Ticku M, Mehta A, Lehoullier P
Department of Pharmacology, University of Texas Health Science Center, San Antonio 78284-7764.
Adv Biochem Psychopharmacol. 1988;45:151-9.
In summary, spinal cord cultured neurons provide an in vitro model for studying GABA synaptic pharmacology. GABAA agonists stimulate 36Cl-influx in these cells in a concentration-dependent manner. The enhancing effect of GABA is potentiated by BZ agonists, inhibited by GABA antagonists, and attenuated by the inverse agonist beta-carboline, DMCM. These cells also exhibit the specific binding of [3H]flunitrazepam with a pharmacological specificity of the central BZ receptors. Finally, BZ receptors are coupled to GABA, barbiturate, and picrotoxin sites in these cells, as indicated by allosteric interactions both by binding and 36Cl-influx assay.
总之，脊髓培养神经元为研究GABA突触药理学提供了一个体外模型。GABAA激动剂以浓度依赖的方式刺激这些细胞中的36Cl内流。GABA的增强作用被苯二氮卓类激动剂增强，被GABA拮抗剂抑制，并被反向激动剂β-咔啉、DMCM减弱。这些细胞还表现出[3H]氟硝西泮的特异性结合，具有中枢苯二氮卓类受体的药理学特异性。最后，如结合和36Cl内流测定的变构相互作用所示，苯二氮卓类受体在这些细胞中与GABA、巴比妥类和印防己毒素位点偶联。
