Blandizzi C, Bernardini M C, Natale G, Del Tacca M
Institute of Pharmacology, School of Medicine and Dentistry, University of Pisa, Italy.
Pharmacology. 1991;42(3):128-34. doi: 10.1159/000138789.
The present study investigates the effects of centrally or peripherally administered baclofen on gastric acid secretion from pylorus-ligated rats. The influence of baclofen on basal acid secretion from isolated guinea-pig gastric fundus was also evaluated. At all doses employed, intracerebroventricular baclofen significantly decreased acid secretion, this inhibitory action being antagonized by intracerebroventricular phaclofen. Intravenous baclofen induced both gastric inhibitory and excitatory responses at low and high doses, respectively. Intracerebroventricular phaclofen prevented the inhibitory effect, while neither intracerebroventricular nor intravenous phaclofen modified the stimulant action of parenteral baclofen. Both central and parenteral muscimol did not influence gastric acid secretion. Moreover, baclofen or muscimol were without effect on basal acid secretion from isolated guinea-pig gastric fundus, whereas bethanechol caused a marked and concentration-dependent stimulant action. The present results provide further evidence for the inhibitory role of central phaclofen-sensitive GABA-B receptors in the regulation of acid secretion. In addition they indicate that the hypersecretory effect exerted by parenteral baclofen may depend upon the activation of putative peripheral non-A and phaclofen-insensitive GABA-B receptors. Finally, peripheral GABA receptors do not appear to be significantly involved in the direct control of gastric secretion.
本研究调查了中枢或外周给予巴氯芬对幽门结扎大鼠胃酸分泌的影响。还评估了巴氯芬对分离的豚鼠胃底基础酸分泌的影响。在所使用的所有剂量下,脑室内注射巴氯芬均显著降低酸分泌,这种抑制作用可被脑室内注射苯氯芬拮抗。静脉注射巴氯芬在低剂量和高剂量时分别诱导胃抑制和兴奋反应。脑室内注射苯氯芬可防止这种抑制作用,而脑室内或静脉注射苯氯芬均不能改变胃肠外给予巴氯芬的刺激作用。中枢和胃肠外给予的蝇蕈醇均不影响胃酸分泌。此外,巴氯芬或蝇蕈醇对分离的豚鼠胃底基础酸分泌无影响,而氨甲酰甲胆碱则引起明显的浓度依赖性刺激作用。本研究结果为中枢苯氯芬敏感的γ-氨基丁酸B型(GABA-B)受体在酸分泌调节中的抑制作用提供了进一步证据。此外,研究结果表明胃肠外给予巴氯芬产生的胃酸分泌过多效应可能取决于假定的外周非A类和苯氯芬不敏感的GABA-B受体的激活。最后,外周GABA受体似乎未显著参与胃酸分泌的直接调控。