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Technical Data
| Formula | C18H19ClN4 |
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| Molecular Weight | 326.82 | CAS No. | 5786-21-0 | |
| Solubility (25°C)* | In vitro | DMSO | 65 mg/mL (198.88 mM) | |
| Ethanol | 32 mg/mL (97.91 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| 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. | |
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| In vitro | Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus. [1] Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen. [2] Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist. [3] 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. [4] 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. [5] | |
| 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. [6] |
Protocol (from reference)
References
Customer Product Validation
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, , Drug Metab Dispos, 2015, 43(7):1147-53.
Selleck's Clozapine has been cited by 9 publications
| Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] | PubMed: 39581704 |
| Amisulpride as a potential disease-modifying drug in the treatment of tauopathies [ Alzheimers Dement, 2023, 10.1002/alz.13090] | PubMed: 37218673 |
| Clozapine suppresses NADPH oxidase activation, counteracts cytosolic H2O2, and triggers early onset mitochondrial dysfunction during adipogenesis of human liposarcoma SW872 cells [ Redox Biol, 2023, 67:102915] | PubMed: 37866162 |
| A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] | PubMed: 33517273 |
| Neocortical Slow Oscillations Implicated in the Generation of Epileptic Spasms [ Ann Neurol, 2020, 10.1002/ana.25935] | PubMed: 33068018 |
| The evolution of a series of behavioral traits is associated with autism-risk genes in cavefish. [ BMC Evol Biol, 2018, 18(1):89] | PubMed: 29909776 |
| Pharmacokinetic Evaluation of Clozapine in Concomitant Use of Radix Rehmanniae, Fructus Schisandrae, Radix Bupleuri, or Fructus Gardeniae in Rats. [ Molecules, 2016, 21(6)] | PubMed: 27240333 |
| In Vitro Effects of Concomitant Use of Herbal Preparations on Cytochrome P450s Involved in Clozapine Metabolism [ Molecules, 2016, 21(5)597] | PubMed: 27164071 |
| Peony-Glycyrrhiza Decoction, an Herbal Preparation, Inhibits Clozapine Metabolism via Cytochrome P450s, but Not Flavin-Containing Monooxygenase in In Vitro Models. [Wang W, et al. Drug Metab Dispos, 2015, 43(7):1147-53] | PubMed: 25948710 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.