Samidorphan

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. Samidorphan can improve the behavior of depressed animals[1][2][3][4][5].

Product Specifications

CAS Number

[852626-89-2]

Product Name Alternative

ALKS-33; RDC-0313

UNSPSC

12352005

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/samidorphan.html

Concentration

10mM

Purity

99.04

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H26N2O4

Molecular Weight

370.44

References & Citations

[1]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.|[2]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.|[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]Shravni V, et al. Comparative Effects of Buprenorphine and Samidorphan on Locomotor Behavior in vivo. Scientific Research Journal of Pharmacy 2021, Volume 1, Issue: 1 (June-July) . |[5]Smith KL, et al. Opioid system modulators buprenorphine and samidorphan alter behavior and extracellular neurotransmitter concentrations in the Wistar Kyoto rat. Neuropharmacology. 2019 Mar 1;146:316-326.