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Amoxapine

Catalog No. T1568 CAS 14028-44-5

Synonyms: CL-67772

Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.

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Amoxapine, CAS 14028-44-5

Pack Size	Availability	Price/USD	Quantity
500 mg	In stock	$ 64.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 98.84%

Purity: 98.25%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.
Targets&IC50	GlyT1b:1 mM, GlyT2a:92 μM
In vitro	Amoxapine, administered intraperitoneally (i.p.) at doses of 1, 5, and 10 mg/kg, notably at lower doses, was found to decrease paradoxical sleep and increase slow-wave sleep. Throughout the treatment period, a consistent reduction in paradoxical sleep was observed with Amoxapine (10 mg/kg, i.p.), although tolerance to the inhibition effect of cericlamine was noted in this sleep phase. Additionally, Amoxapine (10 mg/kg/day) did not affect the levels of Substance P, dynorphin, and cholecystokinin, but significantly increased leucine-enkephalin levels in the rat cortex, spinal cord, and hypothalamus. Despite not altering opioid receptor binding in the rat cortex, Amoxapine (10 mg/kg/day, i.p.) increased the density of δ- and μ-opioid receptor binding sites in the spinal cord and decreased it in the hypothalamus. Moreover, Amoxapine attenuated spontaneous activity, induced catalepsy and ptosis, and exhibited inhibitory effects on the dyskinetic movements induced by Apomorphine and stereotypy behaviors induced by amphetamine, through altering avoidance behaviors discerned by monkeys.
In vivo	In both oocytes and HEK 293 cells, Amoxapine induces acute hERG channel blockade with IC50 values of 21.6 and 5.1 μM, respectively. In human embryonic kidney 293 cells, it selectively inhibits GLYT2a over its isotype GLYT1b by a factor of 10. Amoxapine leads to a blockade of reverse frequency dependence and causes a leftward shift with accelerated inactivation. Treatment with Amoxapine results in a gradual reduction of hERG transport to the cell membrane surface in HEK 293 cells, with an IC50 of 15.3 μM.

Synonyms	CL-67772
Molecular Weight	313.78
Formula	C17H16ClN3O
CAS No.	14028-44-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (31.87 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Núñez E, et al. Br J Pharmacol. 2000 Jan;129(1):200-6. 2. Obers S, et al. Naunyn Schmiedebergs Arch Pharmacol, 2010, 381(5), 385-400. 3. Hamon M, et al. Neuropharmacology, 1987, 26(6), 531-539. 4. Maudhuit C, et al. Neuropharmacology, 1994, 33(8), 12017-1025. 5. Greenblatt EN, et al. Arch Int Pharmacodyn Ther, 1978, 233(1), 107-135.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library FDA-Approved Drug Library NO PAINS Compound Library ReFRAME Related Library Neuronal Signaling Compound Library Human Metabolite Library Glutamine Metabolism Compound Library Antidepressant Compound Library

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Keywords

Amoxapine 14028-44-5 Neuroscience GlyT inhibit Inhibitor CL-67772 CL 67772 CL67772 inhibitor

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