Metiamide

Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.IC50 Value: 0.92 uM (Ki with glycolaldehyde as the varied substrate for E3)Target: H2 receptorMetiamide is an intermediate compound in the development of the successful anti-ulcer drug cimetidine. in vitro: Metiamide is a competitive with aldehyde substrates and noncompetitive with the Human E3 Aldehyde Dehydrogenase coenzyme, binding to both the free E3 isozyme and the enzyme·coenzyme binary complex withK i values of 0.92 μM glycolaldehyde as the varied substrate[1]. Data was got as percentage change in GTPase activity induced by metiamide compared with the GTPase activity stimulated by HA (100 μM)[2]. in vivo: Metiamide is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. Metiamide inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Metiamide include an increase in gastric bacterial flora such as nitrate-reducing organisms.

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

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Endocrinology

[1]. Alexandra Kikonyogo ,Regina Pietruszko, Cimetidine and Other H2-Receptor Antagonists as Inhibitors of Human E3 Aldehyde Dehydrogenase. Molecular Pharmacology 1997; 52: 2267-271.

[2]. Hendrik Preuss, Prasanta Ghorai1, Anja Kraus, Constitutive Activity and Ligand Selectivity of Human, Guinea Pig, Rat, and Canine Histamine H2 Receptors. JPET 2007 vol. 321no. 3 983-995.

Loratadine | Histamine | Pitolisant hydrochloride | Cimetidine | Osthole | Clemastine fumarate | Ebrotidine | JNJ-7777120 | Famotidine | Cetirizine Dihydrochloride | Desloratadine | Ketotifen fumarate | Lodoxamide | Meclizine dihydrochloride | Chlorpheniramine maleate

MOLECULAR FORMULA :

C9-H16-N4-S2

MOLECULAR WEIGHT :

244.41

WISWESSER LINE NOTATION :

T5M CNJ D1S2MYUS&M1 E1

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 :

1493 mg/kg

TOXIC EFFECTS :

Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

142 mg/kg

TOXIC EFFECTS :

Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

2642 mg/kg

TOXIC EFFECTS :

Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

130 mg/kg

TOXIC EFFECTS :

Behavioral - antipsychotic Lungs, Thorax, or Respiration - respiratory depression

MUTATION DATA

TYPE OF TEST :

DNA inhibition

TEST SYSTEM :

Human Cells - not otherwise specified

DOSE/DURATION :

1 umol/L

REFERENCE :

JIDEAE Journal of Investigative Dermatology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1938- Volume(issue)/page/year: 65,400,1975