Catalog No.S2459 Synonyms: HF 1854, LX 100-129
Molecular Weight(MW): 326.82
Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
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Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON).
Drug Metab Dispos, 2015, 43(7):1147-53.. Clozapine purchased from Selleck.
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|Description||Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.|
Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus.  Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen.  Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist.  Clozapine produces a marked facilitation (300-400%) of NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. Clozapine, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids.  Clozapine is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. Clozapine potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes. 
|In vivo||Clozapine exhibits an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of prepulse inhibition (PPI) at low doses but not at high doses in the rats. Clozapine decreases PPI independent of apomorphine treatment in the rats. |
-  Robertson GS, et al. Neuroscience, 1992, 46(2), 315-328.
-  Nguyen TV, et al. Proc Natl Acad Sci U S A, 1992, 89(10), 4270-4274.
-  Brunello N, et al. Neuropsychopharmacology, 1995, 13(3), 177-213.
|In vitro||DMSO||65 mg/mL (198.88 mM)|
|Ethanol||32 mg/mL (97.91 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||HF 1854, LX 100-129|
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02600741||Completed||Schizophrenia||Janssen Scientific Affairs LLC||July 24 2015||--|
|NCT02926976||Recruiting||Schizophrenia||Shanghai Mental Health Center||November 2016||Not Applicable|
|NCT02893371||Enrolling by invitation||Bipolar Disorder||University of New Mexico|Patient-Centered Outcomes Research Institute|Montana State University|National Alliance on Mental Illness|CGStat LLC|Risk Benefit Statistics LLC||September 2016||--|
|NCT02639702||Recruiting||Schizophrenia|Schizoaffective Disorder||Centre for Addiction and Mental Health||August 2016||Phase 4|
|NCT02714894||Recruiting||Schizophrenia||Centre for Addiction and Mental Health|Canadian Institutes of Health Research (CIHR)||April 2016||--|
|NCT02562287||Unknown status||Bipolar Disorder||Hospital de Clinicas de Porto Alegre|Coordenação de Aperfeiçoamento de Pessoal de Nível Superior.|Conselho Nacional de Desenvolvimento Científico e Tecnológico||October 2015||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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