Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H20N2O2 |
| Molecular Weight | 308.3743 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(\C=C2/CCCN=C2C3=CC=CN=C3)C(OC)=C1
InChI
InChIKey=RPYWXZCFYPVCNQ-RVDMUPIBSA-N
InChI=1S/C19H20N2O2/c1-22-17-8-7-14(18(12-17)23-2)11-15-5-4-10-21-19(15)16-6-3-9-20-13-16/h3,6-9,11-13H,4-5,10H2,1-2H3/b15-11+
GTS-21 (also known as DMBX-A), a selective alpha-7 nicotinic acetylcholine receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. GTS-21 has been studied in Phase II in patients with schizophrenia and in patients with Alzheimer disease. However, these studies were discontinued. GTS-21 was also involved in phase II to reduce negative affect, improve cognition and/or reduce smoking relapse in healthy adult men and women who are chronic cigarette smokers. However, this study was withdrawn. Besides, GTS-21 has participated in phase II to investigate safety and efficacy in adults with attention-deficit hyperactivity disorder.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Gain of function mutation of the alpha7 nicotinic receptor: distinct pharmacology of the human alpha7V274T variant. | 1999 Feb 5 |
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| Metabolism and disposition of GTS-21, a novel drug for Alzheimer's disease. | 1999 Jul |
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| Selective alpha 7 nicotinic receptor stimulation normalizes chronic cocaine-induced loss of hippocampal sensory inhibition in C3H mice. | 1999 Nov 15 |
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| GTS-21, a mixed nicotinic receptor agonist/antagonist, does not affect the nicotine cue. | 1999 Oct |
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| The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). | 2000 Aug |
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| Genetic and pharmacological strategies identify a behavioral function of neuronal nicotinic receptors. | 2000 Aug |
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| Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. | 2003 Mar |
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| GABAergic systems modulate nicotinic receptor-mediated seizures in mice. | 2003 Sep |
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| Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia. | 2004 Jun |
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NCT00952393
Created by
admin on Fri Dec 15 16:07:00 GMT 2023 , Edited by admin on Fri Dec 15 16:07:00 GMT 2023
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PRIMARY | Nicotinic Receptors and Schizophrenia | ||
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8S399XDN2K
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5310985
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GTS-21
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DB05708
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DTXSID701027513
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148372-04-7
Created by
admin on Fri Dec 15 16:07:00 GMT 2023 , Edited by admin on Fri Dec 15 16:07:00 GMT 2023
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ACTIVE MOIETY
