Title of article :
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: A unique structural class of dopamine D4 selective ligands
Author/Authors :
Andrew Thurkauf، نويسنده , , Xi Chen، نويسنده , , Suoming Zhang، نويسنده , , Yang Gao، نويسنده , , Andrzej Kieltyka، نويسنده , , Jan W. F. Wasley، نويسنده , , Robbin Brodbeck، نويسنده , , William Greenlee، نويسنده , , Ashit Ganguly، نويسنده , , He Zhao، نويسنده ,
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 D4 over D2 and other CNS receptors. This compound was identified as a D4 antagonist via its attenuation of dopamine agonist-induced GTPγ35S binding at D4 receptor.
