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 No. 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

Amoxapine Related Products

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 Information & 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


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In vivo
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