research use only
Cat.No.S4053
| Related Targets | Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) |
|---|---|
| Other Serotonin Transporter Inhibitors | Dapoxetine |
|
In vitro |
DMSO
: 69 mg/mL
(201.34 mM)
Ethanol : 15 mg/mL Water : Insoluble |
|
In vivo |
|||||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 342.69 | Formula | C17H17Cl2N.HCl |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 79559-97-0 | -- | Storage of Stock Solutions |
|
|
| Synonyms | CP-51974-1 HCl | Smiles | CNC1CCC(C2=CC=CC=C12)C3=CC(=C(C=C3)Cl)Cl.Cl | ||
| Targets/IC50/Ki |
5-HT
13 nM(Ki)
|
|---|---|
| In vitro |
Sertraline HCl exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, this compound is less selective for blocking 5-HT uptake, relative to DA uptake than these agents.
|
| In vivo |
Sertraline HCl (32μmol/kg i.p.) inhibits serotonin uptake into striatal synaptosomes from rats by more than 50%. This compound 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. This chemical strongly reduces immobility of mice in the Porsolt swim test for antidepressants. After repeated dosing in rats, it diminishes the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephnne, as well as the binding of [3H]dihydroalprenolol to cortical membranes.
|
References |
|
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05730062 | Not yet recruiting | Opioid Induced Respiratory Depression|Depressive Disorder|Anxiety Disorders |
Leiden University Medical Center |
March 15 2023 | Phase 1 |
| NCT05189977 | Terminated | Post-traumatic Stress Disorder (PTSD) |
Otsuka Pharmaceutical Development & Commercialization Inc.|Iqvia Pty Ltd |
September 7 2022 | Phase 1 |
| NCT05210153 | Recruiting | Depressive Disorder Major |
University of Belgrade|Clinical Centre of Serbia|Institute of Mental Health Serbia|Military Medical Academy Belgrade Serbia |
July 16 2020 | -- |
| NCT04147000 | Terminated | Overweight|Depression|Anxiety Disorders |
Linkoeping University|Örebro University Sweden |
January 1 2020 | -- |
| NCT03711708 | Completed | Healthy |
Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer |
November 6 2018 | Phase 4 |
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.