Samidorphan
Samidorphan, also known as ALKS-33 and RDC-0313, is an opioid modulator with μ-antagonist properties. It is under development by Alkermes for the treatment of major depressive disorder and possibly other psychiatric conditions.
For research use only. We do not sell to patients.
Chemical Information
| Name | Samidorphan |
|---|---|
| Synonyms | Samidorphan; RDC 0313; RDC-0313; RDC0313; ALKS-33; ALKS33; ALKS 33; |
| Molecular Formula | C21H26N2O4 |
| Molecular Weight | 370.44 |
| Smile | O=C(C(C(O)=C1[C@@]23C4)=CC=C1C[C@@H](N(CC5CC5)CC3)[C@]2(O)CCC4=O)N |
| InChiKey | RYIDHLJADOKWFM-MAODMQOUSA-N |
| InChi | InChI=1S/C21H26N2O4/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26)/t16-,20-,21-/m1/s1 |
| CAS Number | 852626-89-2 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | 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 |
| Handling | |
| 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. |
| HS Code |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Shram MJ, Silverman B, Ehrich E, Sellers EM, Turncliff R. Use of Remifentanil in a Novel Clinical Paradigm to Characterize Onset and Duration of Opioid Blockade by Samidorphan, a Potent μ-Receptor Antagonist. J Clin Psychopharmacol. 2015 Jun;35(3):242-9. doi: 10.1097/JCP.0000000000000320. PubMed PMID: 25928699; PubMed Central PMCID: PMC4415969.
2: Turncliff R, DiPetrillo L, Silverman B, Ehrich E. Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers. Clin Ther. 2015 Feb 1;37(2):338-48. doi: 10.1016/j.clinthera.2014.10.001. Epub 2014 Oct 29. PubMed PMID: 25456560.
3: Ehrich E, Turncliff R, Du Y, Leigh-Pemberton R, Fernandez E, Jones R, Fava M. Evaluation of opioid modulation in major depressive disorder. Neuropsychopharmacology. 2015 May;40(6):1448-55. doi: 10.1038/npp.2014.330. Epub 2014 Dec 18. PubMed PMID: 25518754; PubMed Central PMCID: PMC4397403.
4: Fava M, Memisoglu A, Thase ME, Bodkin JA, Trivedi MH, de Somer M, Du Y, Leigh-Pemberton R, DiPetrillo L, Silverman B, Ehrich E. Opioid Modulation With Buprenorphine/Samidorphan as Adjunctive Treatment for Inadequate Response to Antidepressants: A Randomized Double-Blind Placebo-Controlled Trial. Am J Psychiatry. 2016 May 1;173(5):499-508. doi: 10.1176/appi.ajp.2015.15070921. Epub 2016 Feb 12. PubMed PMID: 26869247.
5: O'Malley SS, Todtenkopf MS, Du Y, Ehrich E, Silverman BL. Effects of the Opioid System Modulator, Samidorphan, on Measures of Alcohol Consumption and Patient Reported Outcomes in Adults with Alcohol Dependence. Alcohol Clin Exp Res. 2018 Jul 28. doi: 10.1111/acer.13849. [Epub ahead of print] PubMed PMID: 30055046.
6: Ragguett RM, Rong C, Rosenblat JD, Ho RC, McIntyre RS. Pharmacodynamic and pharmacokinetic evaluation of buprenorphine + samidorphan for the treatment of major depressive disorder. Expert Opin Drug Metab Toxicol. 2018 Apr;14(4):475-482. doi: 10.1080/17425255.2018.1459564. Epub 2018 Apr 6. Review. PubMed PMID: 29621905.
7: Silverman BL, Martin W, Memisoglu A, DiPetrillo L, Correll CU, Kane JM. A randomized, double-blind, placebo-controlled proof of concept study to evaluate samidorphan in the prevention of olanzapine-induced weight gain in healthy volunteers. Schizophr Res. 2018 May;195:245-251. doi: 10.1016/j.schres.2017.10.014. Epub 2017 Nov 20. PubMed PMID: 29158012.
8: Sun L, McDonnell D, Liu J, von Moltke L. Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine-Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study. Clin Pharmacol Drug Dev. 2018 Jul 30. doi: 10.1002/cpdd.601. [Epub ahead of print] PubMed PMID: 30059196.
Chemical Structure
