Synthesis and pharmacological evaluation of N-acyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents |
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Authors: | Kubota Hideki Watanabe Toshihiro Kakefuda Akio Masuda Noriyuki Wada Kouichi Ishii Noe Sakamoto Shuichi Tsukamoto Shinichi |
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Affiliation: | Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co. Ltd., 21Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. kubota.hideki@yamanouchi.co.jp |
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Abstract: | A series of N-acyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized and evaluated for their bradycardic activities in isolated guinea pig right atria and in urethane-anesthetized rats. These efforts resulted in identification of the compound 8a, which exhibits potent bradycardic activity with minimal influence on mean blood pressure in urethane-anesthetized rats. Oral administration of compound 8a to conscious rats revealed increased potency and prolonged duration of action when compared to Zatebradine. |
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