General
Preferred name
SAMIDORPHAN
Synonyms
ALKS33 ()
ALKS-33 ()
RDC-0313 ()
SAMIDORPHAN L-MALATE ()
RDC-0313-00 ()
ALKS 33 ()
Samidorfano ()
SAMIDORPHAN COMPONENT OF ALKS-5461 ()
Samidorphan malate ()
RDC-0313-02 ()
Samidorphan l-malate component of lybalvi ()
Samidorphan HCl ()
P&D ID
PD058571
CAS
852626-89-2
2328045-02-7
Tags
drug
available
Drug indication
Alcohol dependence
Eating disorder
bipolar I disorder
Drug Status
approved
investigational
Max Phase
4.0
First approval
2021
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Samidorphan (ALKS-33) is a novel μ-opioid receptor antagonist that was developed by Alkermes . Structurally it is a analogue. The intention was for samidorphan to be used in combination with the atypical antipsychotic (in a formulation known as Lybalvi®, ALKS-3831, or the abbreviation OLZ/SAM) as a therapy for schizophrenia and bipolar disorder. Addition of samidorphan was proposed to mitigate olanzapine-induced weight gain.
(GtoPdb)
DESCRIPTION
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with ¦Ì©\opioid, ¦Ê©\opioid, and ¦Ä©\opioid receptors. Samidorphan acts as an antagonist at ¦Ì©\opioid receptors and acts as a partial agonist at k-opioid and ¦Ä©\opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo[1].
PRICE
538
DESCRIPTION
Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to ??opioid, ??opioid, and delta-opioid receptors. Samidorphan HCl is a novel ??-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
9
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Other bioactive compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
32
Molecular Weight
370.19
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
3
Ring Count
5
Aromatic Ring Count
1
cLogP
1.25
TPSA
103.86
Fraction CSP3
0.62
Chiral centers
3.0
Largest ring
6.0
QED
0.74
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Opioid Receptor
Pathway
GPCR/G protein
Neuronal Signaling
Source data
