Polans A S, Hutchins J B, Werblin F S
Brain Res. 1985 Aug 12;340(2):355-62. doi: 10.1016/0006-8993(85)90932-1.
The pharmacology and autoradiographic localization of muscarinic cholinergic receptors in retinal slices of the larval tiger salamander have been examined using the muscarinic antagonist [3H]propylbenzilylcholine mustard. Under the conditions of these experiments the binding of this ligand is irreversible. Saturation and maximum specific binding of 270 pM of ligand per gram protein are observed after an incubation of 1 h, and autoradiographic studies show that this does not reflect surface binding alone. Muscarinic but not nicotinic drugs suppress the binding of propylbenzilylcholine mustard at physiologically relevant concentrations; half-maximal suppression of binding by the muscarinic antagonists atropine sulfate and quinuclidinyl benzilate occurs, respectively, at 9.0 and 7.5 X 10(-10) M. Light microscopic autoradiography reveals the discrete localization of the ligand to the sites of synaptic contact, the retinal plexiform layers, predominantly the inner plexiform layer. The implications of the present study on current theories of cholinergic function in the vertebrate retina are discussed.
利用毒蕈碱拮抗剂[3H]丙基苯甲酰胆碱氮芥,对虎纹钝口螈幼体视网膜切片中毒蕈碱胆碱能受体的药理学和放射自显影定位进行了研究。在这些实验条件下,该配体的结合是不可逆的。孵育1小时后,观察到每克蛋白质270 pM配体的饱和结合和最大特异性结合,放射自显影研究表明,这并非仅反映表面结合。在生理相关浓度下,毒蕈碱而非烟碱类药物可抑制丙基苯甲酰胆碱氮芥的结合;硫酸阿托品和苯环喹酯这两种毒蕈碱拮抗剂对结合的半数最大抑制浓度分别为9.0和7.5×10(-10)M。光学显微镜放射自显影显示,配体在突触接触部位、视网膜神经纤维层(主要是内神经纤维层)有离散定位。本文研究对脊椎动物视网膜胆碱能功能当前理论的意义进行了讨论。