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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
Structure of SAMIDORPHAN

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

HIDE SMILES / InChI

Molecular Formula C21H26N2O4
Molecular Weight 370.4421
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

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

PubMed

Sample Use Guides

In Vivo Use Guide
Samidorphan (Low Dose). Tablets taken once daily
Route of Administration: Oral
Substance Class Chemical
Record UNII
7W2581Z5L8
Record Status Validated (UNII)
Record Version