Home Neuronal Signaling Dopamine Receptor antagonist Phenothiazine

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Phenothiazine Dopamine Receptor antagonist

Cat.No.S4251

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

Chemical Structure

Molecular Weight: 199.27

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (200.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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 add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 199.27 Formula

C12H9NS

 Storage (From the date of receipt)
CAS No. 92-84-2 Download SDF Storage of Stock Solutions

Synonyms ENT 38 Smiles C1=CC=C2C(=C1)NC3=CC=CC=C3S2

Mechanism of Action

Targets/IC50/Ki
D2 receptor
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-carbamoylalkyl derivatives shows significant activities against Gram-positive Bacillus subtilis with MIC’s in the range of 7.8 μg/mL–30 μg/mL. The tetracyclic compounds (modified with the naphthoquinone ring) shows significant actibacterial activity against S. aureus with the MIC50 of 12.5 μg/mL. These compounds 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)propyl derivatives (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. This class of drugs undergo extensive metabolism in the body before being excreted, mainly ring hydroxylation, ring sulphoxidation, N-demethylation, N-oxidation, sulphate and glucuronide conjugation. They have considerably lower binding affinities to α2-adrenoceptors than to dopamine D2 receptors and al-adrenoceptors. These compounds 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.
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