Formulation: A solid
Formal Name: 3-[[4-(4-chlorophenyl)-1-piperazinyl]methyl]-1H-pyrrolo[2,3-b]pyridine, trihydrochloride
Purity: ≥98%
Formula Markup: C18H19ClN4 • 3HCl
Formula Weight: 472,7
Shelf life (days): 1460
CAS Number: 866021-03-6
Notes: L-745,870 is a dopamine D4 receptor antagonist (Ki = 0.43 nM).{68572} 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 α2A-, α2B-, and α2C-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.{68573}