Samidorphan-d₅  (Synonyms: ALKS-33-d₅; RDC-0313-d₅)

Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound 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].

375.47

C₂₁H₂₁D₅N₂O₄

Solid

O=C(N)C1=CC([2H])=C(C[C@H]([C@@]2(CC3([2H])[2H])O)N(CC4)CC5CC5)C([C@]42C([2H])([2H])C3=O)=C1O

Room temperature in continental US; may vary elsewhere.

• [1]. Russak, et sl. Impact of deuterium substitution on the pharmacokinetics of pharmaceuticals. Annals of Pharmacotherapy 53.2 (2019): 211-236.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]