Vayssette J, Vaysse N, Ribet A
Eur J Pharmacol. 1986 Apr 2;122(3):321-8. doi: 10.1016/0014-2999(86)90412-7.
Dispersed acini from dog pancreas were used to characterize dopamine receptors in a study on the stimulation of cellular cyclic AMP formation and the binding of [3H]dopamine. Dopamine elicited concentration-dependent stimulation of cellular cyclic AMP with a maximal increase occurring at a concentration of 0.1 mM (EC50 = 1 microM). Epinine produced a potent stimulation similar to that by dopamine; the alpha-adrenoceptor agonists (amidephrine and noradrenaline) were less potent. Isoproterenol and apomorphine were ineffective. The effect of dopamine was potently blocked by dopamine receptor antagonists such as cis-(Z)-flupenthixol, haloperidol, fluphenazine, whereas spiperone, sulpiride and domperidone were weakly active. Apomorphine acted as an antagonist to inhibit dopamine-stimulated cellular cyclic AMP formation as well as phenoxybenzamine. Yohimbine, prazosin or clonidine were poorly or not active. The affinity of agents to stimulate cellular cyclic AMP formation or to inhibit dopamine-stimulated cellular cyclic AMP formation was closely related to their affinity to inhibit the binding of [3H]dopamine to pancreatic acini, providing evidence that dopamine binding sites are receptors that mediate the action of dopamine on cAMP accumulation. This was further substantiated by the demonstration of specific binding sites for [3H]cis-(Z)-flupenthixol.
在一项关于刺激细胞环磷酸腺苷(cAMP)形成以及[3H]多巴胺结合的研究中,使用了来自狗胰腺的分散腺泡来表征多巴胺受体。多巴胺以浓度依赖性方式刺激细胞cAMP的形成,在浓度为0.1 mM时出现最大增加(半数有效浓度[EC50]=1 microM)。去甲肾上腺素能产生与多巴胺类似的强烈刺激;α-肾上腺素能受体激动剂(酰胺福林和去甲肾上腺素)的效力较弱。异丙肾上腺素和阿扑吗啡无效。多巴胺的作用被多巴胺受体拮抗剂如顺式(Z)-氟哌噻吨、氟哌啶醇、氟奋乃静有效阻断,而螺哌隆、舒必利和多潘立酮的活性较弱。阿扑吗啡与苯氧苄胺一样,作为拮抗剂抑制多巴胺刺激的细胞cAMP形成。育亨宾、哌唑嗪或可乐定的活性较差或无活性。刺激细胞cAMP形成或抑制多巴胺刺激的细胞cAMP形成的药物亲和力与它们抑制[3H]多巴胺与胰腺腺泡结合的亲和力密切相关,这表明多巴胺结合位点是介导多巴胺对cAMP积累作用的受体。[3H]顺式(Z)-氟哌噻吨特异性结合位点的证明进一步证实了这一点。