Homatropine

Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent[1].

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs, and produces a dose ratio of only 95.0 when combined with Hexamethonium Bromide (HY-B0569) in atrium from guinea-pigs[1]. Homatropine has affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses[2].

Homatropine methylbromide (9 mm x 5 mm conical suppository) causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure in rats[3]. Animal Model: Male albino rats[3] Dosage: 9 mm x 5 mm conical suppository Administration: By suppository Result: Blocked cardiovascular responses to vagal stimulation and acetylcholine; 10-20 min after insertion of the suppository the effects of vagal stimulation over a range of 2-16 Hz, 5 V, on pulse rate was virtually abolished and remained unchanged at 45-60 min.

DATA ITEMS CITED :

5

MOLECULAR FORMULA :

C16-H21-N-O3

MOLECULAR WEIGHT :

275.38

WISWESSER LINE NOTATION :

T56 A ANTJ A1 GOVYQR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

180 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,156,1959

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1307 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

370 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1800 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84350 No. of Facilities: 170 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 2582 (estimated)