Home Neuronal Signaling Dopamine Receptor antagonist Phenothiazine For research use only.

Phenothiazine

Synonyms: ENT 38

Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.

Phenothiazine Chemical Structure

Phenothiazine Chemical Structure

CAS: 92-84-2

Purity & Quality Control

Batch: S425101 DMSO] 40 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.31%
99.31

Phenothiazine Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Choose Selective Dopamine Receptor Inhibitors

Biological Activity

Description Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
Targets
D2 receptor [2]
In vitro
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]

Chemical Information & Solubility

Molecular Weight 199.27 Formula

C12H9NS
CAS No. 92-84-2 SDF Download Phenothiazine SDF
Smiles C1=CC=C2C(=C1)NC3=CC=CC=C3S2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (200.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Tech Support

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