8139. Reproterol
Nomenclature
CAS number: 54063-54-6
7-[3-[[2-(3,5-Dihydroxyphenyl)-2-hydroxyethyl]amino]propyl]-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione; 7-[3-[(β,3,5-trihydroxyphenethyl)amino]propyl]theophylline; D-1959. C18H23N5O5; mol wt 389.41.
C 55.52%, H 5.95%, N 17.98%, O 20.54%.
Description and references
Theophylline deriv which has selective activity on β2 receptors. Prepn: FR M5969 (1968 to Degussa), C.A. 71, 70644c (1969). See also FR Addn. 0308 (1970 to Degussa), C.A. 78, 72216h (1973). Synthesis: K. H. Klingler, Arzneim.-Forsch. 27, 4 (1977). Toxicology: S. Habersang, ibid. 45. Series of articles on metabolism, pharmacology and clinical trials: ibid. 15-76. Other clinical studies: D. Nolte et al., Dtsch. Med. Wochenschr. 102, 619 (1977); H. Budmiger et al., Schweiz. Med. Wochenschr. 108, 1190 (1978).
Derivative
Hydrochloride.Nomenclature
CAS number: 13055-82-8
W-2946M; Asmaterolo (Lusofarmaco); Bronchodil (Viatris); Bronchospasmin (Viatris). C18H23N5O5.HCl; mol wt 425.87.
C 50.76%, H 5.68%, N 16.44%, O 18.78%, Cl 8.32%.
Properties
Crystals, mp 249-250°. LD50 in mice (mg/kg): 148 i.v., >10,000 orally (Habersang).Therapeutic Category
Bronchodilator.
Keywords
β-Adrenergic Agonist; Bronchodilator; Ephedrine Derivatives