Title: Rilmenidine
CAS Registry Number: 54187-04-1
CAS Name: N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine
Additional Names: 2-[N-(dicyclopropylmethyl)amino]oxazoline; oxaminozoline
Manufacturers' Codes: S-3341
Molecular Formula: C10H16N2O
Molecular Weight: 180.25
Percent Composition: C 66.63%, H 8.95%, N 15.54%, O 8.88%
Literature References: a2-Adrenoceptor agonist. Prepn: C. Malen et al., DE 2362754; eidem, US 4102890 (1974, 1978 both to Sci. Union et Cie. - Soc. Franc. Recher. Med.). Adrenoceptor binding study: P. Guicheney et al., J. Pharmacol. 12, 255 (1981). Pharmacokinetics in hypertensive subjects: J. Velly et al., ibid. 13, 413 (1982). Animal pharmacology: M. Laubie et al., ibid. 16, 259 (1985); P. A. van Zwieten et al., Arch. Int. Pharmacodyn. 279, 130 (1986). Hypotensive effect in humans: K. Weerasuriya et al., Eur. J. Clin. Pharmacol. 27, 281 (1984). Mechanism of action study: R. E. Gomez et al., Eur. J. Pharmacol. 195, 181 (1991). Review: T. J. Verbeuren et al., Cardiovasc. Drug Rev. 8, 56-70 (1990).
Properties: Crystals from hexane, mp 106-107°.
Melting point: mp 106-107°
Derivative Type: Phosphate
Manufacturers' Codes: S-3341-3
Trademarks: Hyperium (Biopharma)
Molecular Formula: C10H16N2O.H3PO4
Molecular Weight: 278.24
Percent Composition: C 43.17%, H 6.88%, N 10.07%, O 28.75%, P 11.13%
Properties: pKa 9.3. Soly in H2O: ~19% w/v; in methanol: ~7% w/v; in chloroform and ethanol: ~0.7% w/v. LD50 orally in mice, rats: 375, 295 mg/kg (Verbeuren).
pKa: pKa 9.3
Toxicity data: LD50 orally in mice, rats: 375, 295 mg/kg (Verbeuren)
Derivative Type: Fumarate
Molecular Formula: C14H20N2O5
Molecular Weight: 296.32
Percent Composition: C 56.75%, H 6.80%, N 9.45%, O 27.00%
Properties: Crystals from ethanol, mp 170°.
Melting point: mp 170°
Therap-Cat: Antihypertensive.
Keywords: a-Adrenergic Agonist; Antihypertensive. |