| 名称 | Phenothiazine |
| 描述 | 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. |
| 体外活性 | 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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (225.82 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | inhibit | Antibiotic | antibacterial | neurological | Inhibitor | Bacterial | ENT-38 | fungicidal | Fungal | ENT38 | insecticidal | anthelmintic | Phenothiazine |
| 相关产品 | Neomycin sulfate | Dehydroacetic acid sodium | Potassium gluconate | Ampicillin sodium | Methyl anthranilate | Kanamycin sulfate | Sulfamethoxazole sodium | Metronidazole | Doxycycline | Geraniol | EDTA copper(II) disodium salt | Dimethyl sulfoxide |
| 相关库 | 神经退行性疾病化合物库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 抗真菌库 | 神经递质受体化合物库 | 药物片段库 | 已知活性化合物库 | GPCR靶点分子库 | 抗感染化合物库 |
United States
