL
InjectionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Spray, meteredNasal4 mg/1mL
SolutionOral
Capsule
SprayNasal4 mg/1mL
SprayNasal
LiquidNasal0.5 mg / act
LiquidNasal4 mg / mL
Prices
Unit descriptionCostUnit
D.H.E. 45 1 mg/ml Solution 1ml Ampule124.61USD ampule
D.H.E. 45 1 mg/ml ampul120.88USD ml
Migranal 4 mg/ml Solution 1ml Glass Container94.46USD container
Migranal nasal spray90.83USD ml
D.h.e.45 1 mg/ml ampul54.46USD ml
Dihydroergotamine 1 mg/ml am38.0USD ml
Dihydroergotamine Mesylate 1 mg/ml Solution 1ml Ampule36.4USD ampule
Migranal 4 mg/ml Spray11.17USD spray
Dihydroergotamine (Dhe) 1 mg/ml4.18USD ml
Dihydroergotamine Mesylate 1 mg/ml3.9USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5169849No1992-12-082009-12-08US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.229 mg/mLALOGPS
logP3.04ALOGPS
logP2.71ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)9.71ChemAxon
pKa (Strongest Basic)8.39ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area118.21 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity159.39 m3·mol-1ChemAxon
Polarizability63.55 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.8348
Blood Brain Barrier-0.9817
Caco-2 permeable-0.7956
P-glycoprotein substrateSubstrate0.8223
P-glycoprotein inhibitor IInhibitor0.556
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.8229
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7227
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorInhibitor0.895
CYP450 2D6 inhibitorNon-inhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.712
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.591
Ames testNon AMES toxic0.897
CarcinogenicityNon-carcinogens0.9549
BiodegradationNot ready biodegradable0.9961
Rat acute toxicity2.9503 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9365
hERG inhibition (predictor II)Non-inhibitor0.5788
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (10.9 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific 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 subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Willems EW, Trion M, De Vries P, Heiligers JP, Villalon CM, Saxena PR: Pharmacological evidence that alpha1-and alpha2-adrenoceptors mediate vasoconstriction of carotid arteriovenous anastomoses in anaesthetized pigs. Br J Pharmacol. 1999 Jul;127(5):1263-71. [Article]
  2. Villalon CM, Centurion D, Willems EW, Arulmani U, Saxena PR, Valdivia LF: 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine. Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90. [Article]
  3. Buzzi MG, Moskowitz MA: Evidence for 5-HT1B/1D receptors mediating the antimigraine effect of sumatriptan and dihydroergotamine. Cephalalgia. 1991 Sep;11(4):165-8. [Article]
  4. Yu XJ, Waeber C, Castanon N, Scearce K, Hen R, Macor JE, Chauveau J, Moskowitz MA: 5-Carboxamido-tryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129, and serotonin-5-O-carboxymethyl-glycyl -tyrosinamide block dural plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine1B receptors. Mol Pharmacol. 1996 May;49(5):761-5. [Article]
  5. Pauwels PJ, Palmier C, Dupuis DS, Colpaert FC: Interaction of 5-HT1B/D ligands with recombinant h 5-HT1A receptors: intrinsic activity and modulation by G-protein activation state. Naunyn Schmiedebergs Arch Pharmacol. 1998 May;357(5):490-9. [Article]
  6. Sullivan HJ, Tursi A, Moore K, Campbell A, Floyd C, Wu C: Binding Interactions of Ergotamine and Dihydroergotamine to 5-Hydroxytryptamine Receptor 1B (5-HT1b) Using Molecular Dynamics Simulations and Dynamic Network Analysis. J Chem Inf Model. 2020 Mar 23;60(3):1749-1765. doi: 10.1021/acs.jcim.9b01082. Epub 2020 Mar 2. [Article]
  7. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  8. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific 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 subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Lesage AS, Wouters R, Van Gompel P, Heylen L, Vanhoenacker P, Haegeman G, Luyten WH, Leysen JE: Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. [Article]
  3. Buzzi MG, Moskowitz MA: The trigemino-vascular system and migraine. Pathol Biol (Paris). 1992 Apr;40(4):313-7. [Article]
  4. Buzzi MG, Dimitriadou V, Theoharides TC, Moskowitz MA: 5-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137-49. [Article]
  5. Silberstein SD, McCrory DC: Ergotamine and dihydroergotamine: history, pharmacology, and efficacy. Headache. 2003 Feb;43(2):144-66. [Article]
  6. Hoyer D, Lery H, Waeber C, Bruinvels AT, Nozulak J, Palacios JM: "5-HT1R" or 5-HT1D sites? Evidence for 5-HT1D binding sites in rabbit brain. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):249-54. [Article]
  7. Villalon CM, Centurion D, Willems EW, Arulmani U, Saxena PR, Valdivia LF: 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine. Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90. [Article]
  8. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  9. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  10. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
  11. FDA Approved Drug Products: TRUDHESA (dihydroergotamine mesylate) nasal spray [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific 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 trig...
Gene Name
HTR1F
Uniprot ID
P30939
Uniprot Name
5-hydroxytryptamine receptor 1F
Molecular Weight
41708.505 Da
References
  1. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  2. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Villalon CM, Centurion D, Willems EW, Arulmani U, Saxena PR, Valdivia LF: 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine. Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90. [Article]
  2. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  3. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific 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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific 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 trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Schaerlinger B, Hickel P, Etienne N, Guesnier L, Maroteaux L: Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol. 2003 Sep;140(2):277-84. Epub 2003 Aug 11. [Article]
  3. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  4. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...

Components:
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...

Components:
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
  2. Ramirez Rosas MB, Labruijere S, Villalon CM, Maassen Vandenbrink A: Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs. Expert Opin Pharmacother. 2013 Aug;14(12):1599-610. doi: 10.1517/14656566.2013.806487. Epub 2013 Jul 2. [Article]
  3. FDA Approved Drug Products: D.H.E. 45 (dihydroergotamine mesylate) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR4
Uniprot ID
Q13639
Uniprot Name
5-hydroxytryptamine receptor 4
Molecular Weight
43760.975 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein homodimerization activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
Gene Name
ADRB3
Uniprot ID
P13945
Uniprot Name
Beta-3 adrenergic receptor
Molecular Weight
43518.615 Da
References
  1. Dahlof C, Maassen Van Den Brink A: Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment. Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22. [Article]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Moubarak AS, Rosenkrans CF Jr, Johnson ZB: Modulation of cytochrome P450 metabolism by ergonovine and dihydroergotamine. Vet Hum Toxicol. 2003 Feb;45(1):6-9. [Article]
  2. Zhou Q, Yan XF, Zhang ZM, Pan WS, Zeng S: Rational prescription of drugs within similar therapeutic or structural class for gastrointestinal disease treatment: drug metabolism and its related interactions. World J Gastroenterol. 2007 Nov 14;13(42):5618-28. [Article]
  3. Dihydroergotamine FDA label [File]

Transporters

Details
1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [Article]
  2. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 01, 2021 01:05