ArticleNaunyn-Schmiedeberg's archives of pharmacology
The interactions of 1,4-dihydropyridines bearing a 2-(2-aminoethylthio)methyl substituent at voltage-dependent Ca2+ channels of smooth muscle, cardiac muscle and neuronal tissues.
Article in Naunyn-Schmiedeberg's archives of pharmacology. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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1 citing paper in PubMed, 14 citations in OpenAlex.
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5 authors at 1 institution in 1 country.
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Abstract
The Ca2+ channel antagonistic potencies of tiamdipine [2-(2-aminoethylthio)methyl-3-carboethoxy-5-carbomethoxy-6-m ethyl-4-(3- nitrophenyl)-1,4-dihydropyridine] and nifedipine [2,6-dimethyl-3,5-dicarbomethoxy-4-(2-nitrophenyl)-1,4-dihydrop yri dine] analogs bearing phenyl ring substituents were studied using pharmacologic and radioligand binding techniques. Additionally, analogs of tiamdipine possessing (2-aminoethylthio)methyl-, (2-acetamidoethylthio)methyl- and (2-pyrrolidinylmethylthio)methyl- groups at the C2 position of the 1,4-dihydropyridine ring have been studied. Tiamdipine and nifedipine analogs inhibited K(+)-induced contractile responses in rat tail artery. IC50 values of 4-phenyl ring substituted 2-(2-aminoethylthio)methyl tiamdipine analogs ranged from 10(-7) mol/l to 10(-8) mol/l. However, the corresponding 4-phenyl ring substituted nifedipine analogs covered a wider range of potency from 10(-6) mol/l to 10(-9) mol/l. KI values of the corresponding tiamdipine analogs for the inhibition of specific [3H]PN 200-110 [(+)-[3H]isopropyl-4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-5- methoxycarbonyl-2,6-dimethyl-3-pyridinecarboxylate] binding ranged from 10(-7) mol/l to 10(-9) mol/l in guinea pig ileal and rat heart membranes and rat brain synaptosomes. The two stereoisomers of tiamdipine and its analog 2-(2-acetamidoethylthio)methyl-3-carboethoxy-5-carbomethoxy- 6-methyl-4-(3- nitrophenyl)-1,4-dihydropyridine, and the four stereoisomers of 2-(2-pyrrolidinylmethylthio)methyl-3-carboethoxy-5-carbom eth oxy-6-methyl-4-(3- nitrophenyl)-1,4-dihydropyridine showed high stereoselectivity ratios of approximately (-)/(+) = 100 and 1000 in pharmacologic and binding experiments, respectively. The inhibitory actions of 2-(2-aminoethylthio)methyltiamdipine analogs against K(+)-induced contractile responses in rat tail artery developed very slowly requiring at least 2 h for maximum effect.(ABSTRACT TRUNCATED AT 250 WORDS)
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