A dopamine receptor antagonist (Kis = 9.8 and 1.5 nM for D1 and D2 receptors

Zuclopenthixol – 500 mg

Brand:
Cayman
CAS:
53772-83-1
Storage:
-20
UN-No:
Non-Hazardous - /

Zuclopenthixol is a dopamine receptor antagonist (Kis = 9.8 and 1.5 nM for D1 and D2 receptors, respectively).{39773} It also binds to serotonin (5-HT) receptor subtypes 5-HT2 and 5-HT6, α1-adrenergic, and histamine receptors (Kis = 7.6, 3, 33, and 169 nM, respectively) but not α2-adrenergic receptors (Ki = >4,300 nM).{39773,39774} Zuclopenthixol inhibits dopamine-induced accumulation of cAMP in rat striatal homogenates (IC50 = 330 nM; Ki = 16 nM).{39774} It decreases stereotypic behavior induced by methylphenidate in mice (ED50 = 0.8 µmol/kg) and by apomorphine in rats and dogs (ED50s = 6.0 and 1.3 µmol/kg, respectively). Zuclopenthixol (0.7 and 1.4 mg/kg, i.p.) administered prior to testing enhances memory retrieval in rats in an inhibitory avoidance task without affecting locomotor activity.{39775}  

 

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Description

A dopamine receptor antagonist (Kis = 9.8 and 1.5 nM for D1 and D2 receptors, respectively); binds to 5-HT2 and 5-HT6, α1-adrenergic, and histamine receptors (Kis = 7.6, 3, 33, and 169 nM, respectively); inhibits dopamine-induced accumulation of cAMP in rat striatal homogenates (IC50 = 330 nM; Ki = 16 nM); decreases stereotypic behavior induced by methylphenidate in mice (ED50 = 0.8 µmol/kg); decreases stereotypic behavior induced by apomorphine in rats and dogs (ED50s = 6.0 and 1.3 µmol/kg, respectively); enhances memory retrieval in rats in an inhibitory avoidance task at 0.7 and 1.4 mg/kg, i.p.

Formal name: 4-[(3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)propyl]-1-piperazineethanol

Synonyms:  cis-Clopenthixol|Cisordinol

Molecular weight: 401

CAS: 53772-83-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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