Description
An antagonist of the D2 receptor (Kis = 2.4, 100, and 220 nM for D2, D3, and D4 receptors, respectively); selective for human 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); inhibits quinpirole-stimulated mitogenesis (EC50s = 4.46 and 90.4 nM, respectively, for human D2 and D3 receptors in CHO cells); reversibly blocks D2-mediated currents in Xenopus oocytes via GIRK channels when used at a concentration of 3 μM; inhibits apomorphine-induced climbing behavior in mice (ID50 = 0.3 mg/kg, s.c.); inhibits the conditioned avoidance response in rats (ID50 = 6.1 mg/kg, s.c.); evokes a catalepsy response (AD50 = 7.0 mg/kg, s.c.) and blocks methylphenidate-induced gnawing (ID50 = 2.4 mg/kg, s.c.) in rats
Formal name: 4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)-4-piperidinol
Synonyms:
Molecular weight: 340.9
CAS: 81226-60-0
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis