Samidorphan-d4

Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo[1].

[1]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.|[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]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.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.