6-(4-Benzylpiperazin-1-yl)benzodioxanes as selective ligands at cloned primate dopamine D(4) receptors.
A series of novel 6-(4-benzylpiperazin-1-yl)benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl]piperazin-1-yl)benzodioxane (2d) had high affinity and selectivity for the D(4) dopamine receptor subtype and was identified as a D(4) antagonist via its attenuation of dopamine-induced GTPgamma(35)S binding at the D(4) receptor.
Hodgetts
K J
KJ
Neurogen Corporation, 35 Northeast Industrial Road, Branford, CT 06405, USA. khodgetts@nrgn.com
Kieltyka
A
A
Brodbeck
R
R
Tran
J N
JN
Wasley
J W
JW
Thurkauf
A
A
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D004146:Dioxanes / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D004353:Drug Evaluation, Preclinical; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D008024:Ligands; D010879:Piperazines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011323:Primates; D017448:Receptors, Dopamine D2 / Q000235:genetics / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship
C449100:6-(4-benzylpiperazin-1-yl)benzodioxane; D004146:Dioxanes; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D008024:Ligands; D010879:Piperazines; D017448:Receptors, Dopamine D2; D011994:Recombinant Proteins; D050638:Receptors, Dopamine D4; D016244:Guanosine 5'-O-(3-Thiotriphosphate)