Amoxapine

Catalog No.S4218 Synonyms: CL 67772,Asendin

For research use only.

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

CAS No. 14028-44-5

Purity & Quality Control

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

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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

1mg/mL

Chemical Information

Molecular Weight 313.78
Formula

C17H16ClN3O

CAS No. 14028-44-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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