Endovalpin

Names

[ CAS No. ]:
80-50-2

[ Name ]:
Endovalpin

[Synonym ]:
octatropine methylbromide
Methoxy(benzene-2,4,6-d3)
Anisole-2,4,6-d3
1,3,5-trideuterio-2-methoxy-benzene
CHOLINE IODIDE 1-HYDROXY-α-PHENYLCYCLOPENTANEACETATE
2,4,6-Trideutero-anisol
anisotropine methobromide
2,4,6-Trideuterio-anisol
anisotropine methyl bromide
2,4,6-trideuterioanisole

Biological Activity

[Description]:

Anisotropine methobromide is an orally active anticholinergic muscarinic antagonist. Anisotropine methobromide can inhibit gastric acid secretion and is used as an adjunct to peptic ulcers[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Metabolic Disease

[In Vivo]

Anisotropine methobromide (intravenous injection, 0.5 μM and 0.1 mL, once) can block acetylcholine-induced vocalization, intestinal spasm and intestinal contractions in conscious or anesthetized dogs[1]. Animal Model: Dogs weighing 2.5 to 5.0 kg[1] Dosage: 0.5 μM, 0.1 mL Administration: Intravenous injection; once Result: Inhibited the acetylcholine-induced vocalization with maximum inhibition of 85.1% and the acetylcholine-induced intestinal spasm with maximum inhibition of 79%.

[References]

[1]. K Nakayama, et al. Effects of anisotropine methylbromide (Valpin) and its mixture with sulpyrine on vocalization response and spasm of intestine induced by acetylcholine in dogs. Jpn J Pharmacol. 1972 Apr;22(2):215-20.

Chemical & Physical Properties

[ Melting Point ]:
329ºC

[ Molecular Formula ]:
C₂₇H₄₃NO₉

[ Molecular Weight ]:
525.63200

[ Exact Mass ]:
525.29400

[ PSA ]:
174.31000

[ Storage condition ]:
2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YM3710000

CHEMICAL NAME :: 1-alpha-H,5-alpha-H-Tropanium, 3-alpha-hydroxy-8-methyl-, bromide, 2-propylvalerate

CAS REGISTRY NUMBER :: 80-50-2

LAST UPDATED :: 199504

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C17-H32-N-O2.Br

MOLECULAR WEIGHT :: 362.41

WISWESSER LINE NOTATION :: T56 A AKTJ A1 A1 GOVY3&3 &E

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 :: 705 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,24,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 850 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,24,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 129 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,24,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 133 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,24,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6300 ug/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,70,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M2759 No. of Facilities: 10 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 197 (estimated) No. of Female Employees: 59 (estimated)

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H312-H332-H400

[ Precautionary Statements ]:
P273-P280

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn: Harmful;N: Dangerous for the environment;

[ Risk Phrases ]:
R20/21/22

[ Safety Phrases ]:
36-61-60

[ RIDADR ]:
UN 3077 9/PG 3

[ WGK Germany ]:
3

[ RTECS ]:
YM3710000

Articles

[Pediatric use of a drug, anticholinergic and muscle relaxant on the gastrointestinal tract].

Pediatr. Med. Chir. 4(1-2) , 79-81, (1982)

[Effectiveness of octatropine methylbromide (OMB) in the treatment of gastritis, duodenal ulcer and spastic colon--a double blind study].

ZFA (Stuttgart.) 58(27) , 1481-4, (1982)

[Preliminary clinical research on a new anti-ulcer drug].

Clin. Ter. 89(4) , 365-71, (1979)