IN VITRO STUDIES ON THE PUTATIVE DOPAMINE AUTORECEPTOR AGONIST, B-HT 920

假定的多巴胺自身受体激动剂 B-HT 920 的体外研究

• 批准号: 4694638
• 负责人: C J SCHMIDT
• 金额: --
• 依托单位: NATIONAL HEART, LUNG, AND BLOOD INSTITUTE
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/4694638
• 关键词: antiadrenergic agents; antidepressants; cell population study; chemical stimulation; neuropharmacology; neurotransmitter metabolism; potassium; synapses; tissue /cell culture

Results from numerous in vivo studies have suggested that a new dopamine agonist, B-HT 920, may be selective for stimulation of dopamine autoreceptors. To examine this question, the inhibition of K+stimulated [3H] dopamine and [14C]acetycholine release was used as an in vitro measure of presynaptic and postsynaptic dopamine receptor stimulation, respectively. In contrast to the results of in vivo studies, B-HT 920 was found to be a potent agonist at both pre- and postsynaptic dopamine recetors. Both effects of B-HT 920 were stereospecific and antagnoized by the D2 dopamine antagonist, sulpiride, while the alpha antagonist, tolazoline, was without effect. The presynaptic effect of B-HT 920 was selective to dopamine neurons in that K+-stimulated [3H]serotonin release was not affected.

大量体内研究的结果表明，一种新的多巴胺 激动剂B-HT 920可能对多巴胺的刺激具有选择性 自体感受器 为了验证这个问题，抑制K+刺激 [3H]多巴胺和[14 C]乙酰胆碱释放被用作体外测量 突触前和突触后多巴胺受体的刺激， 分别 与体内研究结果相反，B-HT 920 被发现是突触前和突触后多巴胺的有效激动剂 朗诵者 B-HT 920的这两种作用都是立体特异性的，并且通过 D2多巴胺拮抗剂舒必利，而α拮抗剂， 妥拉唑啉无效。 B-HT 920的突触前效应是 在K+刺激的[3 H]血清素释放中对多巴胺神经元具有选择性， 没有受到影响。