Mebhydrolin napadisylate

Names

[ Name ]:
Mebhydrolin napadisylate

[Synonym ]:
Mebhydroline 1,5-naphthalenedisulfonate salt
diazoline
Naphthalene-1,5-disulfonic acid - 5-benzyl-2-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (1:2)
1,5-Naphthalenedisulfonic acid - 5-benzyl-2-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (1:2)
1,5-Naphthalenedisulfonic acid, compd. with 2,3,4,5-tetrahydro-2-methyl-5-(phenylmethyl)-1H-pyrido[4,3-b]indole (1:2)
Mebhydrolin napadisylate
Mebhydroline Napadisylate

Biological Activity

[Description]:

Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

[Target]

Histamine H1-receptor[1]

[In Vitro]

Mebhydrolin is a specific histamine H1-receptor antagonist with minimal sedative properties and comparing it with the effects of chlorpromazine, the archetypical phenothiazine[1]. Mebhydrolin exerts an antihistaminic effect over the period of the ethanol interaction study[2].

[References]

[1]. O'Neill PA, et al. Chlorpromazine-a specific effect on breathlessness? Br J Clin Pharmacol. 1985 Jun;19(6):793-7.

[2]. Franks HM, et al. Interaction between ethanol and antihistamines: 3. Mebhydrolin. Med J Aust. 1981 Oct 31;2(9):477-9.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
0.9799 (rough estimate)

[ Boiling Point ]:
457.3ºC at 760 mmHg

[ Melting Point ]:
280°C (rough estimate)

[ Molecular Formula ]:
C₄₈H₄₈N₄O₆S₂

[ Molecular Weight ]:
841.048

[ Flash Point ]:
230.4ºC

[ Exact Mass ]:
840.301514

[ PSA ]:
141.84000

[ LogP ]:
10.72560

[ Index of Refraction ]:
1.8676 (estimate)

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ6845000

CAS REGISTRY NUMBER :: 6153-33-9

LAST UPDATED :: 198706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H20-N2.1/2C10-H8-O6-S2

MOLECULAR WEIGHT :: 420.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 300 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: 6,850,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 470 mg/kg

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

REFERENCE :: PHTXA6 Pharmacology and Toxicology. English translation of FATOAO. (New York, NY) V.20-22, 1957-59. Discontinued. Volume(issue)/page/year: 20,539,1957

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 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: 6,850,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 40 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: 6,850,1982

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
QJ6845000

[ 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%

Articles

Three explorative studies on the efficacy of the antihistamine mebhydroline (Omeril).

Int. J. Clin. Pharmacol. Ther. 33 , 373, (1995)

The efficacy of a multiple oral dose treatment with mebhydroline (Omeril coated tablets, 100 mg t.i.d.) was examined in 3 studies which were performed in a randomized, double-blind and placebo-control...

Metabolic factors and risk of hepatocellular carcinoma by chronic hepatitis B/C infection: a follow-up study in Taiwan.

Gastroenterology 135(1) , 111-21, (2008)

This study investigated whether obesity, diabetes, and other metabolic factors are independently associated with hepatocellular carcinoma (HCC), stratified by hepatitis B virus (HBV) and hepatitis C v...

[Agranulocytosis associated with mebhydrolin napadisylate (Incidal)].

Harefuah 106(5) , 208-9, (1984)