5-HT1A and D-2 receptor affinity of o-methoxyphenylpiperazine derivatives with terminal benzamide fragment on N-4 alkyl chain. 2.
The synthesis of some o-methoxyphenylpiperazines with a benzamide moiety on N-4 alkyl chain was accomplished and their affinity for dopamine and serotonin receptor subtypes was assayed by in vitro receptor binding. The results show that several derivatives had a good affinity both on D-2 and 5-HT1A receptors, the IC50s ranging from 10(-7) to 10(-8) M.
Perrone
R
R
Dipartimento Farmaco-Chimico, Bari, Italy. off
Berardi
F
F
Leopoldo
M
M
Tortorella
V
V
Lograno
M D
MD
Daniele
E
E
Govoni
S
S
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000493:pharmacokinetics; D000818:Animals; D001549:Benzamides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D017829:Granisetron / Q000494:pharmacology; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D017294:Ondansetron / Q000494:pharmacology; D010879:Piperazines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017448:Receptors, Dopamine D2 / Q000187:drug effects / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D013134:Spiperone / Q000494:pharmacology; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D001549:Benzamides; D017829:Granisetron; D017294:Ondansetron; D010879:Piperazines; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D013134:Spiperone; C040083:1-(2-methoxyphenyl)piperazine