Title: Amidephrine
CAS Registry Number: 3354-67-4
CAS Name: N-[3-[1-Hydroxy-2-(methylamino)ethyl]phenyl]methanesulfonamide
Additional Names: 3¢-[1-hydroxy-2-(methylamino)ethyl]methanesulfonanilide
Manufacturers' Codes: MJ-1996
Molecular Formula: C10H16N2O3S
Molecular Weight: 244.31
Percent Composition: C 49.16%, H 6.60%, N 11.47%, O 19.65%, S 13.12%
Literature References: a1 Adrenoceptor agonist. Prepn: Larsen, Uloth, FR M3027 (1965 to Mead Johnson), C.A. 62, 13091a (1965); Uloth et al., J. Med. Chem. 9, 88 (1966). Pharmacology of the racemate: Dungan et al., Int. J. Neuropharmacol. 4, 219 (1965); Stanton et al., ibid. 235; of the isomers: Larsen, Lish, Nature 203, 1283 (1964); Buchthal, Jenkinson, Eur. J. Pharmacol. 10, 293 (1970). Toxicology: J. H. Weikel, Jr., K. H. Harper, Toxicol. Appl. Pharmacol. 23, 589 (1972).
Properties: Crystals, mp 159-161°. pKa 9.1.
Melting point: mp 159-161°
pKa: pKa 9.1
Derivative Type: Methanesulfonate
CAS Registry Number: 1421-68-7
Additional Names: Amidephrine mesylate
Manufacturers' Codes: MJ-5190
Trademarks: Fentrinol (Frika)
Molecular Formula: C10H16N2O3S.CH3SO3H
Molecular Weight: 340.42
Percent Composition: C 38.81%, H 5.92%, N 8.23%, O 28.20%, S 18.84%
Properties: Crystals from ethanol, mp 207-209°. LD50 in mice (mg/kg): 2284 orally, 780 i.p., 190 i.v., 1990 s.c.; in male, female Mead Johnson rats (mg/kg): 229, 36 orally; 144, 25 i.p.; in male, female Sprague-Dawley rats (mg/kg): 24, 13 orally; in rabbits (mg/kg): 12 orally, 7.5 intradermally (Weikel, Harper).
Melting point: mp 207-209°
Toxicity data: LD50 in mice (mg/kg): 2284 orally, 780 i.p., 190 i.v., 1990 s.c.; in male, female Mead Johnson rats (mg/kg): 229, 36 orally; 144, 25 i.p.; in male, female Sprague-Dawley rats (mg/kg): 24, 13 orally; in rabbits (mg/kg): 12 orally, 7.5 intradermally (Weikel, Harper)
Therap-Cat: Vasoconstrictor; decongestant (nasal).
Keywords: a-Adrenergic Agonist; Decongestant. |