An agonist of 5-HT1B and 5-HT1D receptors (Kis = 2.51 and 3.98 nM

Frovatriptan (succinate hydrate) – 50 mg

Brand:
Cayman
CAS:
158930-17-7
Storage:
-20
UN-No:
Non-Hazardous - /

Frovatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 2.51 and 3.98 nM, respectively).{45320,45319} It is selective for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2C, 5-HT3, and 5-HT7 receptors, as well as dopamine D1, D2, and D3, histamine H1, and α1-adrenergic receptors (Kis = >50 nM). Frovatriptan induces contractions in human basilar arteries isolated post-mortem, coronary arteries from transplant recipient hearts, and coronary arteries from donor hearts unsuitable for transplantation (EC50s = 13.8, 41.69, and 15.49 nM, respectively).{45321} It increases carotid vascular resistance in closed-chest and open-chest anesthetized dogs (ED50s = 6 and 1 nmol/kg, i.v., respectively).{45322} Formulations containing frovatriptan have been used in the treatment of migraines.  

 

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Description

An agonist of 5-HT1B and 5-HT1D receptors (Kis = 2.51 and 3.98 nM, respectively); selective for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2C, 5-HT3, and 5-HT7 receptors, as well as dopamine D1, D2, and D3, histamine H1, and α1-adrenergic receptors (Kis = >50 nM); induces contractions in human basilar arteries isolated post-mortem, coronary arteries from transplant recipient hearts, and coronary arteries from donor hearts unsuitable for transplantation (EC50s = 13.8, 41.69, and 15.49 nM, respectively); increases carotid vascular resistance in closed-chest and open-chest anesthetized dogs (ED50s = 6 and 1 nmol/kg, i.v., respectively)

Formal name: butanedioic acid, compd. with (R)-2,3,4,9-tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide, hydrate (1:1:1)

Synonyms: 

Molecular weight: 379.4

CAS: 158930-17-7

Purity: ≥98%

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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