神经组织中对血清素敏感的腺苷酸环化酶及其与血清素受体的相似性：麦角酸二乙酰胺可能的作用位点。
Serotonin-sensitive adenylate cyclase in neural tissue and its similarity to the serotonin receptor: a possible site of action of lysergic acid diethylamide.
作者信息
Nathanson J A, Greengard P
出版信息
Proc Natl Acad Sci U S A. 1974 Mar;71(3):797-801. doi: 10.1073/pnas.71.3.797.
Abstract
An adenylate cyclase (EC 4.6.1.1) that is activated specifically by low concentrations of serotonin has been identified in homogenates of the thoracic ganglia of an insect nervous system. The activation of this enzyme by serotonin was selectively inhibited by extremely low concentrations of D-lysergic acid diethylamide (LSD), 2-bromo-LSD, and cyproheptadine, agents which are known to block certain serotonin receptors in vivo. The inhibition was competitive with respect to serotonin, and the calculated inhibitory constant of LSD for this serotonin-sensitive adenylate cyclase was 5 nM. The data are consistent with a model in which the serotonin receptor of neural tissue is intimately associated with a serotonin-sensitive adenylate cyclase which mediates serotonergic neurotransmission. The results are also compatible with the possibility that some of the physiological effects of LSD may be mediated through interaction with serotonin-sensitive adenylate cyclase.
摘要
在一种昆虫神经系统的胸神经节匀浆中，已鉴定出一种腺苷酸环化酶（EC 4.6.1.1），它能被低浓度的血清素特异性激活。血清素对该酶的激活作用被极低浓度的D-麦角酸二乙酰胺（LSD）、2-溴-LSD和赛庚啶选择性抑制，这些试剂在体内已知能阻断某些血清素受体。这种抑制作用对血清素而言是竞争性的，计算得出LSD对这种血清素敏感的腺苷酸环化酶的抑制常数为5 nM。这些数据与一个模型相符，在该模型中神经组织的血清素受体与介导血清素能神经传递的血清素敏感腺苷酸环化酶紧密相关。这些结果也与LSD的某些生理效应可能通过与血清素敏感腺苷酸环化酶相互作用介导的可能性相一致。
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