ICI 162,846

Names

[ Name ]:
ICI 162,846

[Synonym ]:
Tocris-0833

Biological Activity

[Description]:

ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

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

[Target]

H2 Receptor

[References]

[1]. Wilson JA, et al. Inhibition of human gastric secretion by ICI 162,846--a new histamine H2-receptor antagonist. Br J Clin Pharmacol. 1986 Jun;21(6):685-9.

[2]. Gompertz RH, et al. Acid blockade by omeprazole or ICI 162846 in a chronic duodenal ulcer model. Agents Actions. 1991 May;33(1-2):161-3.

Chemical & Physical Properties

[ Density]:
1.45g/cm3

[ Boiling Point ]:
500.4ºC at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₇F₃N₆O

[ Molecular Weight ]:
306.29

[ Flash Point ]:
256.5ºC

[ Exact Mass ]:
306.14200

[ PSA ]:
108.82000

[ LogP ]:
2.30120

[ Index of Refraction ]:
1.563

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ7889000

CHEMICAL NAME :: 1H-Pyrazole-1-pentanamide, 3-((imino((2,2,2-trifluoroethyl)amino)methyl)amino)-

CAS REGISTRY NUMBER :: 84545-30-2

LAST UPDATED :: 199507

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C11-H17-F3-N6-O

MOLECULAR WEIGHT :: 306.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 365 gm/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Gastrointestinal - tumors

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 15,366,1987