EFFECT OF CHOLECYSTOKININ AND ITS ANTAGONISTS LORGLUMIDE, DEVAZEPIDE, AND L-365 260 ON GASTROINTESTINAL MOTILITY IN RATS

被引：0

作者：

WANG, SX

机构：

来源：

ACTA PHARMACOLOGICA SINICA | 1993年 / 14卷 / 05期

关键词：

CHOLECYSTOKININ; SINCALIDE; ILEUM; GASTROINTESTINAL MOTILITY; GASTRIC EMPTYING;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Cholecystokinin (CCK) plays an important role in gallbladder contraction and gut motility. Sincalide (CCK-8) evoked guinea pig isolated ileum contraction at 10(-5)-10(-1) mumol.L-1 in a concentration-dependent manner, EC50 being 207 pmol.L-1. It delayed the gastric emptying as well. The rate of inhibition of gastric emptying was 71+/-12% at 100 mug.kg-1 by ip. Sincalide antagonists. lorglumide, devazepide, and L-365 260 antagonized the ileal smooth muscle response to sincalide in a concentration-dependent manner. Their pA2 were 7. 30, 10.02, and 7.77, respectively. Lorglumide, devazepide, and L-365 260 inhibited the delaying of gastric emptying evoked by sincalide. The IC50 were 0.11, 0.0064, and 0.66 mg-kg-1, respectively.

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页码：443 / 446

页数：4

相关论文

共 14 条

[1] CHOLECYSTOKININ [J].

ALBUS, M .

PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY, 1988, 12 :S5-S21

[2] EVALUATION OF A NEW AND POTENT CHOLECYSTOKININ ANTAGONIST ON MOTOR-RESPONSES OF THE GUINEA-PIG INTESTINE [J].

BARTHO, L ;

HOLZER, P ;

LEMBECK, F ;

LIPPE, IT ;

SETNIKAR, I .

BRITISH JOURNAL OF PHARMACOLOGY, 1987, 90 (04) :753-761

[3] BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF AN EXTREMELY POTENT AND SELECTIVE NONPEPTIDE CHOLECYSTOKININ ANTAGONIST [J].

CHANG, RSL ;

LOTTI, VJ .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (13) :4923-4926

[4] A SIMPLIFIED METHOD FOR ASSESSING DRUG EFFECTS ON GASTRIC-EMPTYING IN RATS [J].

DROPPLEMAN, DA ;

GREGORY, RL ;

ALPHIN, RS .

JOURNAL OF PHARMACOLOGICAL METHODS, 1980, 4 (03) :227-230

[5] CHOLECYSTOKININ AND GASTRIN ANTAGONISTS [J].

FREIDINGER, RM .

MEDICINAL RESEARCH REVIEWS, 1989, 9 (03) :271-290

[6] BENZODIAZEPINE ANALOGS L365,260 AND L364,718 AS GASTRIN AND PANCREATIC CCK RECEPTOR ANTAGONISTS [J].

HUANG, SC ;

ZHANG, L ;

CHIANG, HCV ;

WANK, SA ;

MATON, PN ;

GARDNER, JD ;

JENSEN, RT .

AMERICAN JOURNAL OF PHYSIOLOGY, 1989, 257 (01) :G169-G174

[7] EVIDENCE THAT THE ACTION OF CHOLECYSTOKININ OCTAPEPTIDE ON THE GUINEA-PIG ILEUM LONGITUDINAL MUSCLE IS MEDIATED IN PART BY SUBSTANCE-P RELEASE FROM THE MYENTERIC PLEXUS [J].

HUTCHISON, JB ;

DOCKRAY, GJ .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1981, 69 (01) :87-93

[8] DISTINCT CHOLECYSTOKININ RECEPTORS IN BRAIN AND PANCREAS [J].

INNIS, RB ;

SNYDER, SH .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1980, 77 (11) :6917-6921

[9]

LOTTI VJ, 1987, J PHARMACOL EXP THER, V241, P103

[10] A NEW POTENT AND SELECTIVE NON-PEPTIDE GASTRIN ANTAGONIST AND BRAIN CHOLECYSTOKININ RECEPTOR (CCK-B) LIGAND - L-365,260 [J].

LOTTI, VJ ;

CHANG, RSL .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1989, 162 (02) :273-280