Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H27N3O2 |
| Molecular Weight | 377.4794 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C1CCCN1C2=CN=C(OC3=CC=C4CCN(CCC4=C3)C5CCC5)C=C2
InChI
InChIKey=YFRBKEVUUCQYOW-UHFFFAOYSA-N
InChI=1S/C23H27N3O2/c27-23-5-2-12-26(23)20-7-9-22(24-16-20)28-21-8-6-17-10-13-25(19-3-1-4-19)14-11-18(17)15-21/h6-9,15-16,19H,1-5,10-14H2
| Molecular Formula | C23H27N3O2 |
| Molecular Weight | 377.4794 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
GlaxoSmithKline (GSK) was developing GSK-239512 as a histamine H3 receptor antagonist/inverse agonist as a monotherapy treatment for subjects with mild-to-moderate probable Alzheimer's disease (AD), multiple sclerosis and Schizophrenia. However, in March 2017, GSK globally discontinued the study of GSK-239512 at phase II.
Originator
Approval Year
Sample Use Guides
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 17:43:02 GMT 2023
by
admin
on
Fri Dec 15 17:43:02 GMT 2023
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| Record UNII |
4I7U5C459M
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| Record Status |
Validated (UNII)
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| Record Version |
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100000178152
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CHEMBL3092650
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720691-69-0
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GSK-239512
Created by
admin on Fri Dec 15 17:43:02 GMT 2023 , Edited by admin on Fri Dec 15 17:43:02 GMT 2023
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PRIMARY | This is a randomized, parallel group, placebo-controlled study designed to assess whether GSK239512 can enhance lesion remyelination in subjects with Relapsing Remitting Multiple Sclerosis (RRMS). | ||
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DB15120
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9976892
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admin on Fri Dec 15 17:43:02 GMT 2023 , Edited by admin on Fri Dec 15 17:43:02 GMT 2023
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4I7U5C459M
Created by
admin on Fri Dec 15 17:43:02 GMT 2023 , Edited by admin on Fri Dec 15 17:43:02 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Identifies correct structure of GSK-239512.
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ACTIVE MOIETY |
Class: Anti-dementia, Antipsychotic; Mechanism of Action: Histamine H3 receptor antagonist; Highest Development Phases: Phase II for Multiple sclerosis, No development reported for Alzheimer's disease, Discontinued for Schizophrenia; Most Recent Events: 29 Jun 2015 No recent reports on development identified - Phase-II for Alzheimer's disease in Russia, South Korea, Chile, European Union (PO), 29 Jun 2015 No recent reports on development identified - Phase-I for Alzheimer's disease in Australia (PO), 29 Jun 2015 Discontinued - Phase-II for Schizophrenia in USA (PO)
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ACTIVE MOIETY |
METHODS: The study was conducted in two parts. Part A was a single-blind, placebo run-in, flexible dose titration over 9 days in two cohorts, each consisting of two patients. Part B was a double-blind, randomised, placebo controlled, parallel group, which investigated 3 flexible dose titration regimens over 4 weeks in 3 cohorts, each consisting of eight patients.
RESULTS: Overall, the 5/10/20/40 .MU.g and 10/20/40/80 .MU.g regimens were well-tolerated. The regimen of 10/40/80/150 .MU.g showed the poorest tolerability likely due to the higher starting dose. There were no clinically significant abnormalities in haematology, clinical chemistry, urinalysis parameters and cardiovascular parameters. GSK239512 had positive effects on tasks of attention and memory with effect sizes between 0.56 and 1.37.
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ACTIVE MOIETY |
