An antagonist of the D2 receptor (Kis = 2.4

L-741,626 – 10 mg

Brand:
Cayman
CAS:
81226-60-0
Storage:
-20
UN-No:
Non-Hazardous - /

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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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

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