An atypical antipsychotic; a partial agonist at the 5-HT1A receptor (Ki = 180 nM); binds to the 5-HT2A

Clozapine – 100 mg

Brand:
Cayman
CAS:
5786-21-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Clozapine is a partial agonist at the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 180 nM).{22208,36950} It also binds to the 5-HT2A, 5-HT2C, 5-HT3, 5-HT6 and 5-HT7 receptors (Kis = 3.3, 13, 110, 4, and 21 nM, respectively), as well as the histamine H1 and α1-adrenergic receptors (Kis = 2.1 and 23 nM, respectively). It does not bind to the 5-HT1B receptor and has a lower affinity for dopamine receptors (Kis = 540, 150, and 360 nM for D1-3, respectively). Clozapine induces the release of glutamate and D-serine, an agonist at the glycine site of the NMDA receptor, from astrocytes, and reduces the expression of astrocytic glutamate transporters.{22207} It reverses locomotor hyperactivity and deficits in prepulse inhibition of acoustic startle in a rat neonatal ventral hippocampal ibotenic lesion model of schizophrenia when administered at a dose of 2.5 mg/kg per day.{39941} Formulations containing clozapine have been used in the treatment of schizophrenia.  

 

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Description

An atypical antipsychotic; a partial agonist at the 5-HT1A receptor (Ki = 180 nM); binds to the 5-HT2A, 5-HT2C, 5-HT3, 5-HT6 and 5-HT7 receptors (Kis = 3.3, 13, 110, 4, and 21 nM, respectively); binds to histamine H1 and α1-adrenergic receptors (Kis = 2.1 and 23 nM, respectively); induces the release of glutamate and D-serine from astrocytes; reverses locomotor hyperactivity and deficits in prepulse inhibition of acoustic startle in a rat neonatal ventral hippocampal ibotenic lesion model of schizophrenia at 2.5 mg/kg per day

Formal name: 8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine

Synonyms:  HF 1854

Molecular weight: 326.8

CAS: 5786-21-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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