Paroxetine HCl

製品コードS3005 バッチS300502

化学情報

	Synonyms	BRL-29060A, FG-7051	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₂₀FNO₃.HCl
	分子量	365.83	CAS No.	78246-49-8
Solubility (25°C)*	体外	DMSO	73 mg/mL (199.54 mM)
		Ethanol	35 mg/mL (95.67 mM)
		Water	1 mg/mL (2.73 mM)
* <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	Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type.
in vitro	Paroxetine apparently exerts their antidepressant activity by increasing the concentration of 5-HT in the extracellular compartment, thereby enhancing serotoninergic neurotransmission. Paroxetine (1-300 μM) results in a concentration-dependent reduction in the firing rate of DRN serotoninergic neurons with IC50 values of 1.4 μM in the ACSF superfusing brain stem slices. ^[1] Paroxetine is a highly potent inhibitor of desipramine hydroxylation, the inhibition constant (Ki) value of 2.0 mM indicated greater inhibiting potency than fluoxetine or norfluoxetine. ^[2] Paroxetine is shown to be a potent (Ki = 1.1 nM) and specific inhibitor of [3H]-5-hydroxytryptamine (5-HT) uptake into rat cortical and hypothalamic synaptosomes in vitro. Paroxetine demonstrates weak affinity for muscarinic receptors (Ki = 89 nM) but is at least 15 fold weaker than amitriptyline (Ki = 5.1 nM). ^[3] Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex. ^[4]
in vivo	Paroxetine produces a dose-related inhibition of [3H]-5-HT uptake (ED50 = 1.9 mg/kg) into rat hypothalamic synaptosomes ex vivo with little effect on [3H]-l-noradrenaline (NA) uptake (ED50 greater than 30 mg/kg). Paroxetine (ED50 1-3 mg/kg PO) prevents the 5-HT depleting effect of p-chloroamphetamine (PCA) in rat brain, demonstrating 5-HT uptake blockade in vivo. ^[3]

プロトコル(参考用のみ)

参考

[4] Bertelsen KM, et al. Drug Metab Dispos, 2003, 31(3), 289-293.

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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：

Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034]	PubMed: 35641493
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A multi-residue analytical method for extraction and analysis of pharmaceuticals and other selected emerging contaminants in sewage sludge [ Anal Methods, 2021, 10.1039/d0ay02027c]	PubMed: 33447838

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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