产品
编 号:F467409
分子式:C20H21ClN2O
分子量:340.85
产品类型
结构图
CAS No: 81226-60-0
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产品详情
生物活性:
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively.
体内研究:
L-741626 (1.0 mg/kg; i.h.) is effective at shifting to the right the pramipexole dose-response curve in pramipexole-trained male Sprague Dawley rats.Coadministrating Cocaine with the D2 antagonist L-741626 (3 mg/kg; i.p.; 15 min before Cocaine)for 5 days reduces the Cocaine-induced increase in microglial TNF-α production in adult mice.
体外研究:
Intrinsic activities in a functional assay using inhibition of quinpirole stimulation of mitogenesis in human dopamine D2 or D3 receptors transfected into Chinese hamster ovary (CHO) cells, L-741626 is prepared by literature methods (Ki (D2)=11.2 nM) and displays a D3/D2 and D4/D2 selectivity ratio of 15-fold and 136-fold, respectively.In the functional assay L-741626 is a potent antagonist (EC50 (D2)=4.46 nM) with some D2 selectivity (EC50 (D3)=90.4 nM).