1,4-Dihydropyridine activators in the tiamdipine series.
The pharmacologic and radioligand binding properties of 5-nitro analogs of the 1,4-dihydropyridine Ca2+ channel antagonist, tiamdipine (2-(2-aminoethylthio)methyl-3-carbomethoxy-5-carbomethoxy-6-m ethyl-4-(3-nitrophenyl)-1,4-dihydropyridine) and its N-formyl derivative have been measured in rat tail artery, guinea pig ileum and rat heart. The enantiomers of both analogs showed activator and antagonist properties, the latter being exhibited at lower concentrations.
Galletti
F
F
Department of Biochemical Pharmacology, School of Pharmacy, State University of New York, Buffalo 14260.
Luchowski
E
E
Triggle
D J
DJ
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D004095:Dihydropyridines / Q000378:metabolism / Q000494:pharmacology*; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D017275:Isradipine; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000378:metabolism; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism; D010069:Oxadiazoles / Q000378:metabolism; D011189:Potassium Chloride / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011921:Rats, Inbred WKY; D013237:Stereoisomerism
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D010069:Oxadiazoles; C066605:tiamdipine; D011189:Potassium Chloride; D017275:Isradipine