The canine external carotid vasoconstrictor 5-HT₁ receptor: blockade by 5-HT_1B (SB224289), but not by 5-HT_1D (BRL15572) receptor antagonists

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• 作者：De Vries ; Peter ; Sá ; nchez-Ló ; pez ; Araceli ; Centurió ; n ; David ; Heiligers ; Jan P.C. ; et. al.
• 关键词：5-HT_1B receptor ; BRL15572 ; Carotid vasoconstriction ; canine ; external ; SB224289 ; Sumatriptan
• 刊名：European Journal of Pharmacology
• 出版年：1998
• 出版时间：November 27, 1998
• 年：1998
• 卷：362
• 期：1
• 页码：69-72
• 全文大小：114 K

文摘

In vagosympathectomised dogs pre-treated intravenously (i.v.) with mesulergine (300 μg/kg), 1-min intracarotid (i.c.) infusions of 5-hydroxytryptamine (5-HT; 0.3–30 μg/min) and sumatriptan (1–30 μg/min) dose-dependently decreased external carotid blood flow, without affecting mean blood pressure or heart rate. Treatment with the selective 5-HT_1B receptor antagonist SB224289 (2,3,6,7-tetrahydro-1′-methyl-5-[2′-methyl-4′(5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-carbonyl]furo[2,3f]indole-3-spiro-4′-piperidine hydrochloride; 30–300 μg/kg, i.v.) produced a potent, specific and dose-dependent blockade of this response, whereas the selective 5-HT_1D receptor antagonist BRL15572 (1-(3-chlorophenyl)-4-[3,3-diphenyl(2-(S,R) hydroxypropanyl)piperazine]hydrochloride; 30–300 μg/kg, i.v.) was ineffective. It is concluded that mainly 5-HT_1B, but not 5-HT_1D receptors mediate the canine external carotid vasoconstriction by 5-HT and sumatriptan.