title: Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.
abstract: 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.
authors.affiliation: Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co Ltd, 21 Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. kubota.hideki @yamanouchi.co.jp
authors.forename: Hideki
authors.initials: H
authors.lastname: Kubota
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Watanabe
authors.forename: Akio
authors.initials: A
authors.lastname: Kakefuda
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Masuda
authors.forename: Kouichi
authors.initials: K
authors.lastname: Wada
authors.forename: Noe
authors.initials: N
authors.lastname: Ishii
authors.forename: Shuichi
authors.initials: S
authors.lastname: Sakamoto
authors.forename: Shin-ichi
authors.initials: S
authors.lastname: Tsukamoto
mesh_terms: D000818:Animals; D001919:Bradycardia / Q000188:drug therapy*; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D010881:Piperidones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002316:Cardiotonic Agents; D010881:Piperidones; D044005:Tetrahydroisoquinolines