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

H Kubota, T Watanabe, A Kakefuda, N Masuda…

Index: Kubota, Hideki; Watanabe, Toshihiro; Kakefuda, Akio; Masuda, Noriyuki; Wada, Kouichi; Ishii, Noe; Sakamoto, Shuichi; Tsukamoto, Shinichi Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 5 p. 871 - 882

Full Text: HTML

Citation Number: 7

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 ...