Zelles T, Harsing L G, Vizi E S
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest.
Eur J Pharmacol. 1990 Mar 13;178(1):101-4. doi: 10.1016/0014-2999(90)94799-4.
The release of [3H]acetylcholine [( 3H]ACh) from Auerbach's plexus and the contraction of longitudinal muscle strips in response to the administration of cholecystokinin (CCK) were measured and recorded simultaneously. The peripheral CCK receptor antagonist, 3S(-)-N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-yl)-1H- indole-2-carboxamide (L-364,718), antagonized the ACh releasing effect of CCK in a dose-dependent manner. The IC50 value and the dissociation constant (KD) were 41.0 +/- 2.0 pM and 0.06 +/- 0.01 nM, respectively. These results suggest that L-364,718 is a very potent antagonist of the neuronal CCK receptors.
同时测量并记录了[3H]乙酰胆碱（[3H]ACh）从奥尔巴赫神经丛的释放以及胆囊收缩素（CCK）给药后纵行肌条的收缩情况。外周CCK受体拮抗剂3S(-)-N-(2,3-二氢-1-甲基-2-氧代-5-苯基-1H-1,4-苯并二氮杂䓬-3-基)-1H-吲哚-2-甲酰胺（L-364,718）以剂量依赖性方式拮抗CCK的ACh释放作用。IC50值和解离常数（KD）分别为41.0±2.0 pM和0.06±0.01 nM。这些结果表明L-364,718是神经元CCK受体的一种非常有效的拮抗剂。
