Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H26N2O4 |
Molecular Weight | 370.4421 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)C1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]5(CC(=O)CC[C@@]35O)C2=C1O
InChI
InChIKey=RYIDHLJADOKWFM-MAODMQOUSA-N
InChI=1S/C21H26N2O4/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26)/t16-,20-,21-/m1/s1
Molecular Formula | C21H26N2O4 |
Molecular Weight | 370.4421 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Samidorphan was developed as a sublingually bioavailable µ-opioid receptor antagonist. This drug participated in clinical trials for the treatment of Schizophrenia, Alcohol Dependence, and Binge Eating Disorder. The oral dose pharmacokinetics, safety, and tolerability of samidorphan were evaluated in phase II double blind, placebo-controlled, randomized studies in healthy adults. In addition, the combination of samidorphan (SAM) with buprenorphine (BUP) was studied in phase III clinical trial in patients with major depressive disorder (MDM). It was shown that the long-term treatment did not reveal any new safety findings and confirmed that the risk of abuse and dependence with BUP/SAM was low.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01903837
Samidorphan (Low Dose). Tablets taken once daily
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 17 12:45:43 UTC 2022
by
admin
on
Sat Dec 17 12:45:43 UTC 2022
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Record UNII |
7W2581Z5L8
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C681
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C152293
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11667832
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CHEMBL426084
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7W2581Z5L8
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SUB179484
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852626-89-2
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SAMIDORPHAN
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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TARGET->PARTIAL AGONIST |
weak partial agonist
BINDING
Ki
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TARGET -> INHIBITOR |
could have very weak partial agonist activity
BINDING
Ki
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TARGET->PARTIAL AGONIST |
BINDING
Ki
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Related Record | Type | Details | ||
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ACTIVE MOIETY |