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Cyamemazine

Catalog No. T15026 CAS 3546-03-0

Cyamemazine, contains the phenothiazine chromophore, is a neuroleptic agent used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki: 12 nM), 5-HT2A (Ki: 1.5 nM) and 5-HT2C (Ki: 75 nM) receptors antagonist with antipsychotic activity.

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Cyamemazine, CAS 3546-03-0

Pack Size	Availability	Price/USD
2 mg	5 days	$ 131.00
50 mg	6-8 weeks	$ 744.00
100 mg	6-8 weeks	$ 1,120.00

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Biological Description

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Storage & Solubility Information

Description	Cyamemazine, contains the phenothiazine chromophore, is a neuroleptic agent used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki: 12 nM), 5-HT2A (Ki: 1.5 nM) and 5-HT2C (Ki: 75 nM) receptors antagonist with antipsychotic activity.
Targets&IC50	5-HT2C receptor:12 nM （ki）, 5-HT2A receptor:1.5 nM （ki）, 5-HT3 receptor:75 nM （ki）
In vitro	Cyamemazine shows a high affinity for dopamine receptors. It is consistent with its antipsychotic activity. At muscarinic receptors, the antagonist activity of Cyamemazine is consistent with its affinity for M1 (Ki: 13 nM), M2 (Ki: 42 nM), M3 (Ki: 321 nM), M4 (Ki: 12 nM), and M5 (Ki: 35 nM) receptors [1].
In vivo	Cyamemazine act as an antagonist at the 5-HT3, 5-HT2C, and 5-HT2A receptors in 5-HT3-dependent contraction of isolated guinea pig ileum and bradycardic responses in rats in 5-HT2C-dependent phospholipase C stimulation in the rat brain membrane, and in 5-HT2A-dependent contraction of isolated rat aorta rings and isolated guinea pig trachea. Acute administration of low doses of Cyamemazine can reduces extracellular dopamine and metabolite concentrations in rat striatum [1].

Molecular Weight	323.46
Formula	C19H21N3S
CAS No.	3546-03-0

Storage

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

References and Literature

1. Bourin M, et al. Preclinical and clinical pharmacology of cyamemazine: anxiolytic effects and prevention of alcohol and benzodiazepine withdrawal syndrome. CNS Drug Rev. 2004 Fall;10(3):219-29. 2. Vendrell-Criado V, et al. Photobehavior of the antipsychotic drug cyamemazine in a supramolecular gel protective environment. J Photochem Photobiol B. 2020 Jan;202:111686.

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Keywords

Cyamemazine 3546-03-0 GPCR/G Protein Neuroscience 5-HT Receptor inhibitor inhibit

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