title: 1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
abstract: A series of novel 1H-pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes was prepared and screened at selected dopamine receptor subtypes. Compound 4 (NGB 4420) displayed high affinity and selectivity (>100-fold) for the D(4) over D(2) and other CNS receptors. This compound was identified as a D(4) antagonist via its attenuation of dopamine agonist-induced GTPgamma(35)S binding at D(4) receptor.
authors: Neurogen Corporation, Branford, CT 06405, USA.
authors: Andrew
authors: A
authors: Thurkauf
authors: Xi
authors: X
authors: Chen
authors: Suoming
authors: S
authors: Zhang
authors: Yang
authors: Y
authors: Gao
authors: Andrzej
authors: A
authors: Kieltyka
authors: Jan W F
authors: JW
authors: Wasley
authors: Robbin
authors: R
authors: Brodbeck
authors: William
authors: W
authors: Greenlee
authors: Ashit
authors: A
authors: Ganguly
authors: He
authors: H
authors: Zhao
mesh_terms: D018492:Dopamine Antagonists / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: C493599:DRD4 protein, human; D018492:Dopamine Antagonists; D008024:Ligands; D017448:Receptors, Dopamine D2; D013876:Thiophenes; D050638:Receptors, Dopamine D4