7491. Pirenzepine

Nomenclature

CAS number: 28797-61-7
5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one; LS-519.
C19H21N5O2; mol wt 351.40.
C 64.94%, H 6.02%, N 19.93%, O 9.11%.

Description and references

Tricyclic gastric-acid inhibitor. Prepn: FR 1505795 (1967 to Thomae), C.A. 70, 4154w (1969). Pharmacology: W. Eberlein et al., Arzneim.-Forsch. 27, 356 (1977). Pharmacokinetics: R. Hammes et al., ibid. 928. Mechanism of action: G. Heller et al., Verh. Dtsch. Ges. Inn. Med. 84, 991 (1978), C.A. 90, 132984s (1979). Human pharmacology: H. Brunner et al., Arzneim.-Forsch. 27, 684 (1977). Multicenter controlled clinical trial: Scand. J. Gastroenterol. 17, Suppl. 81, 1-42 (1982). Radioimmunoassay determn in human plasma and urine: C. A. Homon et al., Ther. Drug Monit. 9, 236 (1987). Symposium: ibid. Suppl. 72, 1-273. Review of pharmacology and therapeutic efficacy: A. A. Carmine, R. N. Brogden, Drugs 30, 85-126 (1985). Comprehensive description: H. A. El-Obeid et al., Anal. Profiles Drug Subs. 16, 445-506 (1987).

Chemical structure

Derivative

Dihydrochloride.

Nomenclature

CAS number: 29868-97-1
LS-519-Cl2; Duogastral (ISM); Durapirenz (Durachemie); Gasteril (Ripari-Gero); Gastrozepin (Thomae); Leblon (De Angeli); Maghen (Savio); Renzepin (Bergamon); Tabe (Bernabo); Ulcuforton (Plantorgan); Ulcosan (Dompé).
C19H21N5O2.2HCl; mol wt 424.32.
C 53.78%, H 5.46%, N 16.50%, O 7.54%, Cl 16.71%.

Properties

Sol in water, slightly sol in methanol. Practically insol in ether.

Therapeutic Category

Antiulcerative.

Keywords

Antiulcerative