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Samidorphan

Names

[ CAS No. ]:
852626-89-2

[ Name ]:
Samidorphan

[Synonym ]:
unii-7w2581z5l8
rdc-0313-00
alks 33

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[References]

[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]. 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.  

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H26N2O4

[ Molecular Weight ]:
370.44

[ Exact Mass ]:
370.18900

[ PSA ]:
104.85000

[ LogP ]:
2.07550

Related Compounds