L-741626

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L-741626 是 D2 多巴胺受体的选择性拮抗剂。

L-741626 is a selective antagonist of D2 dopamine receptor (Ki: 2.4, 100, and 220 nM for human D2, D3 and D4 receptors respectively).

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).

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.

3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole

GPCR/G Protein

Dopamine Receptor

human D2 receptor|human D3 receptor|human D4 receptor

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81226-60-0

340.85

C20H21ClN2O

>98% (HPLC)

DMSO : 40 mg/mL?(117.35 mM;?Need ultrasonic)

OC1(CCN(Cc2c[nH]c3c2cccc3)CC1)c(cc1)ccc1Cl

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(-20℃)

With Ice Pack

≥ 2 years