Results 231 to 240 of about 4,995,094 (293)

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

open access: yesBioorganic and Medicinal Chemistry Letters, 2009
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
exaly   +2 more sources
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Fused heterocyclic M1 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2011
Fused 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
openaire   +2 more sources

Screening for positive allosteric modulators of biological targets

Drug Discovery Today, 2006
The 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.
openaire   +2 more sources

Novel bivalent positive allosteric modulators of AMPA receptor

Doklady Biochemistry and Biophysics, 2015
A 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
openaire   +2 more sources

mGlu2 Receptor Positive Allosteric Modulators

2016
Positive 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
openaire   +1 more source

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