Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.
A series of 1,2,3,4-tetrahydroisoquinolines, tetrahydrothieno[2,3-c]pyridines, and related compounds were evaluated for their ability to inhibit binding of [3H]-1-[1-(2-thienyl)piperidine and [3H]-N-allylnormetazocine to phencyclidine (PCP) and sigma receptors, respectively. A representative series of compounds was evaluated in behavioral assays to determine the ability of the compounds to induce PCP-like stereotyped behavior and ataxia. All of the compounds caused stereotyped behavior and ataxia, indicating their agonist actions at the PCP site.
Gray
N M
NM
Central Nervous System Disease Research, G. D. Searle & Co., St. Louis, Missouri 63198.
Cheng
B K
BK
Mick
S J
SJ
Lair
C M
CM
Contreras
P C
PC
D000818:Animals; D001259:Ataxia / Q000139:chemically induced; D001522:Behavior, Animal / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D007546:Isoquinolines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D010620:Phenazocine / Q000031:analogs & derivatives / Q000378:metabolism; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D017981:Receptors, Neurotransmitter / Q000378:metabolism; D017478:Receptors, Phencyclidine; D013239:Stereotyped Behavior / Q000187:drug effects; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines
D007546:Isoquinolines; D017981:Receptors, Neurotransmitter; D017478:Receptors, Phencyclidine; D044005:Tetrahydroisoquinolines; C014843:1,2,3,4-tetrahydroisoquinoline; C012134:SK&F 10047; C012058:tenocyclidine; D010620:Phenazocine; D010622:Phencyclidine