[New intracellular calcium antagonists. I. Synthesis and pharmacological evaluation of 2,3,4,5-tetrahydro-1,5-benzothiazepine analogs].
A series of 2,3,4,5-tetrahydro-1,5-benzothiazepine and related compounds were prepared, and the intracellular Ca2+ inhibitory effects were examined using methoxamine- or caffeine-induced contraction of isolated rabbit arteries. Structure-activity relationship studies of these compounds are discussed and the results suggest that novel 5-[3-[2-(3,4-dimethoxyphenyl)ethyl]aminopropionyl]-2,3,4,5- tetrahydro-1,5-benzothiazepine fumarate (20d) showed the most potent inhibitory action on the intracellular Ca2+ release.
Ueyama
N
N
Kotobuki Research Laboratories, Kotobuki Pharmaceutical Company Ltd., Nagano, Japan.
Wakabayashi
S
S
Tomiyama
T
T
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013841:Thiazepines / Q000138:chemical synthesis* / Q000494:pharmacology
D002121:Calcium Channel Blockers; D013841:Thiazepines; C051271:KT 362; D002118:Calcium