Naratriptan

Identification

Summary

Naratriptan is a 5-HT1B/1D receptor agonist used to treat migraines.

Generic Name

Naratriptan

DrugBank Accession Number

DB00952

Background

Naratriptan is a triptan drug that is selective for the 5-hydroxytryptamine1 receptor subtype. It is typically used for the treatment of migraine headaches.

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Naratriptan (DB00952)

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Weight

Average: 335.464
Monoisotopic: 335.166747749

Chemical Formula

C₁₇H₂₅N₃O₂S

Synonyms

• N-methyl-2-(3-(1-methylpiperiden-4-yl)indole-5-yl)ethanesulfonamide
• N-methyl-2-[3-(1-methyl-4-piperidyl)-1H-indol-5-yl]-ethanesulfonamide
• Naratriptán
• Naratriptan
• Naratriptanum

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Pharmacology

Indication

For the acute treatment of migraine attacks with or without aura in adults.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Acute migraine with aura		••••••••••••	•••••
Treatment of	Acute migraine without aura		••••••••••••	•••••

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Contraindications & Blackbox Warnings

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Pharmacodynamics

Naratriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonist. Naratriptan has only a weak affinity for 5-HT_1A, 5-HT_5A, and 5-HT₇ receptors and no significant affinity or pharmacological activity at 5-HT₂, 5-HT₃ or 5-HT₄ receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Naratriptan also activates 5-HT₁ receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Naratriptan in humans.

Mechanism of action

Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.

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

Well absorbed (74% oral biovaility), absorption is rapid with peak plasma concentrations after 2-5 hours. The rate of absorption is slower during a migraine attack.

Volume of distribution

• 170 L

Protein binding

28%-31% (over the concentration range of 50 to 1000 ng/mL)

Metabolism

Primarily hepatic. In vitro, naratriptan is metabolized by a wide range of cytochrome P450 isoenzymes into a number of inactive metabolites.

Route of elimination

Not Available

Half-life

5-8 hours

Clearance

• 6.6 mL/min/kg

Adverse Effects

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Toxicity

Symptoms of overdose include light-headedness, loss of coordination, tension in the neck, and tiredness.

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

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 naratriptan when treating (condition: cluster headache).	Details

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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 Naratriptan is combined with 1,2-Benzodiazepine.
Acebutolol	Naratriptan may decrease the antihypertensive activities of Acebutolol.
Aceclofenac	The risk or severity of hypertension can be increased when Naratriptan is combined with Aceclofenac.
Acemetacin	The risk or severity of hypertension can be increased when Naratriptan is combined with Acemetacin.
Acenocoumarol	The risk or severity of adverse effects can be increased when Naratriptan is combined with Acenocoumarol.

Food Interactions

• Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Naratriptan hydrochloride	10X8X4P12Z	143388-64-1	AWEZYKMQFAUBTD-UHFFFAOYSA-N

Product Images

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International/Other Brands

Naramig

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Amerge	Tablet	2.5 mg	Oral	Glaxosmithkline Inc	1998-05-05	2022-12-14
Amerge	Tablet, film coated	1 mg/1	Oral	GlaxoSmithKline LLC	1998-02-26	2023-02-28
Amerge	Tablet	1 mg	Oral	Glaxosmithkline Inc	1998-05-05	2022-08-25
Amerge	Tablet, film coated	2.5 mg/1	Oral	GlaxoSmithKline LLC	1998-02-26	2023-02-28

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Apo-naratriptan	Tablet	2.5 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Apo-naratriptan	Tablet	1 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Naratriptan	Tablet, film coated	2.5 mg/1	Oral	Sun Pharmaceutical Industries Limited	2011-02-22	2017-11-30
Naratriptan	Tablet	2.5 mg/1	Oral	Heritage Pharmaceuticals Inc. d/b/a Avet Pharmaceuticals Inc.	2011-03-15	Not applicable
Naratriptan	Tablet, film coated	2.5 mg/1	Oral	Teva	2013-08-09	2015-10-31

Categories

ATC Codes

N02CC02 — Naratriptan

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

Drug Categories

• Agents that produce hypertension
• Amines
• Analgesics
• Antidepressive Agents
• Antimigraine Preparations
• Biogenic Amines
• Biogenic Monoamines
• Cardiovascular Agents
• Central Nervous System Depressants
• Heterocyclic Compounds, Fused-Ring
• Indoles
• Monoamine Oxidase A Substrates
• Nervous System
• Neurotransmitter Agents
• 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
• Triptans
• Vasoconstrictor Agents

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as 3-alkylindoles. These are compounds containing an indole moiety that carries an alkyl chain at the 3-position.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Indoles and derivatives

Sub Class

Indoles

Direct Parent

3-alkylindoles

Alternative Parents

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

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Substituents

3-alkylindole / Amine / Aminosulfonyl compound / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / 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 / Piperidine / Pyrrole / Substituted pyrrole / Sulfonyl / Tertiary aliphatic amine / Tertiary amine

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Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

sulfonamide, tryptamines, heteroarylpiperidine (CHEBI:7478)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

QX3KXL1ZA2

CAS number

121679-13-8

InChI Key

AMKVXSZCKVJAGH-UHFFFAOYSA-N

InChI

InChI=1S/C17H25N3O2S/c1-18-23(21,22)10-7-13-3-4-17-15(11-13)16(12-19-17)14-5-8-20(2)9-6-14/h3-4,11-12,14,18-19H,5-10H2,1-2H3

IUPAC Name

N-methyl-2-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]ethane-1-sulfonamide

SMILES

CNS(=O)(=O)CCC1=CC2=C(NC=C2C2CCN(C)CC2)C=C1

References

Synthesis Reference

Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Sandip Vasant Chikhalikar, Maruti Ghagare, "Process for the synthesis of naratriptan." U.S. Patent US20120220778, issued August 30, 2012.

US20120220778

General References

1. Massiou H: Naratriptan. Curr Med Res Opin. 2001;17 Suppl 1:s51-3. [Article]
2. Lambert GA: Preclinical neuropharmacology of naratriptan. CNS Drug Rev. 2005 Autumn;11(3):289-316. [Article]
3. Villalon CM, Centurion D, Valdivia LF, de Vries P, Saxena PR: Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol. 2003 Mar;1(1):71-84. [Article]

External Links

Human Metabolome Database

HMDB0015087

KEGG Drug

D08255

KEGG Compound

C07792

PubChem Compound

4440

PubChem Substance

46507243

ChemSpider

4287

BindingDB

50073682

RxNav

141366

ChEBI

7478

ChEMBL

CHEMBL1278

ZINC

ZINC000000004076

Therapeutic Targets Database

DAP000890

PharmGKB

PA450597

Guide to Pharmacology

GtP Drug Page

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

PDRhealth

PDRhealth Drug Page

Wikipedia

Naratriptan

FDA label

Download (1.93 MB)

MSDS

Download (29.8 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Other	Workplace Migraine Treatment	1
4	Terminated	Not Available	Antisocial Personality Disorder (ASPD) / Impulse Regulation Disorder / Intermittent Explosive Disorder / Psychosis	1
4	Terminated	Treatment	Post-Traumatic Headaches	1
3	Withdrawn	Treatment	Headache / Migraine	2
1, 2	Unknown Status	Treatment	Migraine	1

Pharmacoeconomics

Manufacturers

• Glaxosmithkline
• Paddock laboratories inc
• Roxane laboratories inc
• Sandoz inc
• Teva pharmaceuticals usa

Packagers

• GlaxoSmithKline Inc.
• Paddock Labs
• Roxane Labs
• Sandoz
• Teva Pharmaceutical Industries Ltd.

Dosage Forms

Form	Route	Strength
Tablet	Oral	1 mg
Tablet, coated	Oral	2.5 mg
Tablet, coated	Oral	250000 mg
Tablet	Oral	1 mg/1
Tablet	Oral	2.5 mg/1
Tablet, coated	Oral	1 mg/1
Tablet, coated	Oral	2.5 mg/1
Tablet, film coated	Oral	1 mg/1
Tablet, film coated	Oral	2.5 mg/1
Tablet, film coated	Oral	2.50 mg
Tablet	Oral	2.5 mg
Tablet, film coated	Oral	2.5 mg

Prices

Unit description	Cost	Unit
Amerge 9 2.5 mg tablet Box	277.47USD	box
Amerge 9 1 mg tablet Box	275.67USD	box
Amerge 1 mg tablet	32.77USD	tablet
Amerge 2.5 mg tablet	32.77USD	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
US4997841	No	1991-03-05	2010-07-07

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	246 °C (HCl salt)	Not Available
water solubility	35 mg/mL	Not Available
logP	1.6	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.114 mg/mL	ALOGPS
logP	2.16	ALOGPS
logP	1.44	Chemaxon
logS	-3.5	ALOGPS
pKa (Strongest Acidic)	11.55	Chemaxon
pKa (Strongest Basic)	9.18	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	4	Chemaxon
Refractivity	94.26 m3·mol-1	Chemaxon
Polarizability	38 Å3	Chemaxon
Number of Rings	3	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	+	0.9668
Caco-2 permeable	-	0.7657
P-glycoprotein substrate	Substrate	0.6958
P-glycoprotein inhibitor I	Non-inhibitor	0.6055
P-glycoprotein inhibitor II	Non-inhibitor	0.8139
Renal organic cation transporter	Non-inhibitor	0.5982
CYP450 2C9 substrate	Non-substrate	0.8257
CYP450 2D6 substrate	Non-substrate	0.5565
CYP450 3A4 substrate	Substrate	0.6693
CYP450 1A2 substrate	Inhibitor	0.5521
CYP450 2C9 inhibitor	Non-inhibitor	0.9034
CYP450 2D6 inhibitor	Non-inhibitor	0.6785
CYP450 2C19 inhibitor	Non-inhibitor	0.804
CYP450 3A4 inhibitor	Non-inhibitor	0.5914
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.707
Ames test	Non AMES toxic	0.6042
Carcinogenicity	Non-carcinogens	0.8226
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.5630 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Strong inhibitor	0.608
hERG inhibition (predictor II)	Inhibitor	0.6772

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	splash10-0563-6592000000-ddbcdc8fb1564ab67954
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0a4i-0009000000-84e34a57fe2a3792a8dc
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-0009000000-938c8fd42cb3bc2d09cf
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0006-1093000000-e15a2a09f5dc85ea8c7b
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-052r-0097000000-fb5fa1c85cc931972785
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01t9-2091000000-a3b656e9b053c5c77dc6
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-052u-2892000000-dff9f56a028a0118dd70
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]-	198.1950207	predicted	DarkChem Lite v0.1.0
[M-H]-	170.33667	predicted	DeepCCS 1.0 (2019)
[M+H]+	198.9714207	predicted	DarkChem Lite v0.1.0
[M+H]+	172.69467	predicted	DeepCCS 1.0 (2019)
[M+Na]+	198.2612207	predicted	DarkChem Lite v0.1.0
[M+Na]+	178.85826	predicted	DeepCCS 1.0 (2019)

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	45	N/A	N/A	A28741

Details

Binding Properties1. 5-hydroxytryptamine receptor 1A

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 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. Boers PM, Donaldson C, Zagami AS, Lambert GA: Naratriptan has a selective inhibitory effect on trigeminovascular neurones at central 5-HT1A and 5-HT(1B/1D) receptors in the cat: implications for migraine therapy. Cephalalgia. 2004 Feb;24(2):99-109. [Article]
2. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	1.6	N/A	N/A	A28741
Ki (nM)	1.5	N/A	N/A	A28745
Ki (nM)	2.3	N/A	N/A	A28741

Details

Binding Properties2. 5-hydroxytryptamine receptor 1D

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. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine--new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. [Article]
2. Donaldson C, Boers PM, Hoskin KL, Zagami AS, Lambert GA: The role of 5-HT1B and 5-HT1D receptors in the selective inhibitory effect of naratriptan on trigeminovascular neurons. Neuropharmacology. 2002 Mar;42(3):374-85. [Article]
3. Pauwels PJ, Colpaert FC: Selective antagonism of human 5-HT1D and 5-HT1B receptor-mediated responses in stably transfected C6-glial cells by ketanserin and GR 127,935. Eur J Pharmacol. 1996 Apr 4;300(1-2):141-5. [Article]
4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
5. Akin D, Onaran HO, Gurdal H: Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):171-6. [Article]
6. Hoskin KL, Lambert GA, Donaldson C, Zagami AS: The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res. 2004 Feb 13;998(1):91-9. [Article]
7. Boers PM, Donaldson C, Zagami AS, Lambert GA: Naratriptan has a selective inhibitory effect on trigeminovascular neurones at central 5-HT1A and 5-HT(1B/1D) receptors in the cat: implications for migraine therapy. Cephalalgia. 2004 Feb;24(2):99-109. [Article]
8. Johnston MM, Rapoport AM: Triptans for the management of migraine. Drugs. 2010 Aug 20;70(12):1505-18. doi: 10.2165/11537990-000000000-00000. [Article]
9. Dulli DA: Naratriptan: an alternative for migraine. Ann Pharmacother. 1999 Jun;33(6):704-11. [Article]
10. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [Article]
11. Massiou H: Naratriptan. Curr Med Res Opin. 2001;17 Suppl 1:s51-3. [Article]
12. Lambert GA: Preclinical neuropharmacology of naratriptan. CNS Drug Rev. 2005 Autumn;11(3):289-316. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	9.4	N/A	N/A	A28745
Ki (nM)	5.1	N/A	N/A	A28745
Ki (nM)	3.3	N/A	N/A	A28741

Details

Binding Properties3. 5-hydroxytryptamine receptor 1B

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. Akin D, Onaran HO, Gurdal H: Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):171-6. [Article]
2. Hoskin KL, Lambert GA, Donaldson C, Zagami AS: The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res. 2004 Feb 13;998(1):91-9. [Article]
3. Boers PM, Donaldson C, Zagami AS, Lambert GA: Naratriptan has a selective inhibitory effect on trigeminovascular neurones at central 5-HT1A and 5-HT(1B/1D) receptors in the cat: implications for migraine therapy. Cephalalgia. 2004 Feb;24(2):99-109. [Article]
4. 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]
5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
6. Johnston MM, Rapoport AM: Triptans for the management of migraine. Drugs. 2010 Aug 20;70(12):1505-18. doi: 10.2165/11537990-000000000-00000. [Article]
7. Dulli DA: Naratriptan: an alternative for migraine. Ann Pharmacother. 1999 Jun;33(6):704-11. [Article]
8. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [Article]
9. Massiou H: Naratriptan. Curr Med Res Opin. 2001;17 Suppl 1:s51-3. [Article]
10. Lambert GA: Preclinical neuropharmacology of naratriptan. CNS Drug Rev. 2005 Autumn;11(3):289-316. [Article]

Details4. 5-hydroxytryptamine receptor 1F

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
2. Hoskin KL, Lambert GA, Donaldson C, Zagami AS: The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res. 2004 Feb 13;998(1):91-9. [Article]
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Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55