Naltrexone

• CAT Number: I002171
• CAS Number: 16590-41-3
• Molecular Formula: C20H23NO4
• Molecular Weight: 341.4
• Purity: ≥95%
• Target: Opioid Receptor
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: -20°C
• IUPAC Name: (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
• InChI: InChI=1S/C20H23NO4/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11/h3-4,11,15,18,22,24H,1-2,5-10H2/t15-,18+,19+,20-/m1/s1
• InChIKey: DQCKKXVULJGBQN-XFWGSAIBSA-N
• SMILES: C1CC1CN2CCC34C5C(=O)CCC3(C2CC6=C4C(=C(C=C6)O)O5)O

Naltrexone (CAT: I002171) is a medication primarily used to manage alcohol and opioid dependence. It belongs to the class of drugs known as opioid antagonists, which work by blocking the effects of opioids in the brain. Naltrexone binds to opioid receptors and prevents the euphoric and sedative effects of opioids, reducing the cravings for opioids or alcohol. It can be taken orally in tablet form or as an extended-release injection. In addition to its use in addiction treatment, naltrexone has also been investigated for its potential in treating other conditions, such as fibromyalgia and impulse control disorders.

Overview of Clinical Research

Naltrexone is an opioid receptor antagonist. The phase II study for Alcoholism in USA starts in 2020. The fixed combination of extended-release naltrexone and bupropion has been developed as a weight loss agent and was approved for use in the United States in 2014.

Reference

1:The Use of Naltrexone in Low Doses Beyond the Approved Indication [Internet]. Ringerike T, Pike E, Nevjar J, Klemp M.Oslo, Norway: Knowledge Centre for the Health Services at The Norwegian Institute of Public Health (NIPH); 2015 Apr. PMID: 28510411 Free Books & Documents
2:New opioid receptor antagonist: naltrexone-14-O-sulfate synthesis and pharmacology. Zádor F, Király K, Váradi A, Balogh M, Fehér Á, Kocsis D, Erdei AI, Lackó E, Zádori ZS, Hosztafi S, Noszál B, Riba P, Benyhe S, Fürst S, Al-Khrasani M.Eur J Pharmacol. 2017 May 11. pii: S0014-2999(17)30343-6. doi: 10.1016/j.ejphar.2017.05.024. [Epub ahead of print] PMID: 28502630
3:A comparison of antidepressants with/without naltrexone on sexual side effects. Thapa M, Petrakis I, Ralevski E.J Dual Diagn. 2017 May 8:0. doi: 10.1080/15504263.2017.1326650. [Epub ahead of print] PMID: 28481169
4:Extended-release naltrexone for opioid use disorder started during or following incarceration. Lincoln T, Johnson BD, McCarthy P, Alexander E.J Subst Abuse Treat. 2017 Apr 6. pii: S0740-5472(16)30501-3. doi: 10.1016/j.jsat.2017.04.002. [Epub ahead of print] PMID: 28479011
5:Corrigendum to /'An evaluation of hepatic enzyme elevations among HIV-infected released prisoners enrolled in two randomized placebo-controlled trials of extended release naltrexone/' [Journal of Substance Abuse Treatment 47 (2014) 35-40]. Vagenas P, Di Paola A, Herme M, Lincoln T, Skiest DJ, Altice FL, Springer SA.J Subst Abuse Treat. 2017 Jun;77:44. doi: 10.1016/j.jsat.2017.03.008. Epub 2017 Mar 18. No abstract available. PMID: 28476270
6:Relapse to opioid use disorder after inpatient treatment: Protective effect of injection naltrexone. Nunes EV, Gordon M, Friedmann PD, Fishman MJ, Lee JD, Chen DT, Hu MC, Boney TY, Wilson D, O/'Brien CP.J Subst Abuse Treat. 2017 Apr 23. pii: S0740-5472(16)30513-X. doi: 10.1016/j.jsat.2017.04.016. [Epub ahead of print] PMID: 28473233
7:Erratum to “Correlates of retention on extended-release naltrexone among persons living with HIV infection transitioning to the community from the criminal justice system” [Drug Alcohol Depend. 157 (2015) 158–165] [No authors listed]Drug Alcohol Depend. 2016 Apr 1;161:372. doi: 10.1016/j.drugalcdep.2016.02.009. No abstract available. PMID: 28463553 Free PMC Article
8:Predictors of induction onto extended-release naltrexone among unemployed heroin-dependent adults. Jarvis BP, Holtyn AF, Berry MS, Subramaniam S, Umbricht A, Fingerhood M, Bigelow GE, Silverman K.J Subst Abuse Treat. 2017 Apr 20. pii: S0740-5472(16)30371-3. doi: 10.1016/j.jsat.2017.04.012. [Epub ahead of print] PMID: 28449955
9:Naltrexone modulates dopamine release following chronic, but not acute amphetamine administration: a translational study. Jayaram-Lindström N, Guterstam J, Häggkvist J, Ericson M, Malmlöf T, Schilström B, Halldin C, Cervenka S, Saijo T, Nordström AL, Franck J.Transl Psychiatry. 2017 Apr 25;7(4):e1104. doi: 10.1038/tp.2017.79. PMID: 28440810 Free PMC Article
10:Predictors of Naltrexone Response in a Randomized Trial: Reward-Related Brain Activation, OPRM1 Genotype, and Smoking Status. Schacht JP, Randall PK, Latham PK, Voronin KE, Book SW, Myrick H, Anton RF.Neuropsychopharmacology. 2017 Apr 14. doi: 10.1038/npp.2017.74. [Epub ahead of print] PMID: 28409564