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Effects of S20749, a close analogue of sumatriptan, on porcine carotid haemodynamics and human isolated coronary artery.
Saxena, P R; Maassen vandenBrink, A; Heiligers, J P; Scalbert, E; Lemaitre, B G.
Afiliación
  • Saxena PR; Department of Pharmacology, Faculty of Medicine and Health Sciences, Erasmus University Rotterdam, Dutch Migraine Research Group, The Netherlands.
Pharmacol Toxicol ; 79(4): 199-204, 1996 Oct.
Article en En | MEDLINE | ID: mdl-8899861
ABSTRACT
Several acutely acting antimigraine drugs, including sumatriptan and other second generation 5-HT1D receptor agonists, have the ability to constrict porcine arteriovenous anastomoses. Sumatriptan also constricts the human isolated coronary artery. These two experimental models seem to serve as indicators, respectively, for the therapeutic and coronary side-effect potential of the compounds. Using these two models, we have now investigated the effects of S20749 (1-[2-(dimethylamino)ethyl]-naphthalene-7-methylsulfonamide), a close analogue of sumatriptan. S20749 (30, 100, 300 and 1000 micrograms.kg-1) decreased the total carotid blood flow by exclusively decreasing arteriovenous anastomotic blood flow; capillary blood flow was moderately increased. These changes were statistically significant with the highest two doses. S20749 moderately constricted the human isolated coronary artery (pD2 < or = 4.5 Fmax > 11% of the contraction to 100 mM K+). The above results suggest that S20749 should be able to abort migraine headaches in patients.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Anastomosis Arteriovenosa / Arterias Carótidas / Agonistas de Receptores de Serotonina / Sumatriptán / Vasos Coronarios / Naftalenos Límite: Animals / Humans Idioma: En Revista: Pharmacol Toxicol Asunto de la revista: FARMACOLOGIA / TOXICOLOGIA Año: 1996 Tipo del documento: Article País de afiliación: Países Bajos
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Anastomosis Arteriovenosa / Arterias Carótidas / Agonistas de Receptores de Serotonina / Sumatriptán / Vasos Coronarios / Naftalenos Límite: Animals / Humans Idioma: En Revista: Pharmacol Toxicol Asunto de la revista: FARMACOLOGIA / TOXICOLOGIA Año: 1996 Tipo del documento: Article País de afiliación: Países Bajos