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L-745870

Chemical Structure : L-745870

CAS No.: 158985-00-3

L-745870 (L-745,870)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 326.83
Formula C18H19ClN4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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