MacDonald J F, Barker J L, Paul S M, Marangos P J, Skolnick P
Science. 1979 Aug 17;205(4407):715-7. doi: 10.1126/science.37602.
Mouse spinal neurons grown in tissue culture were used to study the membrane effects of the benzodiazepine flurazepam and the naturally occurring purine nucleoside inosine, which competes for benzodiazepine receptor sites in the central nervous system. Application of inosine elicited two types of transmitter-like membrane effects: a rapidly desensitizing excitatory response and a nondesensitizing inhibitory response. Flurazepam produced a similar excitatory response which showed cross-desensitization with the purine excitation. Flurazepam also blocked the inhibitory inosine response. The results provide electrophysiological evidence that an endogenous purine can activate two different conductances on spinal neurons and that flurazepam can activate one of the conductances and antagonize the other.
在组织培养中生长的小鼠脊髓神经元被用于研究苯二氮䓬类药物氟西泮和天然存在的嘌呤核苷肌苷对膜的影响,肌苷在中枢神经系统中与苯二氮䓬受体位点竞争。应用肌苷引发了两种类似递质的膜效应:一种快速脱敏的兴奋性反应和一种非脱敏的抑制性反应。氟西泮产生了类似的兴奋性反应,该反应与嘌呤激发表现出交叉脱敏。氟西泮还阻断了肌苷的抑制性反应。这些结果提供了电生理证据,即内源性嘌呤可以激活脊髓神经元上两种不同的电导,并且氟西泮可以激活其中一种电导并拮抗另一种电导。