Humphrey P P
Br J Pharmacol. 1978 Aug;63(4):671-5. doi: 10.1111/j.1476-5381.1978.tb17281.x.
1 5-Hydroxytryptamine (5-HT) contracted isolated saphenous vein strips of the dog, producing a biphasic concentration-effect curve. The first phase occurred with low concentrations of 5-HT (1.0 X 10(-8) TO 5.0 X 10(-6) mol/l) with a plateau between 1.0 x 10(-6) mol/l and 1.0 x 10(-5) mol/l. The second phase occurred with high concentrations of 5-HT (greater than 1.0 x 10(-5) mol/l). 2 The alpha-adrenoceptor antabonists, phentolamine (5.0 x 10(-8) to 5.0 x 10(-7) mol/l), labetalol (1.0 x 10(-6) to 1.0 x 10(-5) mol/l) and thymoxamine (1.0 x 10(-6) to 1.0 x 10(-5) mol/l), antagonized responses to high concentrations of 5-HT but responses to low concentrations of 5-HT were not antagonized. 3 The effects of high concentrations of 5-HT were antagonized by cocaine (1.0 x 10(-6) to 1.0 x 10(-5) mol/l) and were not evident in veins removed from dogs pretreated with syrosingopine. 5-HT receptors and that high concentrations of 5-HT also act indirectly on alpha-adrenoceptors by displacing noradrenaline from neuronal stores.
5-羟色胺(5-HT)使犬的离体隐静脉条收缩,产生双相浓度-效应曲线。第一相出现在低浓度5-HT(1.0×10⁻⁸至5.0×10⁻⁶mol/L)时,在1.0×10⁻⁶mol/L至1.0×10⁻⁵mol/L之间出现平台期。第二相出现在高浓度5-HT(大于1.0×10⁻⁵mol/L)时。
α-肾上腺素能受体拮抗剂酚妥拉明(5.0×10⁻⁸至5.0×10⁻⁷mol/L)、拉贝洛尔(1.0×10⁻⁶至1.0×10⁻⁵mol/L)和噻吗洛尔(1.0×10⁻⁶至1.0×10⁻⁵mol/L)可拮抗高浓度5-HT的反应,但不拮抗低浓度5-HT的反应。
高浓度5-HT的作用可被可卡因(1.0×10⁻⁶至1.0×10⁻⁵mol/L)拮抗,在用萝芙木碱预处理的犬所取的静脉中不明显。5-HT受体,且高浓度5-HT还通过从神经储存部位置换去甲肾上腺素而间接作用于α-肾上腺素能受体。