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Purity: ≥98%
Phenothiazine (NSC 2037; ENT38; ENT 38; NSC-2037) is a potent dopamine-2 (D2) receptor antagonist used as antipsychotic medications for the treatment of schizophrenia and manifestations of psychotic disorders. It acts by preventing the dopamine-2 (D2) receptor, which lessens dopamine's effects on the brain.
| Targets |
D2 receptor
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
BECAUSE OF ITS LOW SOLUBILITY, RATE OF ITS ABSORPTION FROM GI TRACT IS DEPENDENT ON PARTICLE SIZE. MICRONIZED FORM OF DRUG IS ABSORBED RAPIDLY. ...ABOUT 30-50% OF ORAL DOSE PASSES THROUGH ALIMENTARY TRACT UNCHANGED. SOME PHENOTHIAZINE IS CONVERTED WITHIN GUT TO SOL DERIV...WHICH ARE ABSORBED INTO PORTAL VENOUS SYSTEM. ...DERIV ARE SECRETED IN URINE & ARE RESPONSIBLE FOR ITS RED COLOR WHEN EXPOSED TO AIR. THEY ALSO APPEAR IN BILE & IN MILK OF LACTATING ANIMALS. URINARY & FECAL EXCRETION OF PHENOTHIAZINE OR ITS DERIV ACCOUNTS FOR 80% OF ORAL DOSE IN SHEEP; FATE OF REMAINING 20% IS UNKNOWN. URINARY & FECAL EXCRETION OF PHENOTHIAZINE OR ITS DERIV ACCOUNTS FOR 80% OF ORAL DOSE IN SHEEP; FATE OF REMAINING 20% IS UNKNOWN. ABSORBED BY SKIN. ... Phenothiazine was readily absorbed from the alimentary tract, with the free drug and reddish oxidation products appearing in the urine. Metabolism / Metabolites SOME PHENOTHIAZINE IS CONVERTED WITHIN GUT TO SOL DERIV, MAINLY PHENOTHIAZINE SULFATE... YIELDS 3-HYDROXYPHENOTHIAZINE IN DOGS. /FROM TABLE/ THE ANTHELMINTIC, PHENOTHIAZINE, WAS OXIDIZED TO SULFOXIDE BY ENZYMES OF THE PROGLOTTIDS OF THE CESTODE, MONIEZIA EXPANSA & CYTOSOL OF INTESTINAL EPITHELIAL CELLS OF THE NEMATODE ASCARIS SUUM. ENZYMES IN THESE TISSUES ALSO DECR SULFOXIDES TO THIOETHERS IN ABSENCE OF O. RAT, MOUSE, & GERBIL EXCRETED THE MAJORITY OF PHENOTHIAZINE IN CONJUGATED FORM. THE RAT, MOUSE, & GERBIL PRODUCED LEUCOPHENOTHIAZONE SULFATE AS MAJOR METABOLITE, RELYING MORE ON C-OXIDATION PATHS THAN THE HAMSTER WHICH EXCRETED LARGE AMT OF PHENOTHIAZINE N-GLUCURONIDE. |
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| Toxicity/Toxicokinetics |
Interactions
PREVIOUS DRENCHING WITH CARBON TETRACHLORIDE MAY ALSO SERVE TO INCR ITS TOXICITY. ANTIOXIDANTS, EG PHENOTHIAZINE, INHIBITED THE MUTAGENICITY OF BENZO(A)PYRENE & SOME OF ITS DERIVATIVES TOWARDS SALMONELLA TYPHIMURIUM STRAIN TA98; THIS INHIBITION WAS CONCN DEPENDENT. Non-Human Toxicity Values LD50 Rat oral 5000 mg/kg. |
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| References | |||
| Additional Infomation |
Phenothiazine is a light green to steel-blue powder. Acquires a greenish-brown tint under exposure to sunlight. (NTP, 1992)
10H-phenothiazine is the 10H-tautomer of phenothiazine. It has a role as a plant metabolite, a radical scavenger and a ferroptosis inhibitor. It is a tautomer of a 4aH-phenothiazine, a 1H-phenothiazine and a 3H-phenothiazine. Phenothiazine (PTZ) is an organic thiazine compound. Phenothiazine has been reported in Mimosa pudica with data available. Phenothiazine 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. In addition, these agents have peripherally or centrally antagonistic activity against alpha adrenergic, serotonergic, histaminic, and muscarinic receptors. (NCI) See also: Promethazine (has subclass); Chlorpromazine (has subclass); Trifluoperazine (has subclass) ... View More ... Therapeutic Uses Antibiotics, Macrolide; Antiprotozoal Agents AT ONE TIME EMPLOYED IN HUMAN MEDICINE AS ANTHELMINTIC & URINARY ANTISEPTIC. MEDICATION (VET): ...EMPLOYED IN...VET MEDICINE FOR PINWORM, THREADWORM & ROUNDWORM INFESTATIONS. IT HAS ALSO BEEN USED AS URINARY ANTISEPTIC... MEDICATION (VET): IT IS STILL OF VALUE FOR TREATMENT OF HELMINTHIASIS IN SHEEP & OTHER DOMESTIC ANIMALS. For more Therapeutic Uses (Complete) data for PHENOTHIAZINE (8 total), please visit the HSDB record page. Drug Warnings VET: ...ANIMALS.../HAVE/ DIED AFTER RECEIVING...THERAPEUTIC DOSE, WHEREAS OTHERS HAVE SURVIVED MANY TIMES THIS AMT. ...VARIATION IN TOXICITY...ADEQUACY OR OTHERWISE OF DIET, & PARTICULARLY ITS PROTEIN CONTENT, IS IMPORTANT FACTOR. DEHYDRATION IS ANOTHER, MORTALITY IN LAMBS BEING HIGHEST UNDER DROUGHT CONDITIONS. SUSCEPTIBILITY TO TOXIC EFFECTS...CONSIDERED...GREATEST IN HORSE, LESS SO IN DOG & PIG, WHILE RUMINANTS & BIRDS APPEAR...RESISTANT. ...TOXIC EFFECTS... MORE FREQUENTLY IN CATTLE THAN IN SHEEP & GOATS. YOUNG & DEBILITATED ANIMALS...MORE SUSCEPTIBLE... DIGESTIVE DISTURBANCES...PROMOTE ABSORPTION... Use of the drug in weak animals, particularly those that are anemic and emaciated, is strictly contraindicated. Animals known to be constipated should not be treated with phenothiazine, since retention of the drug in the digestive tract and resulting absorption of greater than normal quantities is likely to lead to drug poisoning. Use of phenothiazine in pregnancy is contraindicated only during the last month of gestation. |
| Molecular Formula |
C12H9NS
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| Molecular Weight |
199.27
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| Exact Mass |
199.045
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| Elemental Analysis |
C, 72.33; H, 4.55; N, 7.03; S, 16.09
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| CAS # |
92-84-2
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| Related CAS # |
Phenothiazine-d8; 1219803-41-4
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| PubChem CID |
7108
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| Appearance |
Off-white to light green solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
371.0±12.0 °C at 760 mmHg
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| Melting Point |
184 °C
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| Flash Point |
178.2±19.6 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
4.15
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
187
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2C(=CC=CC=2)NC2C1=CC=CC=2
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| InChi Key |
WJFKNYWRSNBZNX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H9NS/c1-3-7-11-9(5-1)13-10-6-2-4-8-12(10)14-11/h1-8,13H
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| Chemical Name |
10H-phenothiazine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0183 mL | 25.0916 mL | 50.1832 mL | |
| 5 mM | 1.0037 mL | 5.0183 mL | 10.0366 mL | |
| 10 mM | 0.5018 mL | 2.5092 mL | 5.0183 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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