rel-Paroxetine hydrochloride

Modify Date: 2024-01-14 17:29:44

rel-Paroxetine hydrochloride Structure
rel-Paroxetine hydrochloride structure
Common Name rel-Paroxetine hydrochloride
CAS Number 1217683-35-6 Molecular Weight 369.851
Density N/A Boiling Point N/A
Molecular Formula C19H17D4ClFNO3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of rel-Paroxetine hydrochloride


rel-Paroxetine hydrochloride is a 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].

 Names

Name (3S,4R)-3-[(1,3-Benzodioxol-5-yloxy)methyl]-4-[4-fluoro(2H4)phenyl]piperidine hydrochloride (1:1)
Synonym More Synonyms

 rel-Paroxetine hydrochloride Biological Activity

Description rel-Paroxetine hydrochloride is a 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].
Related Catalog
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].
In Vivo Paroxetine (15 mg/kg/d; p.o.; 15 d) obviously attenuates the symptoms of collagen-induced arthritis (CIA) rats[2]. 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.

 Chemical & Physical Properties

Molecular Formula C19H17D4ClFNO3
Molecular Weight 369.851
Exact Mass 369.144501

 Synonyms

(3S,4R)-3-[(1,3-Benzodioxol-5-yloxy)methyl]-4-[4-fluoro(2H4)phenyl]piperidine hydrochloride (1:1)
Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl-2,3,5,6-d4)-, (3S,4R)-, hydrochloride (1:1)