A potent 5-HT1B and 5-HT1D receptor agonist (IC50s = 9.4 and 1.5 nM

Naratriptan (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
143388-64-1
Storage:
-20
UN-No:
Non-Hazardous - /

Naratriptan is a potent agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 9.4 and 1.5 nM, respectively, in a radioligand binding assay using human recombinant receptors).{38513} It is selective for 5-HT1B and 5-HT1D, lacking activity in rat aorta, guinea pig colon, and pig vena cava, that highly express 5-HT2A, 5-HT4, and 5-HT7 receptors, respectively, at concentrations up to 10 μM.{38514} Naratriptan induces contraction of isolated human coronary arteries (EC50 = 170 nM). In vivo, naratriptan (1-300 μg/kg) induces dose-dependent vasoconstriction of the carotid vascular bed in dogs. It also inhibits plasma protein extravasation induced by electrical stimulation of the trigeminal ganglion in the dura of anesthetized rats. Formulations containing naratriptan have been used in the treatment of migraine headaches.  

 

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Description

A potent 5-HT1B and 5-HT1D receptor agonist (IC50s = 9.4 and 1.5 nM, respectively, in a radioligand binding assay using human recombinant receptors); selective for 5-HT1B and 5-HT1D, lacking activity in rat aorta, guinea pig colon, and pig vena cava that highly express 5-HT2A, 5-HT4, and 5-HT7 receptors, respectively, at concentrations up to 10 μM; induces contraction of isolated human coronary arteries (EC50 = 170 nM); induces dose-dependent vasoconstriction of the carotid vascular bed in dogs when administered at doses ranging from 1-300 μg/kg; inhibits plasma protein extravasation induced by electrical stimulation of the trigeminal ganglion in the dura of anesthetized rats,

Formal name: N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulfonamide, monohydrochloride

Synonyms: 

Molecular weight: 371.9

CAS: 143388-64-1

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Cardiovascular System|Vasculature|Vasoconstriction||Research Area|Neuroscience|Pain Research

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