Itonaga M, Uruno T, Kubota K
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
Jpn J Pharmacol. 1988 Apr;46(4):319-24. doi: 10.1254/jjp.46.319.
Two beta-carboline esters, methyl or ethyl beta-carboline-3-carboxylate, beta-CCM and beta-CCE, were found to antagonize the antinociceptive and satiety action of the sulfated octapeptide cholecystokinin (CCK8) which was administered intracisternally to mice. beta-CCM did not affect the antinociception induced by morphine. The two beta-carboline esters weakly inhibited the food intake in mice. However, when they were administered after CCK8 administration, they reversed the CCK8-induced satiety. Since the two beta-carboline esters have been previously shown to act as selective cholecystokinin (CCK) receptor antagonists in the isolated guinea-pig gallbladder muscle, they are suggested to antagonize the central action of CCK through acting on the CCK receptor in the central nervous system. The results obtained from the present paper also suggest that benzodiazepine receptor ligands seem in general to act as CCK receptor antagonists as well.
两种β-咔啉酯，即β-咔啉-3-羧酸甲酯和乙酯（β-CCM和β-CCE），被发现可拮抗硫酸化八肽胆囊收缩素（CCK8）对小鼠脑池内给药后的镇痛和饱腹感作用。β-CCM不影响吗啡诱导的镇痛作用。这两种β-咔啉酯对小鼠的食物摄入量有微弱抑制作用。然而，当它们在CCK8给药后给药时，可逆转CCK8诱导的饱腹感。由于这两种β-咔啉酯先前已被证明在离体豚鼠胆囊肌中可作为选择性胆囊收缩素（CCK）受体拮抗剂，因此提示它们通过作用于中枢神经系统中的CCK受体来拮抗CCK的中枢作用。本文获得的结果还表明，苯二氮䓬受体配体似乎通常也可作为CCK受体拮抗剂。
