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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-L-745870
L-745870

Chemical Structure : L-745870

CAS No.: 158985-00-3

L-745870 (L-745,870)

货号: PC-21106Not For Human Use, Lab Use Only.

L-745870 (L-745,870) is is a potent, selective, brain-penetrant and orally active dopamine D4 receptor (D4R) antagonist with Ki of 0.43 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

L-745870 (L-745,870) is is a potent, selective, brain-penetrant and orally active dopamine D4 receptor (D4R) antagonist with Ki of 0.43 nM.
L-745870 is >100-fold selective for D4R over other dopamine receptors (D1R, D2R, D3R, and D5R) with subnanomolar affinity.
L-745870 blocks the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells.
L-745870 blocks dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells.
L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia.

物理化学性质&存储条件

分子量 326.83
分子式 C18H19ClN4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[[4-(4-Chlorophenyl)-1-piperazinyl]methyl]-1H-pyrrolo[2,3-b]pyridine

参考文献

1. Patel S, et al. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47.

2. Bristow LJ, et al. Trends Pharmacol Sci. 1997 Jun;18(6):186-8.

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