Diphenmanil (methylsulfate)

Modify Date: 2024-01-02 15:03:32

Diphenmanil (methylsulfate) Structure
Diphenmanil (methylsulfate) structure
 Common Name Diphenmanil (methylsulfate)
CAS Number 62-97-5 Molecular Weight 389.50800
Density N/A Boiling Point N/A
Molecular Formula C21H27NO4S Melting Point 194-195ºC
MSDS N/A Flash Point N/A

 Use of Diphenmanil (methylsulfate)


Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.IC50 value: Target: mAChRDiphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. M3 receptors are located in the smooth muscles of the blood vessels, as well as in the lungs. This means they cause vasodilation and bronchoconstriction. They are also in the smooth muscles of the gastrointestinal tract (GIT), which help in increasing intestinal motility and dilating sphincters. The M3 receptors are also located in many glands which help to stimulate secretion in salivary glands and other glands of the body.

 Names

Name diphemanil methylsulfate
Synonym More Synonyms

 Diphenmanil (methylsulfate) Biological Activity

Description Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.IC50 value: Target: mAChRDiphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. M3 receptors are located in the smooth muscles of the blood vessels, as well as in the lungs. This means they cause vasodilation and bronchoconstriction. They are also in the smooth muscles of the gastrointestinal tract (GIT), which help in increasing intestinal motility and dilating sphincters. The M3 receptors are also located in many glands which help to stimulate secretion in salivary glands and other glands of the body.
Related Catalog
References

[1]. Küng M, Diamond L. Effect of inhaled diphemanil methylsulfate, a parasympatholytic agent, on histamine induced bronchoconstriction in asymptomatic asthmatics. Ann Allergy. 1984 Jan;52(1):22-5.

[2]. Vidal AM, Rey E, Pons G et al. Pharmacokinetics of diphemanil methylsulphate in healthy subjects. Eur J Clin Pharmacol. 1992;42(6):689-91.

[3]. Vidal AM, Chéron G, Rey E et al. Pharmacokinetics of diphemanil methylsulphate in infants. Eur J Clin Pharmacol. 1993;45(1):89-91.

[4]. Chéron G, Vidal AM, Rey E et al. [Pharmacokinetics of diphemanil methylsulfate in infants]. Arch Pediatr. 1994 Jan;1(1):33-7.

[5]. Adamantidis M, Dumotier B, Caron J, Dupuis B. [Electrophysiologic effects and arrhythmogenic potential of diphemanil methylsulfate on rabbit purkinje fibers. Correlations with clinical observations of QT prolongation in pediatrics]. Arch Mal Coeur Vaiss.

 Chemical & Physical Properties

Melting Point 194-195ºC
Molecular Formula C21H27NO4S
Molecular Weight 389.50800
Exact Mass 389.16600
PSA 74.81000
LogP 4.49130

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TN5075000
CHEMICAL NAME :
Piperidinium, 4-(diphenylmethylene)-1,1-dimethyl-, methyl sulfate
CAS REGISTRY NUMBER :
62-97-5
LAST UPDATED :
199203
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C20-H24-N.C-H3-O4-S
MOLECULAR WEIGHT :
389.55
WISWESSER LINE NOTATION :
T6K DYTJ A1 A1 DUYR&R &WSO&O1

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 :
1107 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,576,1951
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 23,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
317 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,576,1951
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
47 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,576,1951
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
4012 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 103,100,1955
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
42 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - other changes
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,576,1951
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
404 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,576,1951

 Synonyms

Talpran
Diphenmethanil
Nivelona
Demotil
DIPHEMANIL METHYLSULFATE
Diphemanil Methylsulfate
Variton
Diphemanil metilsulfate
Diphenmanil (methylsulfate)
Diphemanil
4-benzhydrylidene-1,1-dimethyl-piperidinium,methyl sulfate
4-Benzhydryliden-1,1-dimethyl-piperidinium,Methylsulfat
4-benzhydrylidene-1,1-dimethylpiperidin-1-ium,methyl sulfate
Prantal
Nivelon
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