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苯甲酰胺作用于α2 - 肾上腺素能受体可改变儿茶酚胺诱导的豚鼠胃环形平滑肌的收缩和舒张。

Benzamide action at alpha 2-adrenoceptors modifies catecholamine-induced contraction and relaxation of circular smooth muscle from guinea-pig stomach.

作者信息

Sahyoun H A, Costall B, Naylor R J

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):8-11. doi: 10.1007/BF00491470.

Abstract

Dopamine was shown to act on the circular smooth muscle of the stomach body to cause contraction at a yohimbine-sensitive site (alpha 2) and a relaxation at a prazosin-sensitive site (alpha 1). Metoclopramide and tiapride failed to modify either response, failed to antagonise a relaxation to phenylephrine at alpha 1 sites in the same tissue, and failed to modify the contractions caused by dopamine and phenylephrine at an alpha 1-adrenoceptor site in the pyloric sphincter. However, (+)- and (-)-sultopride and (+)-sulpiride antagonised the dopamine-induced contractions of the stomach body indicating an alpha 2-antagonist action. An ability to attenuate the relaxation of this tissue may reflect a displacement of the contraction curve to the right rather than an alpha 1-antagonist action since the response to phenylephrine was not antagonised either in this tissue or in the pyloric sphincter. Within the central nervous system the (-)-enantiomers of sultopride and sulpiride have a highly selective dopamine receptor blocking action. This contrasts with the present findings in the stomach musculature of a non-stereospecific antagonism at alpha 2-type adrenoceptors.

摘要

多巴胺被证明作用于胃体的环形平滑肌,在育亨宾敏感位点(α2)引起收缩,在哌唑嗪敏感位点(α1)引起舒张。甲氧氯普胺和硫必利未能改变任何一种反应,未能拮抗同一组织中α1位点对去氧肾上腺素的舒张作用,也未能改变多巴胺和去氧肾上腺素在幽门括约肌α1肾上腺素能受体位点引起的收缩。然而,(+)-和(-)-舒托必利以及(+)-舒必利拮抗了多巴胺诱导的胃体收缩,表明具有α2拮抗剂作用。减弱该组织舒张的能力可能反映收缩曲线向右移位,而非α1拮抗剂作用,因为在该组织或幽门括约肌中对去氧肾上腺素的反应均未被拮抗。在中枢神经系统内,舒托必利和舒必利的(-)-对映体具有高度选择性的多巴胺受体阻断作用。这与目前在胃肌肉组织中α2型肾上腺素能受体存在非立体特异性拮抗作用的发现形成对比。

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