Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers.
Voltage Activated Calcium Channel (VACC) blockers have been demonstrated to have utility in the treatment of pain and stroke. A series of aminomethyl substituted isoquinolinol derivatives with potent functional activity for N-type VACC's have been identified. Their synthesis and preliminary pharmacology are discussed herein.
Yuen
P
P
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Schelkun
R M
RM
Szoke
B
B
Tarczy-Hornoch
K
K
D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D002121:Calcium Channel Blockers; D007546:Isoquinolines