effects of 4-(2-alkylthio-1-benzyl-5-imidazolyl)-dihydropyridines on the isolated rat colon and right atrium contractility
نویسندگان
چکیده
objectives in order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. the tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nifedipine as a positive control substance. materials and methods isolated rat colon and atrial tissues were prepared. rat colon was contracted with 80 mm kcl, and maximum response was recorded (100%). after washing tissue with krebs solution it was preincubated with different concentrations of test compounds and again kcl was added and percent change in contraction was calculated. spontaneous contractions and its frequency for colon and atrium before and after addition of test compounds were also recorded and percent change was calculated. nifedipine (10-8 -10-5 m) was used as positive control at all experiments. results the compounds showed similar effects to that of nifedipine on the isolated rat colon. the potency of these analogues with concentration range 10-5 to 10-4 m was compared to potency of nifedipine which was effective at 10-8 to 10-5 m (p<0.01). however, unlike nifedipine, the test compounds exerted significant positive inotropic effect on the isolated rat atrium (p < 0.01). our observations suggest that these analogues of nifedipine selectively enhance contractility of heart muscle while causing relaxation of intestinal smooth muscle. conclusion these compounds may serve as valuable probes to develop novel dihydropyridines with dual smooth muscle relaxant effect and positive inotropic action.
منابع مشابه
Effects of 4-(2-Alkylthio-1-benzyl-5-imidazolyl)-Dihydropyridines on the Isolated Rat Colon and Right Atrium Contractility
Objectives In order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. The tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nif...
متن کاملEffects of 4-(2-Alkylthio-1-benzyl-5-imidazolyl)-Dihydropyridines on the Isolated Rat Colon and Right Atrium Contractility
Objectives In order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. The tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nife...
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The o-nitrophenyl group at position 4 of dihydropyridine of nifedipine analogues was replaced with 2-alkylthio-1-benzyl-5-imidazolyl substituent. Starting from dihydroxyacetone 2-alkythio-1-benzyl- 5-formyl imidazole (3) was first synthesized which was subsequently used in synthesizing symmetrical (5a-f) and asymmetrical (6a,b) dihydropyridines. Primarily pharmacological studies of the title co...
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a series of 1,4-dihydropyridine calcium channel blockers bearing 1-(4-x -benzyl)-5-imidazolyl substituent at 4 position (5a-e) (x=h, f) were synthesized and tested for antihypertensive activity in desoxycorticosterone acetate (doca)-induced hypertension in rats. amlodipine was used as the standard dihydropyridine. all compounds tested showed lower antihypertensive activity than that of amlodipi...
متن کاملsynthesis of 4-(1-benzyl-5-imidazolyl)-1,4-dihydropyridines
the o-nitrophenyl group at position 4 of dihydropyridine of nifedipine analogues was replaced with 2-alkylthio-1-benzyl-5-imidazolyl substituent. starting from dihydroxyacetone 2-alkythio-1-benzyl- 5-formyl imidazole (3) was first synthesized which was subsequently used in synthesizing symmetrical (5a-f) and asymmetrical (6a,b) dihydropyridines. primarily pharmacological studies of the title co...
متن کاملSynthesis of Novel 4-[1-(4-fluorobenzyl)-5-imidazolyl] Dihydropyridines and Studying their Effects on Rat Blood Pressure
Objective(s) Calcium-channel blockers have an important role in the treatment of several cardiovascular disorders. Derivatives of 1, 4-dihydropyridine are one of the most potent calcium antagonists. In this study four novel ', 4-dihydropyridine calcium channel blockers were synthesized and their hypotensive properties were investigated in male rats. Materials and Methods Four 1, 4-dihydropyr...
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عنوان ژورنال:
iranian journal of basic medical sciencesجلد ۱۱، شماره ۳، صفحات ۱۵۹-۱۶۵
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