New Intracellular Calcium Antagonists. I. Synthesis and Pharmacological Evaluation of 2, 3, 4, 5-Tetrahydro-1, 5-benzothiazepine Analogs
| Autor: | Tsuyoshi Tomiyama, Shuichi Wakabayashi, Naoto Ueyama |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Male
Pharmacology Contraction (grammar) Thiazepines Chemistry Pharmaceutical Science Blood Pressure In Vitro Techniques Calcium Channel Blockers Inhibitory postsynaptic potential Muscle Smooth Vascular Calcium in biology Methoxamine Rats Structure-Activity Relationship medicine Animals Calcium Rabbits Rats Wistar Intracellular Muscle Contraction medicine.drug |
| Zdroj: | YAKUGAKU ZASSHI. 116:106-124 |
| ISSN: | 1347-5231 0031-6903 |
| DOI: | 10.1248/yakushi1947.116.2_106 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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