Samidorphan hydrochloride
Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals.
For research use only. We do not sell to patients.
- CAS No.: 2328045-02-7
- Formula: C21H27ClN2O4
- Molecular Weight:406.90
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Opioid Receptor Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.8 nM
Compound: 1
|
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | EC50 |
3.3 nM
Compound: 1
|
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
0.88 nM
Compound: 1
|
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
38 nM
Compound: 1
|
Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding
Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
6.9 nM
Compound: 1
|
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
Samidorphan (hydrochloride) (0-10 mg/kg, s.c., 3 h-1 week) can alter the behavior and extracellular neurotransmitter concentration of rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:WKY rat[5]
-
Dosage:0, 0.3, 1, 3, 10 mg/kg
-
Administration:Subcutaneous injection (s.c.) for 3 h, 24 h, and 1 week
-
Result:Had no significant effect at any of the doses or time points tested.
Concurrant administration of BUP (HY-177072) (0.1 mg/kg) significantly reduced immobility at 3h (p<0.01) and this effect persisted up to 1 week.
Abolished this BUPinduced hyperlocomotion.
Significantly reduced the number of marbles buried compared with vehicle-treated rats.
Attenuated BUP-induced changes of extracellular levels of serotonin and dopamine in the medial prefrontal cortex and nucleus accumbens shell.
-
Animal Model:Swiss mice (180-250 g)[4]
-
Dosage:10 mg/kg
-
Administration:Oral gavage (p.o.) for 2 weeks
-
Result:Significantly higher (P<0.05) line crossing frequency compared to stressed group in the open field maze.
Significant decrease (P<0.01) in the rearing frequency compared to control group.
Chemical Information
-
CAS No. 2328045-02-7
-
Molecular Weight 406.90
-
Formula C21H27ClN2O4
-
SMILES
O[C@@]12[C@]3(CC(CC2)=O)C4=C(O)C(C(N)=O)=CC=C4C[C@@]1([H])N(CC3)CC5CC5.Cl
-
Synonyms
ALKS-33 hydrochloride; RDC-0313 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Samidorphan hydrochloride Related Classifications
HY-123689A Related Classifications
Powered by Bioz