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
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
PubMed
| Title | Date | PubMed |
|---|---|---|
| The safety, tolerability, pharmacokinetics and cognitive effects of GSK239512, a selective histamine H₃ receptor antagonist in patients with mild to moderate Alzheimer's disease: a preliminary investigation. | 2013 Mar |
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| A randomized, double-blind, placebo-controlled, 16-week study of the H3 receptor antagonist, GSK239512 as a monotherapy in subjects with mild-to-moderate Alzheimer's disease. | 2014 Jan |
|
| Lesion remyelinating activity of GSK239512 versus placebo in patients with relapsing-remitting multiple sclerosis: a randomised, single-blind, phase II study. | 2017 Feb |
Sample Use Guides
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100000178152
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CHEMBL3092650
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720691-69-0
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GSK-239512
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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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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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4I7U5C459M
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ACTIVE MOIETY
