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1229-35-2

1229-35-2 structure
1229-35-2 structure
  • Name: Methdilazine Hydrochloride
  • Chemical Name: 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine,hydrochloride
  • CAS Number: 1229-35-2
  • Molecular Formula: C18H21ClN2S
  • Molecular Weight: 332.89100
  • Catalog: Signaling Pathways Anti-infection Bacterial
  • Create Date: 2018-04-09 08:00:00
  • Modify Date: 2024-01-27 21:45:48
  • 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].
Name 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine,hydrochloride
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
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
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.

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

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
RIDADR NONH for all modes of transport
HS Code 2934300000
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%

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