Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan.

Abstract:

OBJECTIVE:To determine the pharmacological profile of frovatriptan. BACKGROUND:Frovatriptan is a new 5-HT(1B/1D) agonist developed for the treatment of migraine. METHODS:Pharmacological studies were performed using in vitro and in vivo techniques. RESULTS:Radioligand-binding studies showed that frovatriptan has a high affinity for 5-HT(1B) and 5-HT(1D) receptors, and moderate affinity for 5-HT(1A), 5-HT(1F), and 5-HT(7) receptors. In vitro, frovatriptan acts as a potent full agonist at human cloned 5-HT(1B) and 5-HT(1D) receptors, and as a moderately potent full agonist at 5-HT(7) receptors. Studies of frovatriptan in isolated human arteries demonstrated a lower threshold for constriction of cerebral than coronary vasculature and a bell-shaped dose-response curve was apparent in the coronary arteries. In anesthetized dogs, frovatriptan administration produced no measurable effect on cardiac function or on blood pressure. Frovatriptan had no effects on coronary blood flow following transient coronary artery occlusion, whereas sumatriptan produced a prolonged and significant decrease in coronary blood flow. CONCLUSION:The pharmacology of frovatriptan suggests that it should be an effective agent for the acute treatment of migraine, with a low potential for undesirable peripheral effects.

journal_name

Headache

journal_title

Headache

authors

Comer MB

doi

10.1046/j.1526-4610.42.s2.2.x

keywords:

subject

Has Abstract

pub_date

2002-04-01 00:00:00

pages

S47-53

eissn

0017-8748

issn

1526-4610

pii

hed02067

journal_volume

42 Suppl 2

pub_type

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