product name Paroxetine HCl
Description: Paroxetine hydrochloride (also known as BRL-29060A, FG-7051) is a selective serotonin uptake inhibitor (SSRI) that is effective in the treatment of depression. 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.
References: Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200.
365.83
Formula
C19H20FNO3.HCl
CAS No.
78246-49-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (199.5 mM)
Water: 10 mg/mL (27.3 mM)
Ethanol: 35 mg/mL (95.7 mM)
Solubility (In vivo)
Synonyms
BRL-29060A, FG-7051
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390472
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200. |
Related Posts
product name Paroxetine HCl
Description: Paroxetine hydrochloride (also known as BRL-29060A, FG-7051) is a selective serotonin uptake inhibitor (SSRI) that is effective in the treatment of depression. 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.
References: Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200.
365.83
Formula
C19H20FNO3.HCl
CAS No.
78246-49-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (199.5 mM)
Water: 10 mg/mL (27.3 mM)
Ethanol: 35 mg/mL (95.7 mM)
Solubility (In vivo)
Synonyms
BRL-29060A, FG-7051
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390472
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200. |