For research use only.
Catalog No.S3005 Synonyms: BRL-29060A, FG-7051
CAS No. 78246-49-8
Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type.
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|Description||Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type.|
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.  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.  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).  Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex. 
|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. |
-  Le Poul E, et al. Naunyn Schmiedebergs Arch Pharmacol, 1995, 352(2), 141-148.
-  von Moltke LL, et al. J Clin Psychopharmacol, 1995, 15(2), 125-131.
-  Thomas DR, et al. Psychopharmacology (Berl), 1987, 93(2), 193-200.
|In vitro||DMSO||73 mg/mL (199.54 mM)|
|Water||1 mg/mL (2.73 mM)|
|Ethanol||''' 35 mg/mL|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03329573||Completed||Drug: Paroxetine IR tablets A|Drug: Paroxetine IR tablets B||Anxiety Disorders||GlaxoSmithKline||May 30 2018||Phase 1|
|NCT02932904||Completed||Drug: Vortioxetine|Drug: Paroxetine|Drug: Placebo||Healthy Volunteers||Takeda||November 21 2016||Phase 4|
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