8274. Roxatidine Acetate

Nomenclature

CAS number: 78628-28-1
2-(Acetyloxy)-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]acetamide; aceroxatidine.
C19H28N2O4; mol wt 348.44.
C 65.49%, H 8.10%, N 8.04%, O 18.37%.

Description and references

Histamine H2-receptor antagonist. Prepn and anti-ulcerative activity: K. Shibata et al., EP 24510; eidem, US 4293557 (both 1981 to Teikoku Hormone). Pharmacology in animals: M. Tarutani et al., Arzneim.-Forsch. 35, 703 (1985). Comparison with cimetidine of effect on gastric acid secretion and ulcer formation in animals: eidem, ibid. 844. Metabolism in humans: S. Honma et al., Oyo Yakuri 30, 555 (1985); C.A. 104, 61453n (1985).

Chemical structure

Properties

mp 59-60°. LD50 orally in male mice: 1000 mg/kg (Shibata).

Derivative

Hydrochloride.

Nomenclature

CAS number: 93793-83-0
Pifatidine; HOE-760; TZU-0460; Altat (Teikoku Hormone); Gastralgin (De Angeli); Neo H2 (Boehringer, Ing.); Roxit (Aventis).
C19H28N2O4.HCl; mol wt 384.90.
C 59.29%, H 7.59%, N 7.28%, O 16.63%, Cl 9.21%.

Properties

mp 145-146°.

Therapeutic Category

Antiulcerative.

Keywords

Antiulcerative; Histamine H2-Receptor Antagonist