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Phenothiazine

Catalog No. T0776 CAS 92-84-2

Synonyms: ENT 38

Phenothiazine (ENT 38) is a class of agents exhibiting antiemetic, antipsychotic, antihistaminic, and anticholinergic activities. Phenothiazines antagonize the dopamine D2-receptor in the chemoreceptor trigger zone (CTZ) of the brain, potentially preventing chemotherapy-induced emesis.

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Phenothiazine, CAS 92-84-2

Pack Size	Availability	Price/USD	Quantity
500 mg	In stock	$ 42.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.94%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

In vitro

Phenothiazines mostly substitutes at position 10 with the dialkylaminoalkyl groups and additionally at position 2 with small groups exhibit valuable activities such as neuroleptic, antiemetic, antihistaminic, antipuritic, analgesic and antihelmintic. 2-trifluoromethyl-10-(4-aminobutyl)phenothiazine inhibits S. cerevisiae strains and T. mentagrophites with MIC of 0.4 μg/mL and 1.5 μg/mL, respectively. 10-carbamoylalkylphenothiazines shows significant activities against Gram-positive Bacillus subtilis with MIC's in the range of 7.8 μg/mL–30 μg/mL. The tetracyclic phenothiazines (modified with the naphthoquinone ring) shows significant actibacterial activity against S. aureus with the MIC50 of 12.5 μg/mL. Phenothiazines with the butylene linker are more effective than with the propylene linker, the 2-chloro-10-chloroethylureidobutyl derivative giving GI50 of 1.4 μM and 1.6 μM against 4 leukemia cell lines and 7 colon cancer cell lines. 10-Amino(hydroxy)propylphenothiazines (5 μM) induces a marked G2/M phase of cell-cycle arrest followed by cell death in human transformed WI38VA cells after 2-day incubation. [1] Phenothiazine drugs undergo extensive metabolism in the body before being excreted, mainly ring hydroxylation, ring sulphoxidation, N-demethylation, N-oxidation, sulphate and glucuronide conjugation. Phenothiazines have considerably lower binding affinities to α2-adrenoceptors than to dopamine D2 receptors and al-adrenoceptors. [2] Phenothiazines have significant in vitro activity against susceptible, polydrug- and multidrug-resistant strains of M. tuberculosis, as well as enhancing the activity of some agents employed for first-line treatment. [3]

Synonyms	ENT 38
Molecular Weight	199.27
Formula	C12H9NS
CAS No.	92-84-2

Storage

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

Solubility Information

DMSO: 38 mg/mL (190.7 mM)

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

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

References and Literature

1. Pluta K, et al. Eur J Med Chem, 2011, 46(8), 3179-3189. 2. Hals PA, et al. Eur J Pharmacol, 1986, 125(3), 373-381. 3. Amaral L, et al. J Antimicrob Chemother, 2001, 47(5), 505-511.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Infection Compound Library Anti-Fungal Compound Library Antibiotics Library Anti-Parkinson's Disease Compound Library Neuronal Signaling Compound Library Anti-Bacterial Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Phenothiazine 92-84-2 GPCR/G Protein Microbiology/Virology Neuroscience Dopamine Receptor Antibacterial Antibiotic Antifungal inhibit antibacterial ENT 38 neurological Inhibitor Bacterial ENT-38 fungicidal Fungal ENT38 insecticidal anthelmintic inhibitor

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