Home Neuronal Signaling Serotonin Transporter inhibitor - 5-HT Receptor inhibitor Sertraline HCl For research use only.

Sertraline HCl

Synonyms: CP-51974-1 HCl

Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.

Sertraline HCl Chemical Structure

Sertraline HCl Chemical Structure

CAS No. 79559-97-0

Purity & Quality Control

Sertraline HCl Related Products

Biological Activity

Description Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.
Targets
5-HT [1]
13 nM(Ki)
In vitro
In vitro 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. [1]
In Vivo
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. [1]
Animal Research Animal Models Rats, Mice
Dosages --
Administration i.p.
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

Chemical Information & Solubility

Molecular Weight 342.69 Formula

C17H17Cl2N.HCl
CAS No. 79559-97-0 SDF --
Smiles CNC1CCC(C2=CC=CC=C12)C3=CC(=C(C=C3)Cl)Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (201.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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