L-745,870 (hydrochloride)

L-745,870 is a dopamine D4 receptor antagonist (Ki = 0.43 nM). It is selective for dopamine D4 receptors over dopamine D2 and D3 receptors (Kis = 960 and 2,300 nM, respectively). It is also selective for dopamine D4 receptors over alpha2A-, alpha2B-, and alpha2C-adrenergic receptors (IC50s = 0.00043, 0.16, 0.17, and 0.23 µM, respectively) and the serotonin (5-HT) receptor subtypes 5-HT2C and 5-HT1A (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.Formal Name: 3-[[4-(4-chlorophenyl)-1-piperazinyl]methyl]-1H-pyrrolo[2,3-b]pyridine, trihydrochloride. CAS Number: 866021-03-6. Molecular Formula: C18H19ClN4 . 3HCl. Formula Weight: 472.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: ClC1=CC=C(N2CCN(CC2)CC3=CNC4=NC=CC=C43)C=C1.Cl.Cl.Cl. InChi Code: InChI=1S/C18H19ClN4.3ClH/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18,,,/h1-7,12H,8-11,13H2,(H,20,21),3*1H. InChi Key: KJSOYZLYCFYXFC-UHFFFAOYSA-N.