Title: Pinacidil
CAS Registry Number: 60560-33-0
CAS Name: N-Cyano-N¢-4-pyridinyl-N¢¢-(1,2,2-trimethylpropyl)guanidine
Manufacturers' Codes: P-1134
Molecular Formula: C13H19N5
Molecular Weight: 245.32
Percent Composition: C 63.65%, H 7.81%, N 28.55%
Literature References: Potassium channel opening vasodilator. Prepn: H. J. Petersen, DE 2557438; idem, US 4057636 (1976, 1977 both to Leo Pharm.); H. J. Petersen et al., J. Med. Chem. 21, 773 (1978). Mechanism of action: E. Arrigoni-Martelli et al., Experientia 36, 445 (1980); K. M. Bray et al., Br. J. Pharmacol. 91, 421 (1987). Metabolism: E. Eilertsen et al., Xenobiotica 12, 187 (1982). Bioavailability: eidem, ibid. 177. Determn in plasma: M. Hamilton et al., J. Chromatogr. 375, 359 (1986). Pharmacokinetics and hypotensive effects: J. W. Ward et al., Eur. J. Clin. Pharmacol. 26, 603 (1984). Clinical comparison with hydralazine, q.v.: R. L. Byyny et al., Clin. Pharmacol. Ther. 42, 50 (1987). Review of pharmacology and mechanism of action: M. L. Cohen: Drug Dev. Res. 9, 249-258 (1986).
Derivative Type: Monohydrate
CAS Registry Number: 85371-64-8
Trademarks: Pindac (Leo Pharm)
Molecular Formula: C13H19N5.H2O
Molecular Weight: 263.34
Percent Composition: C 59.29%, H 8.04%, N 26.59%, O 6.08%
Properties: Crystals, mp 164-165°. LD50 in mice, rats (mg/kg): 600, 570 orally (Petersen, 1978).
Melting point: mp 164-165°
Toxicity data: LD50 in mice, rats (mg/kg): 600, 570 orally (Petersen, 1978)
Therap-Cat: Antihypertensive.
Keywords: Antihypertensive; Guanidine Derivatives; Potassium Channel Activator/Opener. |