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溴隐亭(CB - 154)对“调节性”多巴胺受体的刺激作用。

Stimulation of "regulatory" dopamine receptors by bromocriptine (CB-154).

作者信息

Di Chiara G, Porceddu M L, Vargiu L, Gessa G L

出版信息

Pharmacology. 1978;16 Suppl 1:135-42. doi: 10.1159/000136814.

Abstract

Bromocriptine produces long-lasting hypomotility and decreases brain dihydroxyphenylacetic acid (DOPAC) in mice. These effects are obtained with doses much lower than those which produce hypermotility. The decrease of brain DOPAC is correlated to the hypomotility both on a dose and on a time basis. Potent DA receptor blockers as pimozide, benzperidol and droperidol antagonize the hypomotility and the decrease of brain DOPAC produced by bromocriptine. These effects are obtained with very low doses (0.05-0.3 mg/kg) of neuroleptics which per se do not affect motility or brain DOPAC. The maximal decrease of brain DOPAC produced by bromocriptine is similar to that produced by apomorphine and the combination of these drugs does not result in a further decrease. On the basis of these results it is postulated that bromocriptine decreases DA turnover and produces hypomotility by acting on "regulatory" DA receptors different from the postsynaptic ones of the "terminal" dopaminergic areas.

摘要

溴隐亭可使小鼠产生持久的运动迟缓,并降低其脑内二羟基苯乙酸(DOPAC)水平。产生这些效应所需的剂量远低于引起运动亢进的剂量。脑内DOPAC的降低在剂量和时间上均与运动迟缓相关。强效多巴胺受体阻滞剂如匹莫齐特、苯哌利多和氟哌利多可拮抗溴隐亭引起的运动迟缓及脑内DOPAC的降低。这些效应可通过极低剂量(0.05 - 0.3毫克/千克)的抗精神病药物获得,这些药物本身并不影响运动或脑内DOPAC。溴隐亭引起的脑内DOPAC的最大降低幅度与阿扑吗啡引起的相似,且这两种药物联合使用不会导致进一步降低。基于这些结果,推测溴隐亭通过作用于不同于“终末”多巴胺能区域突触后受体的“调节性”多巴胺受体来降低多巴胺周转率并产生运动迟缓。

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Evidence for selective and long-lasting stimulation of "regulatory" dopamine-receptors by bromocriptine (CB 154).
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A comparison of the potencies of various dopamine receptor agonists in models for pre- and postsynaptic receptor activity.
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