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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H25NO3
Molecular Weight 339.4281
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ORG-25935

SMILES

COC1=CC=C2[C@H]([C@@H](CN(C)CC(O)=O)CCC2=C1)C3=CC=CC=C3

InChI

InChIKey=UEBBYLJZCHTLEG-UTKZUKDTSA-N
InChI=1S/C21H25NO3/c1-22(14-20(23)24)13-17-9-8-16-12-18(25-2)10-11-19(16)21(17)15-6-4-3-5-7-15/h3-7,10-12,17,21H,8-9,13-14H2,1-2H3,(H,23,24)/t17-,21+/m1/s1

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24525661 | https://www.ncbi.nlm.nih.gov/pubmed/22394471

Org 25935 (SCH 900435) is a synthetic drug developed by Organon International, which acts as a selective inhibitor of the glycine transporter GlyT-1. In human trial for prevention of relapse in alcohol-dependent patients in Org 25935 demonstrated no benefit over placebo in preventing alcohol relapse. Org 25935 was tested as an adjunctive treatment to atypical antipsychotics in predominant persistent negative symptoms of schizophrenia, where it did not differ significantly from placebo in reducing negative symptoms or improving cognitive functioning. Clinical trials against panic disorder did not show any benefit compared to placebo.

Originator

Curator's Comment: Aquired by Shering-Plough, and then by Merck

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P48067
Gene ID: 6536.0
Gene Symbol: SLC6A9
Target Organism: Homo sapiens (Human)
5.96 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
159 ng/mL
8 mg 2 times / day multiple, oral
dose: 8 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ORG-25935 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
165 ng/mL
12 mg 2 times / day multiple, oral
dose: 12 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ORG-25935 plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
243 ng/mL
16 mg 2 times / day multiple, oral
dose: 16 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ORG-25935 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
72 ng/mL
4 mg 2 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
ORG-25935 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
16 mg 2 times / day multiple, oral (max)
Highest studied dose
Dose: 16 mg, 2 times / day
Route: oral
Route: multiple
Dose: 16 mg, 2 times / day
Sources: Page: p.194
unhealthy, 38.8± 11.0
n = 73
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 38.8± 11.0
Sex: M+F
Population Size: 73
Sources: Page: p.194
PubMed

PubMed

TitleDatePubMed
Glycine transporter-1 blockade leads to persistently reduced relapse-like alcohol drinking in rats.
2010 Oct 15
Evaluation of the glycine transporter inhibitor Org 25935 as augmentation to cognitive-behavioral therapy for panic disorder: a multicenter, randomized, double-blind, placebo-controlled trial.
2012 May
The selective glycine uptake inhibitor org 25935 as an adjunctive treatment to atypical antipsychotics in predominant persistent negative symptoms of schizophrenia: results from the GIANT trial.
2014 Apr
Efficacy and safety of the glycine transporter-1 inhibitor org 25935 for the prevention of relapse in alcohol-dependent patients: a randomized, double-blind, placebo-controlled trial.
2014 Sep
Patents

Patents

Sample Use Guides

In clinical trial against schizophrenia Org 25935 was tested at 4 to 8 mg twice daily and 12 to 16 mg twice daily.
Route of Administration: Oral
Compound inhibition of GlyT-1 activity was determined with a scintillation proximity assay (SPA) using radiolabeled glycine ([14C]-glycine) and Cytostar-T plates. ORG 25935 inhibited GlyT-1 with IC50 of 5.96 nM.
Name Type Language
ORG-25935
Common Name English
SCH 900435
Code English
ORG 25935
Code English
GLYCINE, N-METHYL-N-(((1R,2S)-1,2,3,4-TETRAHYDRO-6-METHOXY-1-PHENYL-2-NAPHTHALENYL)METHYL)-
Systematic Name English
SCH-900435
Code English
ORG-25935 FREE BASE
Common Name English
Code System Code Type Description
DRUG BANK
DB12220
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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WIKIPEDIA
ORG 25935
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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PUBCHEM
11717074
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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EPA CompTox
DTXSID401045253
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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FDA UNII
55L20667O4
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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SMS_ID
100000175270
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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CAS
1147011-84-4
Created by admin on Fri Dec 15 16:24:27 GMT 2023 , Edited by admin on Fri Dec 15 16:24:27 GMT 2023
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