Clozapine

製品コードS2459 バッチS245902

化学情報

	Synonyms	HF 1854, LX 100-129	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₉ClN₄
	分子量	326.82	CAS No.	5786-21-0
Solubility (25°C)*	体外	DMSO	65 mg/mL (198.88 mM)
		Ethanol	10 mg/mL (30.59 mM)
		Water	Insoluble
* <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.

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生物活性

製品説明	Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
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]

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: , , Drug Metab Dispos, 2015, 43(7):1147-53.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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