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This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease.
Colleen M. Niswender +2 more
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Fused heterocyclic M1 positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters, 2011Fused aromatics such as naphthalene were identified as highly potent and CNS penetrant M(1) positive allosteric modulators during an SAR study to replace the phenyl B-ring linkage.
Scott D, Kuduk +10 more
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Screening for positive allosteric modulators of biological targets
Drug Discovery Today, 2006The benefit of using positive allosteric modulators of protein function in the therapy of human diseases is becoming more apparent. The advantage of positive allosteric modulators is that they can possess specificity and selectivity profiles as well as concentration-independent limits on activity that can significantly reduce off-target effects in vivo.
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Novel bivalent positive allosteric modulators of AMPA receptor
Doklady Biochemistry and Biophysics, 2015A positive allosteric modulator of AMPA receptors has been designed using computer-aided molecular modeling techniques. It possessed a record high experimentally confirmed potency in the picomolar concentration range and belongs to a new type of bivalent AMPA receptor ligands containing bicyclo[3.3.1]nonane scaffold. The suggested structure could serve
M I, Lavrov +4 more
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mGlu2 Receptor Positive Allosteric Modulators
2016Positive allosteric modulation of the metabotropic glutamate type 2 (mGlu2) receptor has emerged as a promising mechanism for the treatment of central nervous system diseases, with the potential to provide a new and more effective avenue for the treatment of schizophrenia. Since the first discovery of mGlu2 receptor positive allosteric modulators (PAMs)
A. A. Trabanco, J. M. Cid, G. Tresadern
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