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Naltrexone

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Definition: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.     
Pharmacological Action Narcotic Antagonists
Other names Schering Plough Brand of Naltrexone Hydrochloride; Hydrochloride, Naltrexone; EN1639A; EN 1639A; Bristol Myers Squibb Brand of Naltrexone Hydrochlo; United Drug Brand of Naltrexone Hydrochloride; Trexan; Schering-Plough Brand of Naltrexone Hydrochloride; ReVia; Pharmazam Brand of Naltrexone Hydrochloride; Orphan Brand of Naltrexone Hydrochloride; Nemexin; Naltrexone Hydrochloride; Nalorex; Lamepro Brand of Naltrexone Hydrochloride; Lacer Brand of Naltrexone Hydrochloride; EN-1639A; Du Pont Brand of Naltrexone Hydrochloride; Celupan; Bristol-Myers Squibb Brand of Naltrexone HydrochloDrugs* : REVIA; VIVITROL; NALTREXONE HYDROCHLORIDE
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
N-naphthoyl-beta-naltrexamine  0   Naltrexone/*analogs & derivatives Receptors, Opioid, mu/agonists Receptors, Opioid, kappa/agonists. J Med Chem. 2012 Jan 26;55(2):
iodobenzoylnaltrexamide  0   Naltrexone/*analogs & derivatives Analgesics, Opioid. Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19778-83
SDM 25N  0   Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. J Neurosci 2011 Sep 21;31(38):13346-56
KNT 93  0   *Bridged Compounds Naltrexone/*analogs & derivatives Receptors, Opioid, mu/agonists. Bioorg Med Chem Lett 2011 Jul 1;21(13):4023-6
Contrave  0   *Naltrexone *Bupropion Obesity/drug therapy Drugs, Investigational. Drugs R D. 2010;10(1):25-32
morphine, naltrexone combination  0   *Morphine *Naltrexone Drug Combinations Pain/drug therapy. J Pain. 2010 Apr;11(4):303-11EMBEDA
KMN-21 compound  0   *Guanidines Naltrexone/*analogs & derivatives. Bioorg Med Chem Lett 2009 Dec 15;19(24):6978-80
SG-II-49 compound  0   Naltrexone. Psychopharmacology (Berl) 2009 Sep;205(4):565-75
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5',6'-dihydro-3-methoxy-4'H-pyrrolo(3,2,1-ij)quinolino(2',1'-6,7)morphinan-14-ol  0   Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. Bioorg Med Chem 2008 Sep 1;16(17):7956-67
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-8'-fluoro-5',6'-dihydro-4'H-pyrrolo(3,2,1-ij)quinolino(2',1'-6,7)morphinan-3,14-diol  0   Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. Bioorg Med Chem 2008 Sep 1;16(17):7956-67
Oxytrex  0   *Naltrexone *Oxycodone. J Pain 2005 Jun;6(6):392-9
6'-guanidinonaltrindole  0   *Guanidines Naltrexone/*analogs & derivatives Receptors, Opioid/agonists. Proc Natl Acad Sci U S A 2005 Jun 21;102(25):9050-5
naltrexone-3-O-(2'-ethylbutyrate)  0   *Butyrates Naltrexone/*analogs & derivatives. J Pharm Sci. 2005 Apr;94(4):828-36
naltrexone-3-O-valerate  0   *Valerates Naltrexone/*analogs & derivatives. J Pharm Sci. 2005 Apr;94(4):828-36
3,3'-di-(N-cyclopropylmethyl-4,5-epoxy-14-hydroxymorphinan-6-one-3-yl)carbonate  0   Naltrexone/*analogs & derivatives. J Control Release 2004 Jun 18;97(2):283-90
KDAN 18  0   *Amides Naltrexone/*analogs & derivatives Receptors, Opioid, delta/agonists Receptors, Opioid, kappa/agonists. J Med Chem 2005 Mar 24;48(6):1713-6
17,17'-bis(cyclopropylmethyl)-6,6',7,7'-tetrahydro-4,5-4',5'-diepoxy-6,6'-(benzylimino)(7,7'-bimorphinan)-3,3',14,14'-tetrol  0   Naltrexone/*analogs & derivatives Receptors, Opioid, mu/agonists Receptors, Opioid, kappa/antagonists & inhibitors. J Med Chem 2005 Mar 10;48(5):1676-9
5'-acetamidinoethylnaltrindole  0   Naltrexone/*analogs & derivatives. Psychopharmacology (Berl) 2004 Apr;172(4):463-70
KDN 21  0   *Oligopeptides Naltrexone/*analogs & derivatives Ligands. J Med Chem 2004 Jun 3;47(12):2969-72
N1'-fluoroethyl-(14-formylamino)naltrindole  0   Naltrexone/*analogs & derivatives Ligands. Nucl Med Biol 2002 May;29(4):455-62
N1'-fluoroethyl-naltrindole  0   Naltrexone/*analogs & derivatives Ligands. Nucl Med Biol 2002 May;29(4):455-62
HS 378  0   Naltrexone/*analogs & derivatives. Life Sci 2001 Aug 31;69(15):1775-82
17-(cyclopropylmethyl)-4,5-epoxy-3,4-dihydroxy-6-((phthalaldehydecarboxamido)acetamido)morphinan  0   Naltrexone/*analogs & derivatives. J Med Chem 2001 Mar 29;44(7):1017-20
17-cyclopropylmethyl-6,7-didehydro-4-hydroxy-3-methoxy-6,7-2',3'-indolomorphinan  0   *Indoles Naltrexone/*analogs & derivatives Ligands Receptors, Opioid, delta/antagonists & inhibitors. J Med Chem 1999 May 6;42(9):1673-9
CNGN-TI compound  0   Naltrexone/*analogs & derivatives Receptors, Opioid, kappa/antagonists & inhibitors. J Med Chem 1998 Dec 3;41(25):4911-4
GNTI compound  0   Naltrexone/*analogs & derivatives Receptors, Opioid, kappa/antagonists & inhibitors. J Med Chem 1998 Dec 3;41(25):4911-4
7-(4-methylbenzylidene)naltrexone  0   *Benzylidene Compounds Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. J Med Chem 1998 Oct 8;41(21):4177-80
7-(2-methoxybenzylidene)naltrexone  0   *Benzylidene Compounds Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. J Med Chem 1998 Oct 8;41(21):4177-80
NTI compound  0   Naltrexone/*analogs & derivatives. Adv Exp Med Biol 1998;437:183-7
3-methoxynaltrexone  0   Naltrexone/*analogs & derivatives Heroin/agonists. FEBS Lett 1997 Jul 21;412(1):35-8
7-(5',6'-benzo-2'-spiroindanyl)naltrexone  0   *Spiro Compounds Naltrexone/*analogs & derivatives Receptors, Opioid, delta/antagonists & inhibitors. J Med Chem 1997 May 23;40(11):1720-5
N-benzylnaltrindole  0   Naltrexone/*analogs & derivatives. J Med Chem 1995 Apr 14;38(8):1337-43
17-cyclopropylmethyl-4,5-epoxy-3,14-dihydroxymorphinan-6-one-7-spiro-2'-indan  153567-07-8   Naltrexone/*analogs & derivatives. J Med Chem 1994 Mar 4;37(5):579-85
17-(cyclopropylmethyl)-7-benzyl-4,5-epoxy-3,14-dihydroxymorphinan-6-one  153567-11-4   Naltrexone/*analogs & derivatives. J Med Chem 1994 Mar 4;37(5):579-85
6-(3-phenylpropyl)oximino naltrexone  127227-11-6 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, O-(3-phenylpropyl)oxime, (5alpha)  *Oximes Naltrexone/*analogs & derivatives Receptors, Opioid/drug effects. Pharmacol Biochem Behav 1993 Jan;44(1):45-50
6-(2-phenylethyl)oximino naltrexone  127227-10-5 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, O-(2-phenylethyl)oxime, (5alpha)  *Oximes Naltrexone/*analogs & derivatives Receptors, Opioid/drug effects. Pharmacol Biochem Behav 1993 Jan;44(1):45-50
6-thioglycolamido-6-desoxynaltrexone  0   Naltrexone/*analogs & derivatives. Neurochem Res 1992 Dec;17(12):1191-4
6-bromoacetamido-6-desoxynaltrexone  91409-49-3   Naltrexone/*analogs & derivatives. Neurochem Res 1992 Dec;17(12):1191-4
7-benzylidenenaltrexone  129468-28-6 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-7-(phenylmethylene)-, (5alpha)  *Benzylidene Compounds Naltrexone/*analogs & derivatives.
Pharma Action Narcotic Antagonists
Eur J Pharmacol 1992 Jul 21;218(1):195-6
naltrexone-estrone azine  140188-23-4 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, ((3beta)-3-hydroxyestra-1,3,5(10)-trien-17-ylidene)hydrazide, (5alpha)  Naltrexone/*analogs & derivatives. Life Sci 1992;50(13):913-21
naltrindole benzofuran  111555-58-9 4,8-Methano-5H-bisbenzofuro(3,2-e:2',3'-g)isoquinoline-1,8a(9H)-diol, 7-(cyclopropylmethyl)-6,7,8,14b-tetrahydro-, (8R-(4bS*,8alpha,8beta,14bbeta))  Naltrexone/*analogs & derivatives.
Pharma Action Narcotic Antagonists
J Pharmacol Exp Ther 1991;257(2):676
naltrexone phenyl oxime  115160-07-1 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, O-phenyloxime, (5alpha)  Naltrexone/*analogs & derivatives. Pharmacol Biochem Behav 1990;37(3):497
6-deoxy-6-fluoronaltrexone  103223-57-0   Naltrexone/*analogs & derivatives. Life Sci 1990;47(24):2232
naltrindole 5'-isothiocyanate  126876-64-0   *Isothiocyanates Naltrexone/*analogs & derivatives. J Med Chem 1990;33(6):1547
naltrexamine, N(beta)-(Leu-Arg-Arg-Leu-Phe)  116764-29-5   Naltrexone/*analogs & derivatives. Int J Pept Protein Res 1988;32(6):476
nalmafene 3-O-diglucuronide  119465-20-2   Naltrexone/*analogs & derivatives. Pharm Res 1989;6(1):28
naltrexone-3-salicylate  110189-11-2   Naltrexone/*analogs & derivatives. Pharm Res 1988;5(2):113
naltrindole  111555-53-4 4,8-Methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9H)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (8R-(4bS*,8alpha,8abeta,14bbeta))  Naltrexone/*analogs & derivatives.
Pharma Action Narcotic Antagonists
Eur J Pharmacol 1988;146(1):185
pregnenolone-naltrexone azine  108743-74-4   Naltrexone/*analogs & derivatives Pregnenolone/*analogs & derivatives. Natl Inst Drug Abuse Res Monogr Ser 1986;75:45
oxymorphone-naltrexonazine  110320-71-3   Naltrexone/*analogs & derivatives Oxymorphone/*analogs & derivatives. Life Sci 1987;41(6):783
oxymorphone-3-methoxynaltrexonazine  110320-72-4   Naltrexone/*analogs & derivatives Oxymorphone/*analogs & derivatives. Life Sci 1987;41(6):783
norbinaltorphimine  105618-26-6   Naltrexone/*analogs & derivatives.
Pharma Action Narcotic Antagonists
Life Sci 1987;40(13):1287
binaltorphimine  105618-27-7   Naltrexone/*analogs & derivatives. Life Sci 1987;40(13):1287
14-chloroacetylnaltrexone  82975-76-6   Naltrexone/*analogs & derivatives Ligands. Biochem Pharmacol 1986;35(22):3995
N-methylfunaltrexamine  83339-80-4   Naltrexone/*analogs & derivatives. J Med Chem 1986;29(8):1551
10-ketonaltrexone  96445-14-6   Naltrexone/*analogs & derivatives. J Med Chem 1985;28(7):974
6,6'-(ethylenebis(oxyethyleneimino))bis(17-cyclopropylmethyl)-4,5-epoxymorphinan-3,14-diol  81919-18-8   Naltrexone/*analogs & derivatives. Life Sci 1985;36(8):801
3,6,14-trihydroxy-6-(2-carboxyallyl)-17-(cyclopropylmethyl)morphinan gamma-lactone 4,5-epoxide  92398-20-4   Naltrexone/*analogs & derivatives. J Med Chem 1984;27(12):1718
3-acetyl-6-deoxy-6-fluoronaltrexone  94696-53-4   Naltrexone/*analogs & derivatives. FEBS Lett 1984;177(2):281
beta-naltrexyl-6-ethylenediamine  0   Naltrexone/*analogs & derivatives. Biochem Biophys Res Commun 1984;119(2):624
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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012

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