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Titolo:
Cranial vascular effects of zolmitriptan, a centrally active 5-HT1B/1D receptor partial agonist for the acute treatment of migraine
Autore:
MacLennan, SJ; Cambridge, D; Whiting, MV; Marston, C; Martin, GR;
Indirizzi:
Wellcome Res Labs, Receptor Pharmacol Grp, Beckenham BR3 3BS, Kent, England Wellcome Res Labs Beckenham Kent England BR3 3BS m BR3 3BS, Kent, England
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 361, anno: 1998,
pagine: 191 - 197
SICI:
0014-2999(19981120)361:2-3<191:CVEOZA>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTIMIGRAINE DRUG SUMATRIPTAN; BLOOD-FLOW; TRIGEMINOVASCULAR SYSTEM; TRIGEMINAL NEURONS; ERGOT ALKALOIDS; BASILAR ARTERY; DURA-MATER; 311C90; INHIBITION; GR43175;
Keywords:
zolmitriptan; sumatriptan; cranial blood flow distribution; migraine; 5-HT1B/1D receptor agonist;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
40
Recensione:
Indirizzi per estratti:
Indirizzo: MacLennan, SJ Roche401osci, Neurobiol Unit, Biol Res Ctr, Dept Mol Pharmacol, MS R2-101,3 Roche Biosci MS R2-101,3401 Hillview Ave Palo Alto CA USA 94304
Citazione:
S.J. MacLennan et al., "Cranial vascular effects of zolmitriptan, a centrally active 5-HT1B/1D receptor partial agonist for the acute treatment of migraine", EUR J PHARM, 361(2-3), 1998, pp. 191-197

Abstract

The anti-migraine drug zolmitriptan is a novel 5-HT1B/1D receptor partial agonist which, unlike sumatriptan, has been shown to cross the intact blood-brain barrier. in this study we examined whether or not the ability to access the cerebro-vascular intima affects the way in which a centrally-active5-HT1B/1D receptor agonist influences cranial haemodynamics. The effects of zolmitriptan on carotid arterial blood flow distribution were studied in anaesthetised cats using radiolabelled microspheres. Zolmitriptan (10-1000 mu g kg(-1) i.v.) selectively reduced arteriovenous-anastomotic (AVA) conductance producing a maximum decrease of 92.5 +/- 2.3%. The drug also produced a modest reduction in extra-cerebral conductance (23.9 +/- 6.5% maximum reduction at 30 mu g kg(-1), i.v.), but was without effect on cerebral conductance. Using laser doppler flowmetry in anaesthetised cats, zolmitriptan (1-30 mu g kg(-1), i.v.) produced dose-dependent decreases in ear microvascular conductance (15 +/- 5 to 60 +/- 6%) which mirrored decreases in carotidarterial conductance (12 +/- 11 to 61 +/- 5%). By contrast, zolmitriptan at doses up to 1000 mu g kg-l was without effect on cerebral microvascular conductance. Although zolmitriptan crosses the blood-brain barrier and can therefore access the cerebro-vascular intima, this study suggests that this property does not adversely affect cerebrovascular function. (C) 1998 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 14:35:41