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  3. rel-Paroxetine-d4 hydrochloride

rel-Paroxetine-d4 hydrochloride  (Synonyms: rel-BRL29060-d4 hydrochloride; rel-BRL29060A-d4)

Cat. No.: HY-151216S
Handling Instructions

rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].

For research use only. We do not sell to patients.

rel-Paroxetine-d<sub>4</sub> hydrochloride Chemical Structure

rel-Paroxetine-d4 hydrochloride Chemical Structure

CAS No. : 1217683-35-6

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Description

rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].

IC50 & Target

IC50: 14 μM (GRK2)[2]; Serotonin-reuptake[4]

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Paroxetine (1 μM and 10 μM; 4 h) distinctly restrains T cell migration induced by CX3CL1 through inhibiting GRK2[2].
Paroxetine (16 h) inhibits GRK2 induced activation of ERK in splenic T cells[2].
Paroxetine (10 μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells[3].
Paroxetine (0-5 μM) leads to a dose-dependent inhibition on LPS-induced production of TNF-α and IL-1β in BV2 cells[3].
Paroxetine also inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in BV2 cells[3].
Paroxetine (5 μM) blocks LPS-induced JNK activation and attenuates baseline ERK1/2 activity in BV2 cells[3].
Paroxetine relieves microglia-mediated neurotoxicity, and suppresses LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Paroxetine (15 mg/kg/d; p.o.; 15 d) obviously attenuates the symptoms of collagen-induced arthritis (CIA) rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Collagen-induced arthritis (CIA) model in rats (around 14-day-old)[2]
Dosage: 15 mg/kg
Administration: Oral gavage; once daily; 15 days
Result: Helped CIA rats to restore more body weight.
Molecular Weight

369.85

Formula

C19H17D4ClFNO3

CAS No.
SMILES

FC(C([2H])=C1[2H])=C([2H])C([2H])=C1[C@H](CCNC2)[C@@H]2COC3=CC=C(OCO4)C4=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
rel-Paroxetine-d4 hydrochloride
Cat. No.:
HY-151216S
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