Benztropine Mesylate

Modify Date: 2024-01-02 21:23:44

Benztropine Mesylate Structure
Benztropine Mesylate structure
 Common Name Benztropine Mesylate
CAS Number 132-17-2 Molecular Weight 403.535
Density N/A Boiling Point 547.8ºC at 760 mmHg
Molecular Formula C22H29NO4S Melting Point 135 °C(lit.)
MSDS Chinese USA Flash Point 285.1ºC
Symbol GHS06
GHS06		 Signal Word Danger

 Use of Benztropine Mesylate


Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease.Target: mAChRBenzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics. Symptoms of Parkinson's disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor [1, 2].Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). BZT analogues also exhibit varied binding affinities for muscarinic M(1) and histamine H(1) receptors. The BZT analogues showed a wide range of histamine H(1) receptor (K(i)=16-37,600 nM) and DAT (K(i)=8.5-6370 nM) binding affinities [3].

 Names

Name benzatropine mesylate
Synonym More Synonyms

 Benztropine Mesylate Biological Activity

Description Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease.Target: mAChRBenzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics. Symptoms of Parkinson's disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor [1, 2].Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). BZT analogues also exhibit varied binding affinities for muscarinic M(1) and histamine H(1) receptors. The BZT analogues showed a wide range of histamine H(1) receptor (K(i)=16-37,600 nM) and DAT (K(i)=8.5-6370 nM) binding affinities [3].
Related Catalog
References

[1]. Wszola, B.A., K.M. Newell, and R.L. Sprague, Risk factors for tardive dyskinesia in a large population of youths and adults. Exp Clin Psychopharmacol, 2001. 9(3): p. 285-96.

[2]. van Harten, P.N., et al., Intermittent neuroleptic treatment and risk for tardive dyskinesia: Curacao Extrapyramidal Syndromes Study III. Am J Psychiatry, 1998. 155(4): p. 565-7.

[3]. Kulkarni, S.S., et al., Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem, 2006. 14(11): p. 3625-34.

 Chemical & Physical Properties

Boiling Point 547.8ºC at 760 mmHg
Melting Point 135 °C(lit.)
Molecular Formula C22H29NO4S
Molecular Weight 403.535
Flash Point 285.1ºC
Exact Mass 403.181732
PSA 75.22000
LogP 4.94050
Vapour Pressure 7.83E-13mmHg at 25°C
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YM3150000
CHEMICAL NAME :
1-alpha-H,5-alpha-H-Tropane, 3-alpha-(diphenylmethoxy)-, methanesulfonate
CAS REGISTRY NUMBER :
132-17-2
LAST UPDATED :
199504
DATA ITEMS CITED :
11
MOLECULAR FORMULA :
C21-H25-N-O.C-H4-O3-S
MOLECULAR WEIGHT :
403.58
WISWESSER LINE NOTATION :
T56 A ANTJ A1 GOYR&R &OSW1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
100 ug/kg
TOXIC EFFECTS :
Behavioral - toxic psychosis
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
65 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
940 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 :
353 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 :
91 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 - mouse
DOSE/DURATION :
103 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 :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
24 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 - cat
DOSE/DURATION :
33 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
80 mg/kg
TOXIC EFFECTS :
Autonomic Nervous System - parasympatholytic

MUTATION DATA

TYPE OF TEST :
DNA adduct
TEST SYSTEM :
Bacteria - Escherichia coli
DOSE/DURATION :
10 umol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 89,95,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5595 No. of Facilities: 46 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1071 (estimated) No. of Female Employees: 681 (estimated)

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301 + H311 + H331
Precautionary Statements Missing Phrase - N15.00950417-P261-P280-P302 + P352 + P312-P304 + P340 + P312-P403 + P233
Hazard Codes T: Toxic;
Risk Phrases R23/24/25
Safety Phrases S36/37/39-S45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS YM3150000
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles1

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 Synonyms

3a-(Diphenylmethoxy)-1aH,5aH-tropane Methanesulfonate
(3-endo)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane methanesulfonate
3-(Benzhydryloxy)-8-methyl-8-azabicyclo[3.2.1]octane methanesulfonate
MFCD00074784
Benztropine methanesulfonate
Benzotropine Mesylate
EINECS 205-048-8
Cobrentin methanesulfonate
BENZTROPINE MESYLATE
Methansulfonsäure--(3-endo)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octan(1:1)
8-Azabicyclo[3.2.1]octane, 3-(diphenylmethoxy)-8-methyl-, (3-endo), methanesulfonate (1:1)
Tropine benzohydryl ether methanesulfonate
endo-3-(Diphenylmethoxy)-8-methyl-8-azoniabicyclo(3.2.1)octane methanesulphonate
(3-endo)-3-(Diphenylmethoxy)-8-methyl-8-azoniabicyclo[3.2.1]octane methanesulfonate
Cogentin
8-Azabicyclo[3.2.1]octane (3-(diphenylmethoxy)-8-methyl
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Chemsrc provides Benztropine Mesylate(CAS#:132-17-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Benztropine Mesylate are included as well.>> amp version: Benztropine Mesylate

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