Sahyoun H A, Costall B, Naylor R J
Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):8-11. doi: 10.1007/BF00491470.
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.
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。