Rodríguez C, Martí-Bonmati E, Esplugues J V, Brage R, Esplugues J
Methods Find Exp Clin Pharmacol. 1986 Jul;8(7):403-6.
The present investigation was carried out to compare the effects of pirenzepine, a novel antimuscarinic drug, with those elicited by atropine and propantheline on gastric acid secretion and gastric emptying in the conscious rat. The administration of all three drugs resulted in a dose-related inhibition on both parameters that at large doses was nearly total. Comparison of the ID50 ratios for each antagonist on gastric emptying versus acid secretion showed that pirenzepine was unique in that it selectively inhibited acid secretion. Its potency on acid secretion was about 15 times higher than that elicited on gastric emptying. The results are compatible with the proposed existence of two different classes of gastric muscarinic receptors mediating secretory and motor activities.
本研究旨在比较新型抗毒蕈碱药物哌仑西平与阿托品和丙胺太林对清醒大鼠胃酸分泌和胃排空的影响。给予这三种药物均导致这两个参数呈剂量依赖性抑制,大剂量时几乎完全抑制。比较每种拮抗剂对胃排空与胃酸分泌的半数抑制剂量(ID50)比值表明,哌仑西平的独特之处在于它选择性地抑制胃酸分泌。其对胃酸分泌的效力比对胃排空的效力高约15倍。这些结果与所提出的存在两类不同的胃毒蕈碱受体介导分泌和运动活动的观点相符。