Document Report Card
Basic Information
ID: ALA1136188
Journal: Bioorg Med Chem Lett
Title: 1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
Authors: Thurkauf A, Chen X, Zhang S, Gao Y, Kieltyka A, Wasley JW, Brodbeck R, Greenlee W, Ganguly A, Zhao H.
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.
CiteXplore: 14611858