An atypical antipsychotic; binds to D2 dopamine and 5-HT1D

Sertindole – 10 mg

Brand:
Cayman
CAS:
106516-24-9
Storage:
-20
UN-No:
Non-Hazardous - /

Sertindole is an atypical antipsychotic that binds to dopamine D2 receptors and the serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 2.7, 20, 0.14, and 6 nM, respectively).{25511} It also binds to histamine H1 and α1- and α2-adrenergic receptors (Kds = 320, 3.9, and 190 nM, respectively). In vivo, sertindole (10 mg/kg) increases extracellular dopamine, acetylcholine (ACh), and glutamate levels in the medial prefrontal cortex in conscious rats.{36801} Sertindole (2.5 mg/kg) reverses ketamine-induced impairments in the extradimensional shift stage of the attentional set-shifting task (ASST) in rats.{36802} It reverses phencyclidine (PCP)-induced selective reversal learning deficits in rats and subchronic PCP-induced deficits in the novel object recognition task in mice.{36803} Sertindole (0.02-0.32 mg/kg) also prevents accuracy deficits and anticipatory over-responding in the 5-choice serial reaction time task (5CSRTT) induced by the NMDA receptor antagonist (R)-CPP (Item No. 21569) in rats.{36804} Formulations containing sertindole have been used in the treatment of schizophrenia.  

 

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Description

An atypical antipsychotic; binds to D2 dopamine and 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kds = 2.7, 20, 0.14, and 6 nM, respectively); binds to histamine H1 and α1- and α2-adrenergic receptors (Kds = 320, 3.9, and 190 nM, respectively); increases extracellular dopamine, ACh, and glutamate levels in the medial prefrontal cortex in concious rats at 10 mg/kg; reverses ketamine-induced impairments in the extradimensional shift stage of the ASST in rats at 2.5 mg/kg; reverses phencyclidine-induced selective reversal learning deficits in rats and subchronic phencyclidine-induced deficits in the novel object recognition task in mice; prevents accuracy deficits and anticipatory over-responding in the 5CSRTT in rats

Formal name: 1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl]ethyl]-2-imidazolidinone

Synonyms: 

Molecular weight: 440.9

CAS: 106516-24-9

Purity: ≥95%

Formulation: A crystalline solid

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

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