Home Neuronal Signaling GlyT inhibitor - Amino acid transporter inhibitor Amoxapine For research use only.

Amoxapine

Synonyms: CL 67772,Asendin

Amoxapine (CL 67772,Asendin) is a tricyclic dibenzoxazepine (an N-aryl piperazine) which acts similarly to several other tricyclic antidepressants, amoxapine inhibits GLYT2a transport activity with IC50 of 92 μM.

Amoxapine Chemical Structure

Amoxapine Chemical Structure

CAS: 14028-44-5

Purity & Quality Control

Batch: S421801 DMSO] 3.1 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.22%
99.22

Related compound libraries

Choose Selective GlyT Inhibitors

Biological Activity

Description Amoxapine (CL 67772,Asendin) is a tricyclic dibenzoxazepine (an N-aryl piperazine) which acts similarly to several other tricyclic antidepressants, amoxapine inhibits GLYT2a transport activity with IC50 of 92 μM.
Targets
GlyT2a [1] GlyT1b [1]
92 μM 1 mM
In vitro
In vitro

Amoxapine displays a selective inhibition of GLYT2a behaving as a 10 fold more efficient inhibitor of this isoform than of GLYT1b in human embryonic kidney 293 cells. Amoxapine behaves as a competitive inhibitor of both glycine and chloride and a mixed-type inhibitor with respect to sodium. [1] Amoxapine causes acute hERG blockade in oocytes with IC50 of 21.6 mM and in HEK 293 cells with IC50 of 5.1 mM. Amoxapine block is reverse frequency-dependent and causes accelerated and leftward-shifted inactivation. Amoxapine application results in chronic reduction of hERG trafficking into the cell surface membrane with IC50 of 15.3 mM in HEK 293 cells. [2]
In Vivo
In vivo

Amoxapine (10 mg/kg i.p., daily) does not affect the levels of dynorphin, substance P and cholecystokinin, but markedly enhances the levels of leu-enkephalin in spinal cord, cerebral cortex and hypothalamus of rats. Amoxapine (10 mg/kg i.p., daily) results in no changes in opioid receptors in the cerebral cortex, but the densities of delta and mu opioid binding sites are increased in the spinal cord, and decreased in the hypothalamus of rats. [3] Amoxapine (1 mg/kg, 5 mg/kg and 10 mg/kg; i.p.) decreases paradoxical sleep and increases deep slow wave sleep especially when it is given at a low dose. Amoxapine (10 mg/kg; i.p.) induces a sustained decrease of paradoxical sleep during the whole treatment, while some tolerance is observed with regard to the inhibitory effect of cericlamine on this state of sleep. [4] Amoxapine decreases locomotor activity, induce ptosis and catalepsy, inhibits apomorphine gnawing and amphetamine stereotyped behavior and by characteristic changes in monkey discriminated avoidance behavior. [5]

Chemical lnformation & Solubility

Molecular Weight 313.78 Formula

C17H16ClN3O
CAS No. 14028-44-5 SDF Download Amoxapine SDF
Smiles C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 3.1 mg/mL ( (9.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Amoxapine | Amoxapine ic50 | Amoxapine price | Amoxapine cost | Amoxapine solubility dmso | Amoxapine purchase | Amoxapine manufacturer | Amoxapine research buy | Amoxapine order | Amoxapine mouse | Amoxapine chemical structure | Amoxapine mw | Amoxapine molecular weight | Amoxapine datasheet | Amoxapine supplier | Amoxapine in vitro | Amoxapine cell line | Amoxapine concentration | Amoxapine nmr