PMID- 2575063 OWN - NLM STAT- MEDLINE DCOM- 19900214 LR - 20190912 IS - 0435-1339 (Print) IS - 0435-1339 (Linking) VI - 24 IP - 6 DP - 1989 Dec TI - Somatostatin receptors and the effect of somatostatin on histamine-stimulated adenylate cyclase activity in isolated gastric glands of guinea pigs. PG - 611-8 AB - To investigate the mechanism of the suppressive action of somatostatin on gastric acid secretion, we determined the somatostatin binding and adenylate cyclase activity on crude membrane fractions of isolated gastric glands of guinea pigs. The binding studies using 125I-Tyr11 somatostatin showed the presence of somatostatin receptors with a single high affinity on crude membrane fractions. The dissociation constant (KD) for somatostatin was 1.05 +/- 0.13 nM, and the number of binding sites (Bmax) was 6.98 +/- 1.27 fmol/mg protein (mean +/- SE, n = 6). The adenylate cyclase activity was increased by histamine, which was completely inhibited by 10(-3) M cimetidine. Somatostatin non-competitively suppressed the histamine-stimulated adenylate cyclase activity in the presence of guanosine 5'-triphosphate (GTP). These results suggest that somatostatin inhibits histamine-stimulated acid secretion through the inhibition of the adenylate cyclase system, via somatostatin receptor and guanine nucleotide binding protein, which is activated by GTP binding. FAU - Yoshida, K AU - Yoshida K AD - Third Department of Internal Medicine, Kyushu University Faculty of Medicine, Fukuoka, Japan. FAU - Nishihara, S AU - Nishihara S FAU - Misawa, T AU - Misawa T FAU - Nawata, H AU - Nawata H LA - eng PT - Journal Article PL - Japan TA - Gastroenterol Jpn JT - Gastroenterologia Japonica JID - 0152744 RN - 0 (Receptors, Neurotransmitter) RN - 0 (Receptors, Somatostatin) RN - 51110-01-1 (Somatostatin) RN - 59481-27-5 (somatostatin, Tyr(11)-) RN - 820484N8I3 (Histamine) RN - EC 4.6.1.1 (Adenylyl Cyclases) SB - IM MH - Adenylyl Cyclases/*metabolism MH - Animals MH - Gastric Acid/*metabolism MH - Gastric Mucosa/*drug effects/enzymology/metabolism MH - Guinea Pigs MH - Histamine/*pharmacology MH - In Vitro Techniques MH - Male MH - Receptors, Neurotransmitter/*drug effects/metabolism MH - Receptors, Somatostatin MH - Somatostatin/*analogs & derivatives/metabolism/pharmacology EDAT- 1989/12/01 00:00 MHDA- 1989/12/01 00:01 CRDT- 1989/12/01 00:00 PHST- 1989/12/01 00:00 [pubmed] PHST- 1989/12/01 00:01 [medline] PHST- 1989/12/01 00:00 [entrez] AID - 10.1007/BF02774158 [doi] PST - ppublish SO - Gastroenterol Jpn. 1989 Dec;24(6):611-8. doi: 10.1007/BF02774158.