ANTAGONIST EFFECT OF LOSARTAN ON ANGIOTENSIN-II-INDUCED CONTRACTION IN 5 ISOLATED SMOOTH-MUSCLE ASSAYS

被引:8
作者
LIU, YJ [1 ]
机构
[1] KINGS COLL,SCH MED & DENT,RAYNE INST,DEPT ANALYT PHARMACOL,LONDON SE5 9NU,ENGLAND
关键词
ANGIOTENSIN-II; LOSARTAN; ANGIOTENSIN RECEPTOR (ANTAGONISM); STOMACH; TRACHEA;
D O I
10.1016/0014-2999(93)90892-L
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Antagonist effect of losartan, a nonpeptide antagonist of angiotensin II, on angiotensin II induced contractile response was studied in five isolated smooth muscle assays. In the rabbit aorta and guinea-pig stomach assays, losartan competed with angiotensin II for the angiotensin receptors in an apparently simple manner, that is compliance with the basic criteria of Schild analysis for simple competition. Noncompliance, however, was observed in the guinea-pig ileum, rat ileum and guinea-pig trachea assays where losartan induced nonparallel rightward shifts of angiotensin II E/log[A] curves and the Schild plots were found to have slopes greater than unity. The observed deviations from simple competitive antagonism appeared to be different from those reported earlier, and a possible explanation involving tissue-dependent noncompetitive factor(s) is discussed.
引用
收藏
页码:147 / 154
页数:8
相关论文
共 29 条
[1]   ANGIOTENSIN INCREASES INOSITOL TRISPHOSPHATE AND CALCIUM IN VASCULAR SMOOTH-MUSCLE [J].
ALEXANDER, RW ;
BROCK, TA ;
GIMBRONE, MA ;
RITTENHOUSE, SE .
HYPERTENSION, 1985, 7 (03) :447-451
[2]   SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].
ARUNLAKSHANA, O ;
SCHILD, HO .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01) :48-58
[3]   PHARMACOLOGICAL ANALYSIS OF THE PENTAGASTRIN-TIOTIDINE INTERACTION IN THE MOUSE ISOLATED STOMACH [J].
BLACK, JW ;
LEFF, P ;
SHANKLEY, NP .
BRITISH JOURNAL OF PHARMACOLOGY, 1985, 86 (03) :589-599
[4]   NOMENCLATURE FOR ANGIOTENSIN RECEPTORS - A REPORT OF THE NOMENCLATURE-COMMITTEE OF THE COUNCIL-FOR-HIGH-BLOOD-PRESSURE-RESEARCH [J].
BUMPUS, FM ;
CATT, KJ ;
CHIU, AT ;
DEGASPARO, M ;
GOODFRIEND, T ;
HUSAIN, A ;
PEACH, MJ ;
TAYLOR, DG ;
TIMMERMANS, PBMWM .
HYPERTENSION, 1991, 17 (05) :720-721
[5]  
CHIU AT, 1990, J PHARMACOL EXP THER, V252, P711
[6]   IDENTIFICATION OF ANGIOTENSIN-II RECEPTOR SUBTYPES [J].
CHIU, AT ;
HERBLIN, WF ;
MCCALL, DE ;
ARDECKY, RJ ;
CARINI, DJ ;
DUNCIA, JV ;
PEASE, LJ ;
WONG, PC ;
WEXLER, RR ;
JOHNSON, AL ;
TIMMERMANS, PBMWM .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 165 (01) :196-203
[7]   The antagonism of acetyl choline by atropine. [J].
Clark, AJ .
JOURNAL OF PHYSIOLOGY-LONDON, 1926, 61 (04) :547-556
[8]   ZIG-ZAG TRACHEAL STRIP [J].
EMMERSON, J ;
MACKAY, D .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1979, 31 (11) :798-798
[9]   The action of adrenalin and ergotamine on the uterus of the rabbit. [J].
Gaddum, JH .
JOURNAL OF PHYSIOLOGY-LONDON, 1926, 61 (01) :141-150
[10]  
GADDUM JH, 1937, J PHYSIOL-LONDON, V89, pP7