CAS 1982-37-2|10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine
Introduction：Basic information about CAS 1982-37-2|10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine | ||
|---|---|---|---|
| CAS Number | 1982-37-2 | Molecular Weight | 296.43000 |
| Density | 1.185 g/cm3 | Boiling Point | 430.4ºC at 760 mmHg |
| Molecular Formula | C18H20N2S | Melting Point | / |
| MSDS | / | Flash Point | 214.1ºC |
Names
| Name | 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine |
|---|---|
| Synonym | More Synonyms |
BiologicalActivity
| Description | Methdilazine is an orally active antibiotic (histamine antagonist). Methdilazine can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases[1][2]. |
|---|---|
| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>InfectionSignaling Pathways >>Anti-infection >>BacterialSignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
| Target | MIC: 5-15 μg/mL (mycobacterium) |
| In Vitro | Methdilazine (0-20 μg/mL approximately, 18 h) inhibits kinds of mycobacterium with MIC values ranging from 5 μg/mL to 15 μg/mL[1]. Cell Proliferation Assay[1] Cell Line: mycobacterium: M. smegmatis 798/1546, M.,fortuitum 1529, M. scrofulaceum 1323, M. gordonae 1324, M. rnarinum 50, M.,flavescens 1541, M. terrae 1450, M. tuberculosis, H37Ra 16, H37Rv 16, K1, K2, ICRC bacillus,'Skinsnes' bacillus. Concentration: 0-20 μg/mL approximately Incubation Time: 18 h Result: Inhibited mycobacterium with MIC values ranging from 5 μg/mL to 15 μg/mL. |
| In Vivo | Methdilazine (Intraperitoneal injection, 10 μg/gm body wt/day, 6 weeks) is antagonistic to mycobacteria in H37Rv infected mice[1]. Methdilazine (Oral administration, 10 mg/kg per day, 28 days) improves survival of Mycobacterium Tuberculosis (Mtb) H37Rv infected mice[2]. Animal Model: H37Rv infected mice[1] Dosage: 10 μg/gm body wt/day, 6 weeks Administration: Intraperitoneal injection Result: Displayed an anti-mycobacterial activity to mycobacteria. Animal Model: Mycobacterium Tuberculosis (Mtb) H37Rv infected Swiss albino male mice[2] Dosage: 10 mg/kg per day for 28 days Administration: Oral administration Result: Increased surviving time to 28 days with no sign of disease, showed 71.42% survival. |
| References | [1]. A N Chakrabarty, et al. Antimycobacterial activity of methdilazine (Md), an antimicrobic phenothiazine. APMIS. 1993 Jun;101(6):449-54. [2]. Noton K Dutta, et al. Activity of the phenothiazine methdilazine alone or in combination with isoniazid or streptomycin against Mycobacterium tuberculosis in mice. J Med Microbiol. 2009 Dec;58(Pt 12):1667-1668. |
Chemical & Physical Properties
| Density | 1.185 g/cm3 |
|---|---|
| Boiling Point | 430.4ºC at 760 mmHg |
| Molecular Formula | C18H20N2S |
| Molecular Weight | 296.43000 |
| Flash Point | 214.1ºC |
| Exact Mass | 296.13500 |
| PSA | 31.78000 |
| LogP | 4.24390 |
| InChIKey | HTMIBDQKFHUPSX-UHFFFAOYSA-N |
| SMILES | CN1CCC(CN2c3ccccc3Sc3ccccc32)C1 |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 4 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - other changes
- REFERENCE :
- 34ZIAG "Toxicology of Drugs and Chemicals," Deichmann, W.B., New York, Academic Press, Inc., 1969 Volume(issue)/page/year: -,379,1969
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 162 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 225 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 183 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 263 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
Safety Information
| HS Code | 2934300000 |
|---|
Customs
| HS Code | 2934300000 |
|---|---|
| Summary | 2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Synonyms
| 10-[(1-methyl-3-pyrrolidinyl)methyl]phenothiazine |
| Tacazyl |
| 10-(1-methyl-pyrrolidin-3-ylmethyl)-phenothiazine |
| 10-(1-Methyl-pyrrolidin-3-ylmethyl)-phenothiazin |
| 10-<1-Methyl-pyrrolidinyl-(3)-methyl>-phenothiazin. |
| methdilazine |
| Methdilazinum |
| Metodilazina |
| Tacryl |
| Methodilazine |
| Methdilazinum [INN-Latin] |
| Disyncram |
| Tacaryl |
| Metodilazina [INN-Spanish] |
| 10-(1-methyl-pyrrolidin-3-ylmethyl)-10H-phenothiazine |
