Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.

Hideki Kubota, Toshihiro Watanabe, Akio Kakefuda, Noriyuki Masuda, Kouichi Wada, Noe Ishii, Shuichi Sakamoto, Shin-ichi Tsukamoto

文献索引：Bioorg. Med. Chem. Lett. 14 , 3049-3052, (2004)

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摘要

A series of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized, and their bradycardic activities were investigated in the isolated right atria of guinea pigs and in conscious rats. These efforts identified the achiral compound 2f, which exhibited potent and long-lasting bradycardic activity with minimal effects on mean blood pressure in conscious rats.