Title: Methylnaltrexone Bromide
CAS Registry Number: 73232-52-7; 83387-25-1 (methylnaltrexonium)
CAS Name: 17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-17-methyl-6-oxo-morphinanium bromide
Additional Names: N-cyclopropylmethyl-noroxymorphone methobromide; naltrexone methobromide
Molecular Formula: C21H26BrNO4
Molecular Weight: 436.34
Percent Composition: C 57.80%, H 6.01%, Br 18.31%, N 3.21%, O 14.67%
Literature References: Peripheral opioid receptor antagonist; quaternary derivative of naltrexone, q.v., that does not readily cross the blood brain barrier. Prepn: L. I. Goldberg et al., US 4176186 (1979 to Boehringer Ing.). Determn by HPLC and solid phase extraction in plasma and urine: J. Osinski et al., J. Chromatogr. B 780, 251 (2002). Clinical evaluation in methadone-induced constipation: C.-S. Yuan et al., J. Am. Med. Assoc. 283, 367 (2000). Clinical pharmacokinetics: idem et al., J. Clin. Pharmacol. 45, 538 (2005). Review of therapeutic potential in opioid-induced bowel dysfunction: J. F. Foss, Am. J. Surg. 182, 19S-26S (2001); of preclinical and clinical experience: C.-S. Yuan, J. Support Oncol. 2, 111-117 (2004).
Properties: Crystals from methanol/ether, mp 253°.
Melting point: mp 253°
Therap-Cat: Narcotic antagonist. In treatment of opioid bowel dysfunction.
Keywords: Narcotic Antagonist. |