NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-3-fluorenylcarboxamide and N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-2-biphenylenylcarboxamide were prepared in several steps from 2,3-dichloroaniline. These compounds were identified as highly selective dopamine D3 receptor antagonists.
Yuan
J
J
Department of Medicinal Chemistry, Neurogen Corporation, Branford, CT 06405, USA.
Chen
X
X
Brodbeck
R
R
Primus
R
R
Braun
J
J
Wasley
J W
JW
Thurkauf
A
A
D000818:Animals; D016466:CHO Cells / Q000187:drug effects / Q000378:metabolism; D006224:Cricetinae; D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D065127:Dopamine D2 Receptor Antagonists; D005449:Fluorenes / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D010879:Piperazines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D050637:Receptors, Dopamine D3; D014162:Transfection
C493593:DRD3 protein, human; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; C493595:Drd3 protein, rat; D005449:Fluorenes; C116819:NGB 2849; C116818:NGB 2904; D010879:Piperazines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3