Title: Naltrexone
CAS Registry Number: 16590-41-3
CAS Name: (5a)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
Additional Names: N-cyclopropylmethyl-14-hydroxydihydromorphinone
Manufacturers' Codes: UM-792
Molecular Formula: C20H23NO4
Molecular Weight: 341.40
Percent Composition: C 70.36%, H 6.79%, N 4.10%, O 18.75%
Literature References: Nonselective opioid receptor antagonist; congener of naloxone, q.v. Prepn: H. Blumberg et al., US 3332950 (1967 to Endo). Metabolism study: E. J. Cone, Tetrahedron Lett. 1973, 2607. Pharmacology and toxicity: R. P. Maickel et al., Ann. N.Y. Acad. Sci. 281, 321 (1976). Clinical pharmacology: E. R. Gritz et al., Clin. Pharmacol. Ther. 19, 773 (1976); K. Verebey et al., ibid. 20, 315 (1976). GC determn in urine: H. E. Dayton, C. E. Inturrisi, Drug Metab. Dispos. 4, 474 (1976). Review of pharmacokinetics and therapeutic use in opioid dependence: J. P. Gonzales, R. N. Brogden, Drugs 35, 192-213 (1988). Clinical trials in alcoholism: B. J. Berg et al., Drug Saf. 15, 274 (1996); R. S. Croop et al., Arch. Gen. Psychiatry 54, 1130 (1997).
Properties: Crystals from acetone, mp 168-170°. LD50 in mice (mg/kg): 586 s.c. (Maickel).
Melting point: mp 168-170°
Toxicity data: LD50 in mice (mg/kg): 586 s.c. (Maickel)
Derivative Type: Hydrochloride
CAS Registry Number: 16676-29-2
Manufacturers' Codes: EN-1639A
Trademarks: Antaxone (Zambon); Celupan (Lacer); Nalorex (DuPont Pharma); ReVia (DuPont Pharma)
Molecular Formula: C20H23NO4.HCl
Molecular Weight: 377.86
Percent Composition: C 63.57%, H 6.40%, N 3.71%, O 16.94%, Cl 9.38%
Properties: Crystals from methanol, mp 274-276°.
Melting point: mp 274-276°
Therap-Cat: Narcotic antagonist. In treatment of alcoholism.
Keywords: Narcotic Antagonist; Alcohol Dependence Treatment. |