CAS 1229-35-2|Methdilazine Hydrochloride

Introduction：Basic information about CAS 1229-35-2|Methdilazine Hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Methdilazine Hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
MUTATION DATA
5. Safety Information
6. Customs
7. Synonyms

Common Name	Methdilazine Hydrochloride
CAS Number	1229-35-2	Molecular Weight	332.89100
Density	/	Boiling Point	430.4ºC at 760mmHg
Molecular Formula	C₁₈H₂₁ClN₂S	Melting Point	187.5-189ºC
MSDS	/	Flash Point	214.1ºC

Names

Name	10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine,hydrochloride
Synonym	More Synonyms

Methdilazine Hydrochloride BiologicalActivity

Description	Methdilazine hydrochloride is an orally active antibiotic (histamine antagonist). Methdilazine hydrochloride 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
In Vitro	Methdilazine hydrochloride (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: 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 hydrochloride (Intraperitoneal injection, 10 μg/gm body wt/day, 6 weeks) is antagonistic to mycobacteria in H37Rv infected mice[1]. Methdilazine hydrochloride (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

Boiling Point	430.4ºC at 760mmHg
Melting Point	187.5-189ºC
Molecular Formula	C₁₈H₂₁ClN₂S
Molecular Weight	332.89100
Flash Point	214.1ºC
Exact Mass	332.11100
PSA	31.78000
LogP	5.04590
Vapour Pressure	1.3E-07mmHg at 25°C
Index of Refraction	1.642
InChIKey	IEISBKIVLDXSMZ-UHFFFAOYSA-N
SMILES	CN1CCC(CN2c3ccccc3Sc3ccccc32)C1.Cl

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP3150000

CHEMICAL NAME :: Phenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 1229-35-2

LAST UPDATED :: 199510

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C18-H20-N2-S.Cl-H

MOLECULAR WEIGHT :: 332.92

WISWESSER LINE NOTATION :: T C666 BN ISJ B1- CT5NTJ A1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 260 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 75 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22 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 :: 190 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9880 mg/kg/52W-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 150 mg/kg

SEX/DURATION :: female 2-4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

MUTATION DATA

TYPE OF TEST :: Morphological transformation

TEST SYSTEM :: Rodent - hamster Embryo

DOSE/DURATION :: 10 mg/L

REFERENCE :: ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 8(Suppl 6),4,1986

Safety Information

RIDADR	NONH for all modes of transport
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

MJ 5022

Bristaline

Methdilazine monohydrochloride

Methdilazine Hcl

10-(1-methyl-pyrrolidin-3-ylmethyl)-10H-phenothiazine,monohydrochloride

Tacaryl hydrochloride

Disyncran

Dilosyn

Methdilazine hydrochloride

METHDILAZINE HYDROCHLORIDE

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