Formulation: A crystalline solid
Formal Name: 4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)-4-piperidinol
Purity: ≥98%
Formula Markup: C20H21ClN2O
Formula Weight: 340,9
Shelf life (days): 730
CAS Number: 81226-60-0
Notes: L-741,626 is an antagonist of the dopamine D2 receptor (Kis = 2.4, 100, and 220 nM for human D2, D3, and D4, respectively, in a radioligand displacement assay).{38393} L-741,626 is selective for D2 receptors (Ki = 3.98 nM) over serotonin receptors (Kis ≤ 316.2 nM for human 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT3).{38397} In a functional assay, L-741,626 inhibits quinpirole-stimulated mitogenesis with EC50 values of 4.46 and 90.4 nM in CHO cells transfected with human D2long and D3 receptors, respectively.{38395} L-741,626 (3 μM) reversibly blocks D2-mediated currents in Xenopus oocytes via G protein-gated inwardly rectifying K+ (GIRK) channels.{38396} In models of potential antipsychotic activity, L-741,626 inhibits apomorphine-induced climbing behavior in mice (ID50 = 0.3 mg/kg, s.c.) and the conditioned avoidance response (CAR) in rats (ID50 = 6.1 mg/kg, s.c.).{38398} L-741,626 evokes a catalepsy response (AD50 = 7.0 mg/kg, s.c.) and blocks gnawing induced by methylphenidate (Item No. 11639; ID50 = 2.4 mg/kg, s.c.) in rat models of potential extrapyramidal activity.
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