Title: Guanabenz
CAS Registry Number: 5051-62-7
CAS Name: 2-[(2,6-Dichlorophenyl)methylene]hydrazinecarboximidamide
Additional Names: [(2,6-dichlorobenzylidene)amino]guanidine; N-(2,6-dichlorobenzylidene)-N¢-amidinohydrazine
Manufacturers' Codes: NSC-68982
Molecular Formula: C8H8Cl2N4
Molecular Weight: 231.08
Percent Composition: C 41.58%, H 3.49%, Cl 30.68%, N 24.25%
Literature References: a2-Adrenergic agonist. Prepn: J. Yates, E. Haddock, GB 1019120 (1966 to Shell), C.A. 64, 11132h (1966). Use as antihypertensive: W. J. Houlihan et al., DE 1804634 (1969 to Sandoz), C.A. 71, 89976j (1969). Pharmacology: T. Baum et al., J. Pharmacol. Exp. Ther. 171, 276 (1970); E. Lampa et al., Experientia 36, 228 (1980). Disposition of 14C-guanabenz in humans: R. H. Meacham et al., Clin. Pharmacol. Ther. 27, 44 (1980). Mechanism of action: G. F. DiBona, J. Cardiovasc. Pharmacol. 6, Suppl. 3, S543 (1984). Radioimmunoassay determn in plasma: H. Tatsumi, Arzneim.-Forsch. 34, 1704 (1984). Clinical studies: A. Reppelli et al., Boll. Soc. Ital. Cardiol. 23, 177 (1978); C. V. Ram et al., J. Clin. Pharmacol. 19, 148 (1979). Clinical studies in opiate withdrawal: F. S. Tennant, R. A. Rawson, NIDA Res. Monogr. Ser. 49, 338 (1984); J. T. Murphy, Drug Intell. Clin. Pharm. 19, 32 (1985). Review of pharmacodynamic properties and therapeutic efficacy: B. Holmes et al., Drugs 26, 212-229 (1983). Comprehensive description: C. M. Shearer, Anal. Profiles Drug Subs. 15, 319-336 (1986).
Properties: White solid from acetonitrile, mp 227-229° (dec).
Melting point: mp 227-229° (dec)
Derivative Type: Monoacetate
CAS Registry Number: 23256-50-0
Manufacturers' Codes: Wy-8678
Trademarks: Rexitene (LPD); Tenelid (Helsinn); Wytensin (Wyeth)
Molecular Formula: C10H12Cl2N4O2
Molecular Weight: 291.13
Percent Composition: C 41.26%, H 4.15%, Cl 24.36%, N 19.24%, O 10.99%
Properties: Solid, mp 192.5° (dec). Soly at 25° (mg/ml): water 11; alcohol 50; propylene glycol 100; chloroform 0.6; ethyl acetate 1.
Melting point: mp 192.5° (dec)
Therap-Cat: Antihypertensive.
Keywords: a-Adrenergic Agonist; Antihypertensive; Guanidine Derivatives. |