| Bioactivity | Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo[1][2][3][4]. |
| Formula | C21H21D5N2O4 |
| Molar Mass | 375.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak, et sl. Impact of deuterium substitution on the pharmacokinetics of pharmaceuticals. Annals of Pharmacotherapy 53.2 (2019): 211-236. [2]. McElroy SL, et al. A placebo-controlled pilot study of the novel opioid receptor antagonist ALKS-33 in binge eating disorder. Int J Eat Disord. 2013 Apr;46(3):239-45. [3]. Mark S. Todtenkopf, et al. Buprenorphine in Combination with Samidorphan (ALKS 33) Results in Antidepressive-Like Effects in Two Distinct Rat Models. Eur Neuropsychopharmacol. 2014;24aSuppl 2):S366. [4]. Rehan ST, et al. Samidorphan/olanzapine combination therapy for schizophrenia: Efficacy, tolerance and adverse outcomes of regimen, evidence-based review of clinical trials. Ann Med Surg (Lond). 2022 Jun 30;79:104115. |