7438. Pinacidil

Nomenclature

CAS number: 60560-33-0
N-Cyano-N′-4-pyridinyl-N″-(1,2,2-trimethylpropyl)guanidine; P-1134.
C13H19N5; mol wt 245.32.
C 63.65%, H 7.81%, N 28.55%.

Description and 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).

Chemical structure

Derivative

Monohydrate.

Nomenclature

CAS number: 85371-64-8
Pindac (Leo Pharm).
C13H19N5.H2O; mol wt 263.34.
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).

Therapeutic Category

Antihypertensive.

Keywords

Antihypertensive; Guanidine Derivatives; Potassium Channel Activator/Opener