[CAS NO. 78246-49-8]  Paroxetinehydrochloride

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PRODUCTS SPECIFICATIONS [78246-49-8]

Catalog
HY-B0492
Brand
MCE
CAS
78246-49-8

DESCRIPTION [78246-49-8]

Overview

MDLMFCD00797405
Molecular Weight365.83
Molecular FormulaC19H21ClFNO3
SMILESFC1=CC=C([C@H]2[C@H](COC3=CC=C(OCO4)C4=C3)CNCC2)C=C1.Cl

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


Summary

Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC 50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder [1] [2] [3] .


IC50 & Target

IC50: 14 μM (GRK2) [3]


In Vitro

Paroxetine (1 μM and 10 μM) distinctly restrains T cell migration induced by CX3CL1 through inhibiting GRK2. Paroxetine inhibits GRK2 induced activation of ERK [1] . Paroxetine (10 μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells. Paroxetine (0-5 μM) leads to a dose-dependent inhibition on LPS-induced production of TNF-α and IL-1β in BV2 cells. Paroxetine also inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in BV2 cells. Paroxetine (5 μM) blocks LPS-induced JNK activation and attenuates baseline ERK1/2 activity in BV2 cells. Paroxetine relieves microglia-mediated neurotoxicity, and suppresses LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells [4] .

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


In Vivo

Paroxetine treatment obviously attenuates the symptoms of CIA rats. Paroxetine treatment clearly prevents the histological damage of joints and alleviates T cells infiltration into synovial tissue. Paroxetine reveals a strong effect on inhibiting CX3CL1 production in synovial tissues [1] . Paroxetine (20 mg/kg/day) reduces the myocyte cross-sectional area in rat and ROS formation in the remote myocardium. Paroxetine reduces the susceptibility to ventricular tachycardia. Paroxetine treatment following MI decreases LV remodeling and susceptibility to arrhythmias, probably by reducing ROS formation [2] . In CCI paroxetine-treated group, paroxetine (10 mg/kg, i.p.) produces hyperalgesia at days 7 and 10 (P<0.01), but a decrease in pain behavior is seen at day 14. Moreover, paroxetine (10 mg/kg) significantly attenuates tactile hypersensitivity when compared to CCI vehicle-treated group [5] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01602913 GlaxoSmithKline
Depression, Postpartum
December 2011
NCT05175430 University Hospital, Basel, Switzerland
Healthy
October 24, 2022 Phase 1
NCT02279966 H. Lundbeck A+S
Major Depressive Disorder
October 2014 Phase 3

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 273.35 mM ; Need ultrasonic)

H 2 O : 5 mg/mL ( 13.67 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7335 mL 13.6676 mL 27.3351 mL
5 mM 0.5467 mL 2.7335 mL 5.4670 mL
10 mM 0.2734 mL 1.3668 mL 2.7335 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

  • 4.

    Add each solvent one by one: PBS

    Solubility: 2.03 mg/mL (5.55 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride (1:1), (3S,4R)-
Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride, (3S-trans)-
Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride, (3S,4R)-
Paroxetine hydrochloride
BRL 29060 hydrochloride
BRL 29060A
Paxil
(-)-trans-4-(4-Fluorophenyl)-3-(3,4-methylenedioxyphenoxymethyl)piperidine hydrochloride
Seroxat
Aropax 20
Tagonis
Deroxat
Paroxet
Xanadol