犬类颈外动脉血管收缩5-羟色胺1型受体：被5-羟色胺1B型（SB224289）而非5-羟色胺1D型（BRL15572）受体拮抗剂阻断。
The canine external carotid vasoconstrictor 5-HT1 receptor: blockade by 5-HT1B (SB224289), but not by 5-HT1D (BRL15572) receptor antagonists.
作者信息
De Vries P, Sánchez-López A, Centurión D, Heiligers J P, Saxena P R, Villalón C M
机构信息
Department of Pharmacology, Cardiovascular Research Institute COEUR, Faculty of Medicine and Health Sciences, Erasmus University Rotterdam, The Netherlands.
出版信息
Eur J Pharmacol. 1998 Nov 27;362(1):69-72. doi: 10.1016/s0014-2999(98)00762-6.
In vagosympathectomised dogs pre-treated intravenously (i.v.) with mesulergine (300 microg/kg), 1-min intracarotid (i.c.) infusions of 5-hydroxytryptamine (5-HT; 0.3-30 microg/min) and sumatriptan (1-30 microg/min) dose-dependently decreased external carotid blood flow, without affecting mean blood pressure or heart rate. Treatment with the selective 5-HT1B receptor antagonist SB224289 (2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4'(5-methyl-1,2,4-oxadiazo l-3-yl) biphenyl-4-carbonyl]furo[2,3f]indole-3-spiro-4'-piperidine hydrochloride; 30-300 microg/kg, i.v.) produced a potent, specific and dose-dependent blockade of this response, whereas the selective 5-HT1D receptor antagonist BRL15572 (1-(3-chlorophenyl)-4-[3,3-diphenyl(2-(S,R) hydroxypropanyl)piperazine]hydrochloride; 30-300 microg/kg, i.v.) was ineffective. It is concluded that mainly 5-HT1B, but not 5-HT1D receptors mediate the canine external carotid vasoconstriction by 5-HT and sumatriptan.
在预先经静脉注射美舒麦角（300微克/千克）进行预处理的去迷走神经交感神经犬中，颈内动脉内1分钟输注5-羟色胺（5-HT；0.3 - 30微克/分钟）和舒马曲坦（1 - 30微克/分钟）剂量依赖性地降低颈外动脉血流，而不影响平均血压或心率。用选择性5-HT1B受体拮抗剂SB224289（2,3,6,7-四氢-1'-甲基-5-[2'-甲基-4'（5-甲基-1,2,4-恶二唑-3-基）联苯-4-羰基]呋喃并[2,3f]吲哚-3-螺-4'-哌啶盐酸盐；30 - 300微克/千克，静脉注射）治疗产生了对该反应的强效、特异性和剂量依赖性阻断，而选择性5-HT1D受体拮抗剂BRL15572（1-（3-氯苯基）-4-[3,3-二苯基（2-（S，R）-羟基丙基）哌嗪]盐酸盐；30 - 300微克/千克，静脉注射）无效。得出的结论是，主要是5-HT1B受体而非5-HT1D受体介导5-HT和舒马曲坦引起的犬颈外动脉血管收缩。
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