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
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
DescriptionCurator'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
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.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P48067 Gene ID: 6536.0 Gene Symbol: SLC6A9 Target Organism: Homo sapiens (Human) |
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| 5.96 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
159 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17098748 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17098748 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17098748 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17098748 |
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
| Dose | Population | Adverse 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
| Title | Date | PubMed |
|---|---|---|
| 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
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
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DB12220
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ORG 25935
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11717074
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DTXSID401045253
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100000175270
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1147011-84-4
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
