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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Paroxetine HCl (formerly BRL-29060A, BRL29060A, FG7051; FG-7051), the hydrochloride salt of Paroxetine, is a potent and selective serotonin uptake inhibitor (SSRI) that is effective in the treatment of depression. It is commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM .Paroxetine binds to the pre-synaptic serotonin transporter complex resulting in negative allosteric modulation of the complex thereby blocking reuptake of serotonin by the pre-synaptic transporter. Paroxetine HCl has also displayed a high affinity for muscarinic acetylcholine receptors.
| ln Vitro |
By inhibiting GRK2, paroxetine (1 μM and 10 μM) significantly prevents T cell migration induced by CX3CL1. GRK2-induced ERK activation is inhibited by paroxetine [1]. Proinflammatory cytokines are decreased in LPS-stimulated BV2 cells by paroxetine (10 μM). TNF-α and IL-1β production in BV2 cells is dose-dependently inhibited by paroxetine (0-5 μM). Additionally, inducible nitric oxide synthase (iNOS) expression and lipopolysaccharide (LPS)-induced nitric oxide (NO) production are inhibited by paroxetine in BV2 cells. In BV2 cells, paroxetine (5 μM) reduces basal ERK1/2 activity and inhibits JNK activation triggered by LPS. In primary microglia, paroxetine inhibits NO production and LPS-stimulated pro-inflammatory cytokines, thereby reducing microglia-mediated neurotoxicity [4].
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| ln Vivo |
Treatment with paroxetine hydrochloride considerably reduced the CIA rats' symptoms. Treatment with paroxetine hydrochloride greatly decreased T cell infiltration into synovial tissue and prevented injury to joint tissue. In synovial tissue, the synthesis of CX3CL1 is strongly inhibited by paroxetine hydrochloride [1]. Rats' distal myocardium's myocyte cross-sectional area and ROS production are decreased by paroxetine hydrochloride (20 mg/kg/day). Ventricular tachycardia susceptibility is decreased by paroxetine hydrochloride. After MI, the administration of paroxetine hydrochloride decreases LV remodeling and arrhythmia susceptibility, maybe through lowering ROS production [2]. Paroxetine hydrochloride (10 mg/kg, ip) caused hyperalgesia on days 7 and 10 (P<0.01) in the CCI group, but on day 14, it decreased pain behavior. Furthermore, in comparison with the group given with the CCI vehicle, paroxetine hydrochloride (10 mg/kg) significantly reduced tactile hypersensitivity [5].
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| Additional Infomation |
Paroxetine hydrochloride is the hydrochloride salt of paroxetine. It is an antidepressant drug. It has a role as an antidepressant, an anxiolytic drug, a hepatotoxic agent, a P450 inhibitor and a serotonin uptake inhibitor. It contains a paroxetinium(1+).
Paroxetine Hydrochloride is the hydrochloride salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. Paroxetine binds to the pre-synaptic serotonin transporter complex resulting in negative allosteric modulation of the complex thereby blocking reuptake of serotonin by the pre-synaptic transporter. Inhibition of serotonin recycling enhances serotonergic function through serotonin accumulation in the synaptic cleft, resulting in long-term desensitization and downregulation of 5HT1 (serotonin) receptors and leading to symptomatic relief of depressive illness. A serotonin uptake inhibitor that is effective in the treatment of depression. See also: Paroxetine (annotation moved to). |
| Molecular Formula |
C19H20FNO3.HCL
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| Molecular Weight |
365.83
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| Exact Mass |
365.119
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| CAS # |
78246-49-8
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| Related CAS # |
Paroxetine;61869-08-7;Paroxetine-d4 hydrochloride;2714485-95-5;Paroxetine hydrochloride hemihydrate;110429-35-1;rel-Paroxetine-d4-1 hydrochloride;1217753-24-6
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| PubChem CID |
62878
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| Appearance |
White to off-white solid powder
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| Density |
1.213 g/cm3
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| Boiling Point |
451.7ºC at 760 mmHg
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| Melting Point |
129-131ºC
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| Flash Point |
227ºC
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| LogP |
4.457
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
402
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CNC[C@H]([C@@H]1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4.Cl
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| InChi Key |
GELRVIPPMNMYGS-RVXRQPKJSA-N
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| InChi Code |
InChI=1S/C19H20FNO3.ClH/c20-15-3-1-13(2-4-15)17-7-8-21-10-14(17)11-22-16-5-6-18-19(9-16)24-12-23-18;/h1-6,9,14,17,21H,7-8,10-12H2;1H/t14-,17-;/m0./s1
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| Chemical Name |
(3S,4R)-3-((benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.03 mg/mL (5.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05637671 | Recruiting | Drug: oxybutynin ER Drug: Paroxetine CR |
Vasomotor Symptoms | Cairo University | February 10, 2022 | Phase 3 |
| NCT01841502 | Terminated | Drug: Paroxetine Drug: telaprevir |
Hepatitis C Infection Depression |
Radboud University Medical Center | May 2013 | Phase 2 |
| NCT03504475 | Completed | Drug: Paroxetine Hydrochloride Tablet 20 mg Drug: Paxil® 20 mg |
Major Depressive Disorder Obsessive-Compulsive Disorder Panic Disorder |
Beijing Tongren Hospital | March 29, 2018 | Phase 1 |
| NCT00749359 | Completed | Drug: Paxil CR | Depressive Disorder | GlaxoSmithKline | July 7, 2008 | Phase 1 |
| NCT00841659 | Completed Has Results | Drug: Paroxetine HCl Drug: Paxil® |
Healthy | Teva Pharmaceuticals USA | August 2002 | Phase 1 |
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