Lisdexamfetamine

Identification

Summary

Lisdexamfetamine is a central nervous system (CNS) stimulant used to treat attention deficit hyperactivity disorder (ADHD) and moderate to severe eating disorders.

Brand Names

Vyvanse

Generic Name

Lisdexamfetamine

DrugBank Accession Number

DB01255

Background

Also known as Vyvanse, lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine ⁴. It is paired with the essential amino acid L-lysine. Lisdexamfetamine dimesylate increases attention span and decreases restlessness in children and adults who are overactive/hyperactive, cannot concentrate for long periods, or are easily distracted or impulsive ².

As a central nervous system stimulant, lisdexamfetamine is utilized as an adjunct therapy in the treatment of attention deficit hyperactivity disorder (ADHD). As a prodrug, lisdexamfetamine was specifically engineered as an abuse-resistant product ¹¹. The mechanism by which this occurs is through delayed release after ingestion (unlike some other psychostimulant drugs, which may be abused). After oral administration and absorption, enzyme hydrolysis after contact with red blood cells metabolize lisdexamfetamine into L- lysine, a naturally occurring essential amino acid and active d-amphetamine, which is responsible for the drug’s pharmacological effects. Gastrointestinal pH does not affect this conversion, and the addition of the L-lysine slows the amount of d-amphetamine available in the circulation and central nervous system ¹¹.

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

Download

MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Lisdexamfetamine (DB01255)

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Weight

Average: 263.3785
Monoisotopic: 263.199762437

Chemical Formula

C₁₅H₂₅N₃O

Synonyms

• Lisdexamfetamine

Pharmacology

Indication

For the treatment of Attention-deficit/hyperactivity disorder (ADHD) and for moderate to severe binge eating disorder in adults ^Label, ⁴.

This drug is not indicated for weight loss. Use of other sympathomimetic drugs for weight loss is associated with serious cardiovascular effects. The safety and effectiveness of this drug for the treatment of obesity have not yet been determined ^Label.

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Associated Conditions

• Attention Deficit Hyperactivity Disorder (ADHD)
• Binge Eating Disorder (BED)

Contraindications & Blackbox Warnings

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Pharmacodynamics

Lisdexamfetamine dimesylate is a prodrug of d-amphetamine. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulating properties ^Label. This agent works primarily by inducing the release of the neurotransmitters dopamine and norepinephrine from their storage areas in presynaptic nerve terminals ¹⁰. Both of these transmitters contribute to alertness, increased concentration, in addition to effort and motivation.

Mechanism of action

Lisdexamfetamine is a prodrug of dextroamphetamine. The active form of this drug blocks the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. The parent drug, lisdexamfetamine, does not bind to the sites for the reuptake of norepinephrine and dopamine in vitro ^Label. The mechanism of therapeutic action in attention deficit hyperactivity disorder (ADHD) is not fully understood ⁹, ^Label. Amphetamines have been recently found to target the trace amine-associated receptor 1 (TAAR1), which was recently discovered. This may explain some of its effects on the extraneuronal space ⁵, ⁶,⁷. Ultimately, the ability of this agent to increase synaptic concentrations of the catecholamine neurotransmitters noradrenaline and dopamine in the prefrontal cortex (PFC), and in the striatum, results in several behavioral changes ¹⁰, ^Label.

Target	Actions	Organism
UTrace amine-associated receptor 1	agonist	Humans

Absorption

After oral administration, lisdexamfetamine is rapidly absorbed from the gastrointestinal tract ^Label, ⁹.

Chewable tablet form: After a single dose of 60 mg a chewable tablet in healthy subjects under fasted conditions, the Tmax of lisdexamfetamine and dextroamphetamine was reached at about 1 hour and 4.4 hour post administration, respectively ^Label.

Capsule form: Following single-dose oral (30 mg, 50 mg, or 70 mg) in patients ages 6 to 12 years with ADHD under fasted conditions, Tmax of lisdexamfetamine and dextroamphetamine was reached at about 1 hour and 3.5 hours post administration, respectively ^Label.

Volume of distribution

There is no accumulation of d-amphetamine (as measured by AUC) at steady state in healthy adults and no accumulation of lisdexamfetamine dimesylate after once-daily dosing for seven consecutive days ^Label, ⁹.

Protein binding

Not Available

Metabolism

The conversion of Lisdexamfetamine dimesylate (LDX) to the active metabolite d-amphetamine occurs primarily in the blood through enzymatic cleavage after active absorption of LDX from the gastrointestinal lumen ⁴. Lisdexamfetamine dimesylate is hydrolyzed in the blood to d-amphetamine, which is responsible for the drug’s therapeutic activity, as well as L-lysine. Amphetamine is reported to be oxidized at the 4 position of the benzene ring to form 4-hydroxyamphetamine, or on the side chain α or β carbons to form alpha-hydroxy-amphetamine or norephedrine, respectively. Norephedrine and 4-hydroxy-amphetamine are both active and each is subsequently oxidized to form 4-hydroxy-norephedrine. Alpha-hydroxy-amphetamine undergoes the process of deamination to form phenylacetone, which finally forms benzoic acid and its glucuronide and the glycine conjugate, hippuric acid. Although the enzymes involved in amphetamine metabolism have not been clearly identified, CYP2D6 is known to be involved with the formation of 4-hydroxy-amphetamine from amphetamine ⁹.

Hover over products below to view reaction partners

• Lisdexamfetamine
  • Dextroamphetamine + Lysine

Route of elimination

After the oral administration of a 70mg dose of radiolabeled lisdexamfetamine dimesylate to six healthy subjects, about 96% of the oral dose radioactivity was recovered in the urine and only 0.3% recovered in the feces ^Label, ⁹.

Half-life

The mean plasma elimination half-life of dextroamphetamine was about 12 hours after oral administration of lisdexamfetamine dimesylate ^Label.

The plasma elimination half-life of lisdexamfetamine alone averaged less than one hour in studies of lisdexamfetamine dimesylate administered in volunteer subjects ^Label.

Clearance

In a study of 47 subjects aged 55 years of age or older, amphetamine clearance was approximately 0.7L/hr/kg for subjects 55-74 years of age and 0.55L/hr/kg for subjects ≥75 years of age. This is slightly reduced compared to younger adults (approximately 1L/hr/kg for subjects 18-45 years of age) ⁹.

Adverse Effects

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Toxicity

Acute toxicity: Symptoms of acute overdosage with amphetamines include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia, and rhabdomyolysis. Fatigue and depression generally follow the symptoms central nervous system stimulation. Cardiovascular effects include arrhythmias, hypertension or hypotension and/or circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea, and abdominal cramps. Lethal poisoning is usually preceded by convulsions and coma ^Label. Prescribers should consider that serious cardiovascular (CV) events have been reported with this class of drugs ⁹.

Long-term effects: Acute administration of high doses of amphetamine (d- or d,l-) has been shown to produce long-term neurotoxic effects, which include irreversible nerve fiber damage, in rodents. The relevance of these findings to humans is currently unknown ^Label.

Oral LD50 (rat): 7,060 mg/kg ^MSDS

Oral LD50 (mouse): 3,450 mg/kg ^MSDS

Use in Pregnancy

This drug is categorized as a Pregnancy Category C: Animal studies have shown risk to the fetus, there are no controlled studies in women, or studies in women and animals are not available ^Label.

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.

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

Drug	Interaction
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Abatacept	The metabolism of Lisdexamfetamine can be increased when combined with Abatacept.
Abiraterone	The metabolism of Lisdexamfetamine can be decreased when combined with Abiraterone.
Acebutolol	The therapeutic efficacy of Acebutolol can be decreased when used in combination with Lisdexamfetamine.
Aceclofenac	The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Aceclofenac.
Acemetacin	The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Acemetacin.
Acetaminophen	The metabolism of Acetaminophen can be decreased when combined with Lisdexamfetamine.
Acetazolamide	Acetazolamide may decrease the excretion rate of Lisdexamfetamine which could result in a higher serum level.
Acetophenazine	Acetophenazine may decrease the stimulatory activities of Lisdexamfetamine.
Acetylsalicylic acid	The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Lisdexamfetamine.
Aclidinium	The risk or severity of Tachycardia can be increased when Lisdexamfetamine is combined with Aclidinium.

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Food Interactions

• Avoid antacids. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Antacids like sodium bicarbonate alkalinize the urine; therefore, they may reduce lisdexamfetamine elimination.
• Limit foods and supplements high in vitamin C. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Vitamin C acidifies the urine and, therefore, may increase lisdexamfetamine elimination.
• Take with or without food.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Lisdexamfetamine dimesylate	SJT761GEGS	608137-33-3	CETWSOHVEGTIBR-FORAGAHYSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Vyvanse	Capsule	40 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2007-12-10	Not applicable
Vyvanse	Capsule	70 mg/1	Oral	Avera McKennan Hospital	2015-09-30	2017-05-24
Vyvanse	Capsule	10 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2014-08-30	Not applicable
Vyvanse	Tablet, chewable	40 mg	Oral	Takeda	2019-08-06	Not applicable
Vyvanse	Capsule	50 mg/1	Oral	Physicians Total Care, Inc.	2008-07-11	Not applicable
Vyvanse	Tablet, chewable	50 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2017-01-28	Not applicable
Vyvanse	Tablet, chewable	10 mg	Oral	Takeda	2019-08-06	Not applicable
Vyvanse	Tablet, chewable	20 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2017-01-28	Not applicable
Vyvanse	Capsule	60 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2007-12-10	Not applicable
Vyvanse	Capsule	60 mg	Oral	Takeda	2010-04-14	Not applicable

Categories

ATC Codes

N06BA12 — Lisdexamfetamine

• N06BA — Centrally acting sympathomimetics
• N06B — PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
• N06 — PSYCHOANALEPTICS
• N — NERVOUS SYSTEM

Drug Categories

• Agents producing tachycardia
• Agents that produce hypertension
• Amines
• Amphetamines
• Central Nervous System Agents
• Central Nervous System Stimulants
• Central Nervous System Stimulation
• Centrally Acting Sympathomimetics
• Cytochrome P-450 CYP2D6 Inhibitors
• Cytochrome P-450 CYP2D6 Inhibitors (weak)
• Cytochrome P-450 CYP2D6 Substrates
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Dopamine Agents
• Dopamine Uptake Inhibitors
• Ethylamines
• Membrane Transport Modulators
• Nervous System
• Neurotransmitter Agents
• Neurotransmitter Uptake Inhibitors
• Phenethylamines
• Psychoanaleptics
• Psychostimulants, Agents Used for ADHD and Nootropics
• Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
• Sympathomimetics

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.

Kingdom

Organic compounds

Super Class

Organic acids and derivatives

Class

Carboxylic acids and derivatives

Sub Class

Amino acids, peptides, and analogues

Direct Parent

Alpha amino acid amides

Alternative Parents

Amphetamines and derivatives / Phenylpropanes / N-acyl amines / Secondary carboxylic acid amides / Organopnictogen compounds / Organic oxides / Monoalkylamines / Hydrocarbon derivatives / Carbonyl compounds

Substituents

Alpha-amino acid amide / Amine / Amphetamine or derivatives / Aromatic homomonocyclic compound / Benzenoid / Carbonyl group / Carboxamide group / Fatty acyl / Fatty amide / Hydrocarbon derivative

Molecular Framework

Aromatic homomonocyclic compounds

External Descriptors

Not Available

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

H645GUL8KJ

CAS number

608137-32-2

InChI Key

VOBHXZCDAVEXEY-JSGCOSHPSA-N

InChI

InChI=1S/C15H25N3O/c1-12(11-13-7-3-2-4-8-13)18-15(19)14(17)9-5-6-10-16/h2-4,7-8,12,14H,5-6,9-11,16-17H2,1H3,(H,18,19)/t12-,14-/m0/s1

IUPAC Name

(2S)-2,6-diamino-N-[(2S)-1-phenylpropan-2-yl]hexanamide

SMILES

C[C@@H](CC1=CC=CC=C1)NC(=O)[C@@H](N)CCCCN

References

Synthesis Reference

Michael J. Bauer, Gary Richard Callen, Judi Christine Humphrey, Todd Jeffrey Johnson, Matthew Wendell Schiesher, "Methods and Compositions for Preparing Lisdexamfetamine and Salts Thereof." U.S. Patent US20120157706, issued June 21, 2012.

US20120157706

General References

1. Jasinski DR, Krishnan S: Human pharmacology of intravenous lisdexamfetamine dimesylate: abuse liability in adult stimulant abusers. J Psychopharmacol. 2009 Jun;23(4):410-8. doi: 10.1177/0269881108093841. Epub 2008 Jul 17. [Article]
2. Madaan V: Lisdexamfetamine dimesylate for childhood ADHD. Drugs Today (Barc). 2008 May;44(5):319-24. doi: 10.1358/dot.2008.44.5.1215724. [Article]
3. Krishnan S, Moncrief S: An evaluation of the cytochrome p450 inhibition potential of lisdexamfetamine in human liver microsomes. Drug Metab Dispos. 2007 Jan;35(1):180-4. Epub 2006 Oct 11. [Article]
4. Goodman DW: Lisdexamfetamine dimesylate (vyvanse), a prodrug stimulant for attention-deficit/hyperactivity disorder. P T. 2010 May;35(5):273-87. [Article]
5. Miller GM: The emerging role of trace amine-associated receptor 1 in the functional regulation of monoamine transporters and dopaminergic activity. J Neurochem. 2011 Jan;116(2):164-76. doi: 10.1111/j.1471-4159.2010.07109.x. [Article]
6. Liu JF, Li JX: TAAR1 in Addiction: Looking Beyond the Tip of the Iceberg. Front Pharmacol. 2018 Mar 27;9:279. doi: 10.3389/fphar.2018.00279. eCollection 2018. [Article]
7. Pei Y, Asif-Malik A, Canales JJ: Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, Neurochemistry, and Clinical Implications. Front Neurosci. 2016 Apr 5;10:148. doi: 10.3389/fnins.2016.00148. eCollection 2016. [Article]
8. FDA Approved Drug Products: Vyvanse (lisdexamfetamine dimesylate) for oral use [Link]
9. Vyvanse, Canadian Monograph [File]
10. EPAR: Lisdexamfetamine dimesylate [File]
11. WHO Summary: Lisdexamfetamine [File]

External Links

Human Metabolome Database

HMDB0015385

PubChem Compound

11597698

PubChem Substance

46505358

ChemSpider

9772458

RxNav

700810

ChEBI

135925

ChEMBL

CHEMBL1201222

ZINC

ZINC000011680943

Therapeutic Targets Database

DAP000571

PharmGKB

PA164748975

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Lisdexamfetamine

MSDS

Download (33.8 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Not Available	Attention Deficit Hyperactivity Disorder (ADHD)	1
4	Completed	Basic Science	Attention Deficit Hyperactivity Disorder (ADHD)	2
4	Completed	Other	Attention Deficit Hyperactivity Disorder (ADHD)	1
4	Completed	Treatment	ADHD - Inattentive Type / Traumatic Brain Injury (TBI)	1
4	Completed	Treatment	ADHD Specifically With Executive Function Impairment	1
4	Completed	Treatment	Adult Attention Deficit Hyperactivity Disorder (ADHD) With Co-occuring Anxiety and Depressive Disorders	1
4	Completed	Treatment	Attention Deficit Hyperactivity Disorder (ADHD)	14
4	Completed	Treatment	Attention Deficit Hyperactivity Disorder (ADHD) / Deficient Emotional Self-Regulation (DESR)	1
4	Completed	Treatment	Brain Activity / Cognitive Functioning / Menopause	1
4	Completed	Treatment	Chronic Fatigue Syndrome/ Myalgic Encephalitis (CFS/ME) / Cognitive Impairment (CI)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• New River Pharmaceuticals Inc.
• Patheon Inc.
• Physicians Total Care Inc.
• Quality Care
• Shire Inc.

Dosage Forms

Form	Route	Strength
Capsule	Oral
Capsule, coated	Oral	70 mg
Capsule, coated	Oral	30 mg
Capsule, coated	Oral	50 mg
Capsule	Oral	10 mg
Capsule	Oral	10 mg/1
Capsule	Oral	20 mg
Capsule	Oral	20 mg/1
Capsule	Oral	30 mg/1
Capsule	Oral	30 mg
Capsule	Oral	40 mg/1
Capsule	Oral	40 mg
Capsule	Oral	50 mg
Capsule	Oral	50 mg/1
Capsule	Oral	60 mg
Capsule	Oral	60 mg/1
Capsule	Oral	70 mg
Capsule	Oral	70 mg/1
Tablet, chewable	Oral	10 mg
Tablet, chewable	Oral	10 mg/1
Tablet, chewable	Oral	20 mg/1
Tablet, chewable	Oral	20 mg
Tablet, chewable	Oral	30 mg/1
Tablet, chewable	Oral	30 mg
Tablet, chewable	Oral	40 mg
Tablet, chewable	Oral	40 mg/1
Tablet, chewable	Oral	50 mg
Tablet, chewable	Oral	50 mg/1
Tablet, chewable	Oral	60 mg/1
Tablet, chewable	Oral	60 mg
Capsule	Oral	20.0 mg
Capsule	Oral	30.0 mg
Capsule	Oral	40.0 mg
Capsule	Oral	50.0 mg
Capsule	Oral	60.0 mg
Capsule	Oral	70.0 mg
Capsule, coated	Oral	20 mg
Capsule, coated	Oral	40 mg
Capsule, coated	Oral	60 mg

Prices

Unit description	Cost	Unit
Vyvanse 30 mg capsule	6.24USD	capsule
Vyvanse 50 mg capsule	6.02USD	capsule
Vyvanse 70 mg capsule	5.85USD	capsule
Vyvanse 40 mg capsule	5.8USD	capsule
Vyvanse 20 mg capsule	5.26USD	capsule
Vyvanse 60 mg capsule	5.02USD	capsule

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

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US7659253	Yes	2010-02-09	2023-08-24
US7718619	Yes	2010-05-18	2023-08-24
US7659254	Yes	2010-02-09	2023-08-24
US7671030	Yes	2010-03-02	2023-08-24
US7662788	Yes	2010-02-16	2023-08-24
US7687467	Yes	2010-03-30	2023-08-24
US7678770	Yes	2010-03-16	2023-08-24
US7671031	Yes	2010-03-02	2023-08-24
US7713936	Yes	2010-05-11	2023-08-24
US7674774	Yes	2010-03-09	2023-08-24
US7678771	Yes	2010-03-16	2023-08-24
US7655630	Yes	2010-02-02	2023-08-24
US7687466	Yes	2010-03-30	2023-08-24
US7223735	Yes	2007-05-29	2023-08-24
US7700561	Yes	2010-04-20	2023-08-24
US7662787	Yes	2010-02-16	2023-08-24
US7723305	Yes	2010-05-25	2023-08-24
US7105486	Yes	2006-09-12	2023-08-24

Properties

State

Liquid

Experimental Properties

Property	Value	Source
water solubility	792 mg/mL (dimesylate salt)	FDA label
logP	-1.76	https://www.tga.gov.au/sites/.../auspar-lisdexamfetamine-dimesilate-131023-pi.docx
pKa	10.5	https://www.tga.gov.au/sites/.../auspar-lisdexamfetamine-dimesilate-131023-pi.docx

Predicted Properties

Property	Value	Source
Water Solubility	0.0877 mg/mL	ALOGPS
logP	1.01	ALOGPS
logP	1.14	Chemaxon
logS	-3.5	ALOGPS
pKa (Strongest Acidic)	15.89	Chemaxon
pKa (Strongest Basic)	10.21	Chemaxon
Physiological Charge	2	Chemaxon
Hydrogen Acceptor Count	3	Chemaxon
Hydrogen Donor Count	3	Chemaxon
Polar Surface Area	81.14 Å2	Chemaxon
Rotatable Bond Count	8	Chemaxon
Refractivity	78.31 m3·mol-1	Chemaxon
Polarizability	31.28 Å3	Chemaxon
Number of Rings	1	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	+	0.9858
Blood Brain Barrier	+	0.9444
Caco-2 permeable	+	0.664
P-glycoprotein substrate	Substrate	0.6919
P-glycoprotein inhibitor I	Non-inhibitor	0.9264
P-glycoprotein inhibitor II	Non-inhibitor	0.9802
Renal organic cation transporter	Non-inhibitor	0.8398
CYP450 2C9 substrate	Non-substrate	0.8303
CYP450 2D6 substrate	Non-substrate	0.621
CYP450 3A4 substrate	Non-substrate	0.7228
CYP450 1A2 substrate	Non-inhibitor	0.7025
CYP450 2C9 inhibitor	Non-inhibitor	0.9337
CYP450 2D6 inhibitor	Non-inhibitor	0.858
CYP450 2C19 inhibitor	Non-inhibitor	0.7568
CYP450 3A4 inhibitor	Non-inhibitor	0.5499
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.8494
Ames test	Non AMES toxic	0.7156
Carcinogenicity	Non-carcinogens	0.854
Biodegradation	Not ready biodegradable	0.8575
Rat acute toxicity	2.0058 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9688
hERG inhibition (predictor II)	Non-inhibitor	0.9004

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	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Targets

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insights and accelerate drug research.

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Details1. Trace amine-associated receptor 1

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Agonist

General Function

Trace-amine receptor activity

Specific Function

Receptor for trace amines, including beta-phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amin...

Gene Name

TAAR1

Uniprot ID

Q96RJ0

Uniprot Name

Trace amine-associated receptor 1

Molecular Weight

39091.34 Da

References

1. Miller GM: The emerging role of trace amine-associated receptor 1 in the functional regulation of monoamine transporters and dopaminergic activity. J Neurochem. 2011 Jan;116(2):164-76. doi: 10.1111/j.1471-4159.2010.07109.x. [Article]
2. Liu JF, Li JX: TAAR1 in Addiction: Looking Beyond the Tip of the Iceberg. Front Pharmacol. 2018 Mar 27;9:279. doi: 10.3389/fphar.2018.00279. eCollection 2018. [Article]
3. Pei Y, Asif-Malik A, Canales JJ: Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, Neurochemistry, and Clinical Implications. Front Neurosci. 2016 Apr 5;10:148. doi: 10.3389/fnins.2016.00148. eCollection 2016. [Article]

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Drug created at May 15, 2007 01:24 / Updated at March 22, 2023 02:02