Nalmefene
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MedKoo CAT#: 596218

CAS#: 55096-26-9

Description: Nalmefene (trade name Selincro), originally known as nalmetrene, is an opioid antagonist used primarily in the management of alcohol dependence. It has also been investigated for the treatment of other addictions such as pathological gambling. Nalmefene is an opiate derivative similar in both structure and activity to the opioid antagonist naltrexone. Advantages of nalmefene relative to naltrexone include longer half-life, greater oral bioavailability and no observed dose-dependent liver toxicity.


Price and Availability

Size
Price

10mg
USD 265
Size
Price

50mg
USD 390
Size
Price

100mg
USD 590

Nalmefene purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 596218
Name: Nalmefene
CAS#: 55096-26-9
Chemical Formula: C21H25NO3
Exact Mass: 339.1834
Molecular Weight: 339.43
Elemental Analysis: C, 74.31; H, 7.42; N, 4.13; O, 14.14


Synonym: Nalmefene; Nalmefeno; ORF 11676; ORF-11676; ORF11676; JF-1; JF 1;JF1

IUPAC/Chemical Name: (4R,4aS,7aS,12bS)-3-(cyclopropylmethyl)-7-methylene-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol

InChi Key: WJBLNOPPDWQMCH-MBPVOVBZSA-N

InChi Code: InChI=1S/C21H25NO3/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13/h4-5,13,16,19,23-24H,1-3,6-11H2/t16-,19+,20+,21-/m1/s1

SMILES Code: OC(C1=C2[C@@]34[C@@]5([H])O1)=CC=C2C[C@@H](N(CC6CC6)CC4)[C@]3(O)CCC5=C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Guerzoni S, Pellesi L, Pini LA, Caputo F. Drug-drug interactions in the treatment for alcohol use disorders: A comprehensive review. Pharmacol Res. 2018 Apr 30;133:65-76. doi: 10.1016/j.phrs.2018.04.024. [Epub ahead of print] Review. PubMed PMID: 29719204.

2: Uhari-Väänänen J, Raasmaja A, Bäckström P, Oinio V, Carroll FI, Airavaara M, Kiianmaa K, Piepponen P. The κ-opioid receptor antagonist JDTic decreases ethanol intake in alcohol-preferring AA rats. Psychopharmacology (Berl). 2018 May;235(5):1581-1591. doi: 10.1007/s00213-018-4868-x. Epub 2018 Feb 28. PubMed PMID: 29492614.

3: Barrio P, Ortega L, Guardia J, Roncero C, Yuguero L, Gual A. Reply to Braillon et al.: Nalmefene Phase IV Study: A Seeding Flying in the Face of Evidence? Clin Drug Investig. 2018 Apr;38(4):387-388. doi: 10.1007/s40261-018-0625-5. PubMed PMID: 29480453.

4: Khouri C, Arbib F, Revol B, Pepin JL, Tamisier R. Severe central sleep apnoea associated with nalmefene: a case report. Br J Clin Pharmacol. 2018 May;84(5):1075-1076. doi: 10.1111/bcp.13547. Epub 2018 Feb 26. PubMed PMID: 29479731; PubMed Central PMCID: PMC5903229.

5: Braillon A, Taiebi F, Bernoussi A. Nalmefene Phase IV Study: A Seeding Flying in the Face of Evidence? Clin Drug Investig. 2018 Apr;38(4):385-386. doi: 10.1007/s40261-018-0628-2. PubMed PMID: 29476330.

6: Donoghue K. Commentary on Palpacuer et al. (2018): Do small effects on total alcohol consumption translate into clinical practice? Addiction. 2018 Feb;113(2):238-239. doi: 10.1111/add.14081. PubMed PMID: 29314404.

7: Urbanoski K, Cheng J, Rehm J, Kurdyak P. Frequent use of emergency departments for mental and substance use disorders. Emerg Med J. 2018 Apr;35(4):220-225. doi: 10.1136/emermed-2015-205554. Epub 2018 Jan 8. PubMed PMID: 29311114.

8: Spanagel R. Animal models of addiction. Dialogues Clin Neurosci. 2017 Sep;19(3):247-258. PubMed PMID: 29302222; PubMed Central PMCID: PMC5741108.

9: Litten RZ, Falk DE, Ryan ML, Fertig J, Leggio L. Advances in Pharmacotherapy Development: Human Clinical Studies. Handb Exp Pharmacol. 2018 Jan 3. doi: 10.1007/164_2017_79. [Epub ahead of print] PubMed PMID: 29294197.

10: Wu Q, Chen X, Wang J, Sun P, Weng M, Chen W, Sun Z, Zhu M, Miao C. Nalmefene attenuates malignant potential in colorectal cancer cell via inhibition of opioid receptor. Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):156-163. doi: 10.1093/abbs/gmx131. PubMed PMID: 29267844.

11: Salimi V, Mirzaei H, Ramezani A, Tahamtan A, Jamali A, Shahabi S, Golaram M, Minaei B, Gharagozlou MJ, Mahmoodi M, Bont L, Shokri F, Mokhtari-Azad T. Blocking of opioid receptors in experimental formaline-inactivated respiratory syncytial virus (FI-RSV) immunopathogenesis: from beneficial to harmful impacts. Med Microbiol Immunol. 2018 Apr;207(2):105-115. doi: 10.1007/s00430-017-0531-0. Epub 2017 Dec 18. PubMed PMID: 29256094.

12: Antonelli M, Ferrulli A, Sestito L, Vassallo GA, Tarli C, Mosoni C, Rando MM, Mirijello A, Gasbarrini A, Addolorato G. Alcohol addiction - the safety of available approved treatment options. Expert Opin Drug Saf. 2018 Feb;17(2):169-177. doi: 10.1080/14740338.2018.1404025. Epub 2017 Nov 20. Review. PubMed PMID: 29120249.

13: Millier A, Laramée P, Rahhali N, Aballéa S, Daeppen JB, Rehm J, Toumi M. Cost-Effectiveness of Nalmefene Added to Psychosocial Support for the Reduction of Alcohol Consumption in Alcohol-Dependent Patients With High/Very High Drinking Risk Levels: A Microsimulation Model. J Stud Alcohol Drugs. 2017 Nov;78(6):867-876. PubMed PMID: 29087821.

14: Barrio P, Ortega L, Guardia J, Roncero C, Yuguero L, Gual A. Who Receives Nalmefene and How Does It Work in the Real World? A Single-Arm, Phase IV Study of Nalmefene in Alcohol Dependent Outpatients: Baseline and 1-Month Results. Clin Drug Investig. 2018 Feb;38(2):147-155. doi: 10.1007/s40261-017-0590-4. PubMed PMID: 29080208.

15: Coppola M, Mondola R. Opioid receptor antagonists in the treatment of pathological gambling. J Opioid Manag. 2017 Jul/Aug;13(4):205-206. doi: 10.5055/jom.2017.0388. PubMed PMID: 28983886.

16: Palpacuer C, Duprez R, Huneau A, Locher C, Boussageon R, Laviolle B, Naudet F. Pharmacologically controlled drinking in the treatment of alcohol dependence or alcohol use disorders: a systematic review with direct and network meta-analyses on nalmefene, naltrexone, acamprosate, baclofen and topiramate. Addiction. 2018 Feb;113(2):220-237. doi: 10.1111/add.13974. Epub 2017 Sep 20. Review. PubMed PMID: 28940866.

17: Pujol CN, Paasche C, Laprevote V, Trojak B, Vidailhet P, Bacon E, Lalanne L. Cognitive effects of labeled addictolytic medications. Prog Neuropsychopharmacol Biol Psychiatry. 2018 Feb 2;81:306-332. doi: 10.1016/j.pnpbp.2017.09.008. Epub 2017 Sep 14. Review. PubMed PMID: 28919445.

18: Johansen KGV, Tarp S, Astrup A, Lund H, Pagsberg AK, Christensen R. Harms associated with taking nalmefene for substance use and impulse control disorders: A systematic review and meta-analysis of randomised controlled trials. PLoS One. 2017 Aug 29;12(8):e0183821. doi: 10.1371/journal.pone.0183821. eCollection 2017. Review. PubMed PMID: 28850596; PubMed Central PMCID: PMC5574613.

19: Callaghan CK, Rouine J, Dean RL, Knapp BI, Bidlack JM, Deaver DR, O'Mara SM. Antidepressant-like effects of 3-carboxamido seco-nalmefene (3CS-nalmefene), a novel opioid receptor modulator, in a rat IFN-α-induced depression model. Brain Behav Immun. 2018 Jan;67:152-162. doi: 10.1016/j.bbi.2017.08.016. Epub 2017 Aug 24. PubMed PMID: 28844812.

20: Lescut C, Gaboriau L, Carton L, Rolland B. Naltrexone- or Nalmefene-Related Buprenorphine Withdrawal: Treat It With… More Buprenorphine. J Clin Psychopharmacol. 2017 Oct;37(5):631-633. doi: 10.1097/JCP.0000000000000763. PubMed PMID: 28806388.