product name Sertraline HCl
Description: Sertraline HCl (also known as CP-51974-1 HCl) is a 5-HT antagonist with Ki of 13 nM. Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents.
References: J Pharmacol Exp Ther. 1983 Sep;226(3):686-700.
342.69
Formula
C17H17Cl2N.HCl
CAS No.
79559-97-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 69 mg/mL (201.3 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (43.8 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% Propylene glycol: 5 mg/mL
Synonyms
CP-51974-1 HCl
other peoduct :
| In Vitro |
In vitro activity: Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Sertraline HCl (32μmol/kg i.p.) inhibits serotonin uptake into striatal synaptosomes from rats by more than 50%. Sertraline HCl is 6 times more potent than chlorimipramine and 60 times more potent than amitriptyline in reversing the 5-HT depletion elicited by PCA. Acute and repeated dosing of sertraline decreased serotonin content of whole blood. Sertraline HCl strongly reduces immobility of mice in the Porsolt swim test for antidepressants. After repeated dosing in rats, sertraline HCl diminishes the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephnne, as well as the binding of [3H]dihydroalprenolol to cortical membranes. |
| Animal model | |
| Formulation & Dosage | |
| References |
