PD-135158, A CCK(B) GASTRIN RECEPTOR ANTAGONIST, STIMULATES RAT PANCREATIC-ENZYME SECRETION AS A CCK(A) RECEPTOR AGONIST

被引：20

作者：

HOCKER, M

HUGHES, J

FOLSCH, UR

SCHMIDT, WE

机构：

[1] CHRISTIAN ALBRECHTS UNIV KIEL,DEPT MED 1,GASTROINTESTINAL UNIT,MOLEC GASTROENTEROL LAB,D-24105 KIEL,GERMANY

[2] PARKE DAVIS NEUROSCI RES CTR,CAMBRIDGE CB2 2QB,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 242卷 / 01期

关键词：

CCK(B) GASTRIN RECEPTOR ANTAGONISTS; CCK(A) RECEPTOR ANTAGONISTS; LOXIGLUMIDE; PANCREATIC ACINI (ISOLATED; RAT);

D O I：

10.1016/0014-2999(93)90016-B

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The CCK(B)/gastrin receptor antagonist, PD 135158 (CAM 1208), surprisingly stimulates lipase release from isolated rat pancreatic acini dose dependently in a biphasic manner, with identical efficacy but lower potency compared to cholecystokinin octapeptide (CCK-8). Half-maximal stimulation occurred at 0.6 muM and maximal secretion was induced at 50 muM. Supramaximal concentrations decreased lipase release. Acinar lipase secretion in response to 25 pM CCK-8 or 1 muM CAM-1028 was abolished by 5 muM of the specific CCK, receptor antagonist loxiglumide (CR 1505), half-maximal inhibition was observed at 0.6 muM for CCK-8 and 0.4 muM for PD 135158. These data demonstrate that the CCK(B)/gastrin receptor antagonist, PD 135158, acts as a full agonist at the rat pancreatic CCK(A) receptor.

引用

页码：105 / 108

页数：4

共 15 条

[1] A SINGLE AMINO-ACID OF THE CHOLECYSTOKININ-B GASTRIN RECEPTOR DETERMINES SPECIFICITY FOR NONPEPTIDE ANTAGONISTS [J].