Kubota Hideki, Kakefuda Akio, Watanabe Toshihiro, Taguchi Yasuko, Ishii Noe, Masuda Noriyuki, Sakamoto Shuichi, Tsukamoto Shin ichi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co. Ltd., 21Miyukigaoka, Tsukuba, 305-8585, Ibaraki, Japan.
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2155-8. doi: 10.1016/s0960-894x(03)00349-4.
A series of (+/-)-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines were prepared and their bradycardic activities were examined in isolated guinea-pigs' right atria and in anesthetized rats. Modifications on the benzyl moiety of the parent compound, 1, led to the identification of compound 11e as a potent and specific bradycardic agent.
制备了一系列(±)-2-(3-哌啶基)-1,2,3,4-四氢异喹啉,并在离体豚鼠右心房和麻醉大鼠中检测了它们的心动过缓活性。对母体化合物1的苄基部分进行修饰,确定化合物11e为一种强效且特异性的心动过缓剂。