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].

Product Specifications

Product Name Alternative

ALKS-33-d4; RDC-0313-d4

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Opioid Receptor

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Neuronal Signaling; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C(N)C1=CC=C(C[C@H]([C@@]2(CC3)O)N(CC4)CC5C([2H])([2H])C5([2H])[2H])C([C@]42CC3=O)=C1O

Molecular Formula

C21H22D4N2O4

Molecular Weight

374.47

References & Citations

[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.