For research use only.
Catalog No.S2459 Synonyms: HF 1854, LX 100-129
CAS No. 5786-21-0
Clozapine (HF 1854, LX 100-129) 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 (HF 1854, LX 100-129) 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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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04325386||Recruiting||Other: Education Sessions|Other: No Education Session||Schizophrenia Schizoaffective||University of Maryland Baltimore||October 15 2020||Not Applicable|
|NCT03996356||Not yet recruiting||Other: No study intervention - observational study||Weight Gain|Antipsychotic Agents|Pharmacogenetics||Cwm Taf University Health Board (NHS)||March 2020||--|
|NCT04074213||Recruiting||Drug: Clozapine||Lymphoma|Leukemia||University Hospital Caen||March 1 2019||--|
|NCT03076346||Recruiting||--||Schizophrenia|Treatment-resistant Schizophrenia|Schizoaffective Disorder||University of Pittsburgh||September 1 2017||--|
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