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脑室内注射生长抑素sst5受体激动剂可抑制大鼠胃酸分泌。

Intracerebroventricular injection of somatostatin sst5 receptor agonist inhibits gastric acid secretion in rats.

作者信息

Martínez V, Coy D H, Lloyd K C, Taché Y

机构信息

Department of Medicine and Brain Research Institute, UCLA 90073, USA.

出版信息

Eur J Pharmacol. 1996 Jan 25;296(2):153-60. doi: 10.1016/0014-2999(95)00690-7.

DOI:10.1016/0014-2999(95)00690-7
PMID:8838451
Abstract

Somatostatin and its analogs act in the brain to influence gastric acid secretion. Five different somatostatin receptor subtypes have been characterized (sst1 to sst5). We studied the influence of somatostatin (0.18-0.6 nmol/rat) and selective sst2, sst3 and sst5 receptor ligands on basal gastric acid secretion in conscious rats equipped with chronic gastric and intracerebroventricular (i.c.v.) cannulae. Somatostatin-14 (0.36 nmol/rat), the sst2, sst3 and sst5 receptor agonist, Des-AA1,2,4,5,12,13-[D-Tryp8,D-Cys14]somatostatin (SMS 201-995) (0.18-0.36 nmol/rat) and the sst5 receptor agonist, BIM-23052, (0.8-1.2 nmol/rat) injected i.c.v. inhibited gastric acid secretion. Maximal inhibition reaching 42%, 60% and 42% was induced by somatostatin-14 (0.36 nmol/rat), SMS 201-995 (0.18 nmol/rat) and BIM-23052 (0.8 nmol/rat) respectively. The sst2 receptor agonist, DC 32-87 (0.2-0.8 nmol/rat) and sst3 receptor agonist, BIM-23056 (0.2-1.2 nmol/rat), did not modify gastric acid secretion, except the sst3 receptor agonist at 0.4 nmol/rat which increased acid output at 20 min post-injection. The sst2 receptor agonists (0.4 nmol/rat) co-injected i.c.v. with a subthreshold dose of sst5 (0.4 nmol/rat) inhibited gastric acid secretion. These results show that i.c.v. injection of somatostatin-14 inhibits basal gastric acid secretion in conscious rats through an action on sst5 receptor subtype which can be potentiated by sst2 receptor subtype.

摘要

生长抑素及其类似物在大脑中发挥作用，影响胃酸分泌。已鉴定出五种不同的生长抑素受体亚型（sst1至sst5）。我们研究了生长抑素（0.18 - 0.6纳摩尔/大鼠）以及选择性sst2、sst3和sst5受体配体对配备慢性胃和脑室内（i.c.v.）插管的清醒大鼠基础胃酸分泌的影响。生长抑素-14（0.36纳摩尔/大鼠）、sst2、sst3和sst5受体激动剂、去氨基-AA1,2,4,5,12,13-[D-色氨酸8，D-半胱氨酸14]生长抑素（SMS 201-995）（0.18 - 0.36纳摩尔/大鼠）和sst5受体激动剂BIM-23052（0.8 - 1.2纳摩尔/大鼠）经脑室内注射可抑制胃酸分泌。生长抑素-14（0.36纳摩尔/大鼠）、SMS 201-995（0.18纳摩尔/大鼠）和BIM-23052（0.8纳摩尔/大鼠）分别诱导的最大抑制率达到42%、60%和42%。sst2受体激动剂DC 32-87（0.2 - 0.8纳摩尔/大鼠）和sst3受体激动剂BIM-23056（0.2 - 1.2纳摩尔/大鼠）未改变胃酸分泌，但0.4纳摩尔/大鼠的sst3受体激动剂在注射后20分钟增加了酸分泌量。脑室内共同注射sst2受体激动剂（0.4纳摩尔/大鼠）和阈下剂量的sst5（0.4纳摩尔/大鼠）可抑制胃酸分泌。这些结果表明，脑室内注射生长抑素-14通过作用于sst5受体亚型抑制清醒大鼠的基础胃酸分泌，而sst2受体亚型可增强这种作用。

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