Abstract
The optimization of GS39783 into potent, selective, and safe positive allosteric modulators of GABA(B) receptors is presented.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Allosteric Regulation
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Cyclopentanes / chemical synthesis*
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Cyclopentanes / chemistry
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Cyclopentanes / pharmacology*
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Drug Evaluation, Preclinical
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Molecular Structure
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Receptors, GABA-B / chemistry
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Receptors, GABA-B / drug effects*
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Structure-Activity Relationship
Substances
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Cyclopentanes
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N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine
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Pyrimidines
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Receptors, GABA-B