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介导鸡大脑半球中3'-5'-环磷酸腺苷变化的肾上腺素能受体的特性分析。

Characterisation of the adrenoceptor mediating changes in cyclic adenosine 3'-5' monophosphate in chick cerebral hemispheres.

作者信息

Nahorski S R, Rogers K J, Smith B M, Anson J

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1975;291(1):101-10. doi: 10.1007/BF00510824.

Abstract

Noradrenaline, adrenaline, isoprenaline and salbutamol induced marked accumulations of cyclic AMP in incubated slices of chick cerebral hemispheres. Isoprenaline was both more potent and more powerful than adrenaline or noradrenaline and the increase in cyclic AMP elicited by the catecholamines was powerfully antagonized by the beta-adrenoceptor antagonist propranolol but not by the alphapadrenoceptor blocker phentolamine. The order of potency of the catecholamines isoprenaline greater than adrenaline greater than noradrenaline and the ability of the non-catechol salbutamol to stimulate cyclic AMP accumulation in chick cerebral slices suggests that the beta-adrenoceptro may resemble that found in the lung (beta2) rather than that in the heart (beta1). Propranolol proved to be a very potent antagonist of the cyclic AMP response induced by isoprenaline in vivo. Beta-adrenoceptor blockade was still evident 12 hrs after a single injection of the durg although only negligible amounts of 3H-propranolol could be detected in cerebral tissue after 2 hrs.

摘要

去甲肾上腺素、肾上腺素、异丙肾上腺素和沙丁胺醇可使孵育的鸡脑半球切片中环状腺苷酸(cAMP)显著积聚。异丙肾上腺素比肾上腺素或去甲肾上腺素更有效且作用更强,儿茶酚胺引起的cAMP增加可被β肾上腺素能受体拮抗剂普萘洛尔强烈拮抗,而α肾上腺素能受体阻滞剂酚妥拉明则无此作用。儿茶酚胺的效力顺序为异丙肾上腺素>肾上腺素>去甲肾上腺素,非儿茶酚类的沙丁胺醇刺激鸡脑切片中cAMP积聚的能力表明,β肾上腺素能受体可能类似于肺中的受体(β2)而非心脏中的受体(β1)。普萘洛尔被证明是体内异丙肾上腺素诱导的cAMP反应的非常有效的拮抗剂。单次注射该药物12小时后,β肾上腺素能受体阻滞仍很明显,尽管2小时后在脑组织中仅能检测到极少量的3H-普萘洛尔。

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