L-745,870 (hydrochloride)

L-745,870 is a dopamine D₄ receptor antagonist (K_i = 0.43 nM).¹ It is selective for dopamine D₄ receptors over dopamine D₂ and D₃ receptors (K_is = 960 and 2,300 nM, respectively). It is also selective for dopamine D₄ receptors over α_2A-, α_2B-, and α_2C-adrenergic receptors (IC₅₀s = 0.00043, 0.16, 0.17, and 0.23 µM, respectively) and the serotonin (5-HT) receptor subtypes 5-HT_2C and 5-HT_1A (IC₅₀s = 0.2 and 2.9 µM, respectively). L-745,870 (100 nM) inhibits dopamine-induced inhibition of forskolin-induced cAMP production in HEK293 cells expressing human dopamine D₄ receptors. In vivo, L-745,870 (3, 10, and 30 mg/kg) inhibits mescaline-induced head twitches in mice. L-745,870 (1 mg/kg) reduces L-DOPA-induced dyskinesia in a macaque model of MPTP-induced Parkinson’s disease.²

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1. Patel, S., Freedman, S., Chapman, K.L., et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D₄ receptor. J. Pharmacol. Exp. Ther. 283(2), 636-647 (1997).

2. Huot, P., Johnston, T.H., Koprich, J.B., et al. L-745,870 reduces L-DOPA-induced dyskinesia in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned macaque model of Parkinson’s disease. J. Pharm. Exp. Ther. 342(2), 576-585 (2012).