Release of endogenous benzodiazepine receptor ligands (endozepines) from cultured neurons.
Release of endogenous benzodiazepine receptor ligands (endozepines) from cultured neurons.
复制标题
从培养的神经元中释放内源性苯二氮卓受体配体（内氮卓）。
DOI：
10.1016/0304-3940(92)90267-b
复制
发表时间：
1992
影响因子：
2.5
通讯作者：
Costa,E
中科院分区：
文献类型：
--
作者：
Rothstein,JD;Guidotti,A;Costa,E
内氮卓类药物是天然存在的小有机分子，不含肽键和卤素，通过其在苯二氮卓类结合位点的作用充当 GABAA 受体的变构调节剂。内氮平在大脑中以生理学上显着的量存在，并且可以作为 GABAA 受体的有效正变构调节剂。在这项研究中，发现存在于培养的小脑颗粒细胞中的 3 种内氮平以钾刺激、钙依赖性的方式从神经元中释放。这种释放也可以通过增加藜芦定的浓度来模拟。尽管在培养的星形胶质细胞中也发现了内氮平，但它们不能通过钾去极化而大量释放。去极化条件下的差异释放和各种内托品的颗粒细胞含量表明这两个过程之间可能存在代谢关系。
Endozepines are naturally occurring small organic molecules, devoid of peptidic bonds and halogens, that act as allosteric modulators of the GABAAreceptor through their actions at the benzodiazepine binding site. Endozepines are present in physiologically significant amounts in the brain and can act as potent positive allosteric modulators of the GABAAreceptor. In this study, 3 endozepines present in cultured cerebellar granule cells were found to be released from neurons in a potassium-stimulated, calcium-dependent fashion. This release could also be mimicked by increasing concentrations of veratridine. Although endozepines were also found in cultured astrocytes, they could not be released in significant amounts by potassium depolarization. Differential release under depolarizing conditions and granule cell content of the various endozpeines suggested a possible metabolic relationship between these two processes.