CAS 135-23-9|Methapyrilene Hydrochloride
Introduction：Basic information about CAS 135-23-9|Methapyrilene Hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Methapyrilene Hydrochloride | ||
|---|---|---|---|
| CAS Number | 135-23-9 | Molecular Weight | 297.84700 |
| Density | 1.148g/cm3 | Boiling Point | 389.6ºC at 760 mmHg |
| Molecular Formula | C14H20ClN3S | Melting Point | 162° |
| MSDS | ChineseUSA | Flash Point | 189.4ºC |
| Symbol | GHS06 | Signal Word | Danger |
Names
| Name | methapyrilene hydrochloride |
|---|---|
| Synonym | More Synonyms |
Methapyrilene Hydrochloride BiologicalActivity
| Description | Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo[2] |
|---|---|
| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
| Target | H1 Receptor |
| In Vitro | Methapyrilene hydrochloride (650 μM) results in a down-regulation of TF and up-regulation of FTL, while the level of HMOX1 is not changed. Additionally, the levels of CD44 and SOX9 proteins and the expression of PROM1 (CD133), hepatic stem cell-associated markers are increased[1]. Methapyrilene hydrochloride (650 μM) decreases CYP2E1, CYP3A4, NR1l3, ALB, mRNA expression and increases CD133 expression[1]. |
| In Vivo | Methapyrilene hydrochloride (oral gavage; 40 or 80 mg/kg; 5 days per week; 6 weeks) results in changes in the expression of classic hepatotoxicity-related marker genes and iron homeostasis-related genes, especially a prominent, dose-dependent down-regulation of the transferrin (Tf) gene and an up-regulation of the ferritin, light chain (FTL) gene in rats[1]. Methapyrilene hydrochloride (oral gavage; 150 mg/kg; 3 days) causes periportal liver necrosis at high dosage. Methapyrilene is sufficient to induce liver necrosis, or a subtoxic dose of 50 mg/kg/day[2]. |
| References | [1]. Iryna Kindrat, et al.Effect of methapyrilene hydrochloride on hepatic intracellular iron metabolism in vivo and in vitro. Toxicol Lett. 2017 Nov 5;281:65-73. [2]. Andrew Craig, et al. Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat. J Proteome Res. 2006 Jul;5(7):1586-601. [3]. Shawkat-Muhialdin Jangi, et al. H1 histamine receptor antagonists induce genotoxic and caspase-2-dependent apoptosis in human melanoma cells. Carcinogenesis. 2006 Sep;27(9):1787-96. |
Chemical & Physical Properties
| Density | 1.148g/cm3 |
|---|---|
| Boiling Point | 389.6ºC at 760 mmHg |
| Melting Point | 162° |
| Molecular Formula | C14H20ClN3S |
| Molecular Weight | 297.84700 |
| Flash Point | 189.4ºC |
| Exact Mass | 297.10700 |
| PSA | 47.61000 |
| LogP | 3.51330 |
| Vapour Pressure | 2.82E-06mmHg at 25°C |
| InChIKey | BONORRGKLJBGRV-UHFFFAOYSA-N |
| SMILES | CN(C)CCN(Cc1cccs1)c1ccccn1.Cl |
| Storage condition | room temp |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 429 ug/kg
- TOXIC EFFECTS :
- Gastrointestinal - gastritis
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 200 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 150 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 182 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 90 mg/kg
- TOXIC EFFECTS :
- Behavioral - excitement Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 75 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 17500 ug/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 14600 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 9100 mg/kg/26W-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 18200 mg/kg/26W-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 22 gm/kg/64W-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 9625 mg/kg/2Y-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 4813 mg/kg/2Y-C
- TOXIC EFFECTS :
- Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 10080 mg/kg/24W-C
- TOXIC EFFECTS :
- Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
- TYPE OF TEST :
- Morphological transformation
- TYPE OF TEST :
- Unscheduled DNA synthesis
MUTATION DATA - TYPE OF TEST :
- Cytogenetic analysis
- TEST SYSTEM :
- Rodent - hamster Lung
- DOSE/DURATION :
- 2 mmol/L
- REFERENCE :
- MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 341,77,1994 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80458 No. of Facilities: 197 (estimated) No. of Industries: 5 No. of Occupations: 12 No. of Employees: 4170 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80458 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1698 (estimated) No. of Female Employees: 1135 (estimated)
- TYPE OF TEST :
- Cytogenetic analysis
- TEST SYSTEM :
- Rodent - hamster Lung
- DOSE/DURATION :
- 2 mmol/L
- REFERENCE :
- MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 341,77,1994 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80458 No. of Facilities: 197 (estimated) No. of Industries: 5 No. of Occupations: 12 No. of Employees: 4170 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80458 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1698 (estimated) No. of Female Employees: 1135 (estimated)
Safety Information
| Symbol | GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
| Hazard Codes | T |
| Risk Phrases | R25 |
| Safety Phrases | S22;S36;S45 |
| RIDADR | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | UT1750000 |
| Packaging Group | III |
| Hazard Class | 6.1(b) |
Synonyms
| N,N-dimethyl-N'-pyridin-2-yl-N'-(thiophen-2-ylmethyl)ethane-1,2-diamine,hydrochloride |
| Methoxylene |
| EINECS 205-184-8 |
| Methacon |
| Lullamin |
| Histadyl |
| Somnicaps |
| Barhist |
| Coryzol |
| Capathyn |
| MFCD00050665 |
| METHAPYRILENE HYDROCHLORIDE |
| Methapyrilene HCl |
