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α-肾上腺素能受体拮抗剂和甲硫米特对幼鼠可乐定诱导的运动刺激的影响。

The effect of alpha-adrenoceptor antagonists and metiamide on clonidine-induced locomotor stimulation in the infant rat.

作者信息

Nomura Y, Segawa T

出版信息

Br J Pharmacol. 1979 Aug;66(4):531-5. doi: 10.1111/j.1476-5381.1979.tb13691.x.

Abstract

1 Subcutaneous injections of clonidine (3.9 X 10(-8) mol/kg to 3.9 X 10(-6) mol/kg) produced forward locomotion and wall climbing in 7-day-old rats in a dose-dependent manner. 2 The effect was reduced significantly by a preceding intraperitoneal injection of phentolamine (7.9 X 10(-6) mol/kg), phenoxybenzamine (7.4 X 10(-6) mol/kg), yohimbine (1.3 X 10(-6) mol/kg) or piperoxan (7.4 X 10(-6) mol/kg). 3 The pA2-values of the antagonists to the clonidine-induced locomotor hyperactivity were: 5.1 (phenoxybenzamine), 5.2 (phentolamine), 6.4 (yohimbine) and 6.0 (piperoxan). 4 Metiamide (2.5 X 10(-4) mol/kg, 5.0 X 10(-4) mol/kg and 1.0 X 10(-3) mol/kg), a histamine H2-receptor blocker, did not affect the clonidine-induced locomotor stimulation. 5 It is suggested that the receptors which mediate clonidine-induced locomotor stimulation could be alpha-adrenoceptors but not histamine H2-receptors in the central nervous system of the infant rat.

摘要
  1. 皮下注射可乐定(3.9×10⁻⁸摩尔/千克至3.9×10⁻⁶摩尔/千克)可使7日龄大鼠产生向前运动和爬壁行为,且呈剂量依赖性。2. 预先腹腔注射酚妥拉明(7.9×10⁻⁶摩尔/千克)、酚苄明(7.4×10⁻⁶摩尔/千克)、育亨宾(1.3×10⁻⁶摩尔/千克)或哌罗克生(7.4×10⁻⁶摩尔/千克)可显著降低该效应。3. 这些拮抗剂对可乐定诱导的运动性多动的pA2值分别为:5.1(酚苄明)、5.2(酚妥拉明)、6.4(育亨宾)和6.0(哌罗克生)。4. 组胺H2受体阻滞剂甲硫米特(2.5×10⁻⁴摩尔/千克、5.0×10⁻⁴摩尔/千克和1.0×10⁻³摩尔/千克)不影响可乐定诱导的运动刺激。5. 提示在幼鼠中枢神经系统中,介导可乐定诱导的运动刺激的受体可能是α-肾上腺素能受体而非组胺H2受体。

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