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β2 -肾上腺素能受体激动剂克仑特罗和沙丁胺醇通过中枢机制增强8 -羟基-2 -(二正丙基氨基)四氢萘(8 - OH - DPAT)对小鼠的降温作用。

The beta 2-adrenoceptor agonists clenbuterol and salbutamol enhance the hypothermic action of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) in mice by a central mechanism.

作者信息

Green A R, Goodwin G M, De Souza R J, Heal D J

出版信息

Neuropharmacology. 1986 Jan;25(1):21-4. doi: 10.1016/0028-3908(86)90053-5.

Abstract

The hypothermic response of mice to injection of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) was enhanced by injection of the beta 2-adrenoceptor agonist clenbuterol with an ED50 of 0.4 mg/kg. This effect of clenbuterol is through a central mechanism since salbutamol, a beta 2-adrenoceptor agonist with poor penetration into the brain, had no effect at a dose of 2 mg/kg, whereas intracerebroventricular injection of clenbuterol (3 micrograms) or salbutamol (2 micrograms), produced a significant enhancement. The enhancing effect of clenbuterol was unaffected by pretreatment with the beta 1-adrenoceptor antagonist metoprolol but was totally antagonised by the beta 2-adrenoceptor antagonist ICI 118,551 and to a lesser extent by butoxamine. Clenbuterol therefore enhances the function of the presynaptic 5-HT1 receptor through a beta 2-adrenoceptor mechanism.

摘要

给小鼠注射β2肾上腺素能受体激动剂克仑特罗(剂量为0.4mg/kg,半数有效量)可增强其对注射8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)的低温反应。克仑特罗的这种作用是通过中枢机制实现的,因为对脑内穿透力差的β2肾上腺素能受体激动剂沙丁胺醇在剂量为2mg/kg时无作用,而脑室内注射克仑特罗(3微克)或沙丁胺醇(2微克)则产生显著增强作用。克仑特罗的增强作用不受β1肾上腺素能受体拮抗剂美托洛尔预处理的影响,但完全被β2肾上腺素能受体拮抗剂ICI 118,551拮抗,且被丁氧胺部分拮抗。因此,克仑特罗通过β2肾上腺素能受体机制增强突触前5-HT1受体的功能。

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