Results 261 to 270 of about 31,985 (308)

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, Christina N, Di Marco, Victoria, Cofre, William J, Ray, Lei, Ma, Marion, Wittmann, Matthew A, Seager, Kenneth A, Koeplinger, Charles D, Thompson, George D, Hartman, Mark T, Bilodeau   +10 more
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N-Heterocyclic derived M1 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2010
Replacement of a phenyl ring with N-linked heterocycles in a series of quinolone carboxylic acid M1 positive allosteric modulators was investigated. In particular, a pyrazole derivative exhibited improvements in potency, free fraction, and CNS exposure.
Scott D, Kuduk, Christina N, Di Marco, Victoria, Cofre, Daniel R, Pitts, William J, Ray, Lei, Ma, Marion, Wittmann, Lone, Veng, Matthew A, Seager, Kenneth, Koeplinger, Charles D, Thompson, George D, Hartman, Mark T, Bilodeau   +12 more
openaire   +2 more sources

Substrate-selective positive allosteric modulation of PTPRD’s phosphatase by flavonols

Biochemical Pharmacology, 2022
The receptor type protein tyrosine phosphatase D (PTPRD) is expressed by neurons and implicated in interesting phenotypes that include reward from addictive substances, restless leg syndrome and neurofibrillary tangle densities in Alzheimer's disease (AD-NFTs).
Ian M. Henderson, Carlissa Marez, Karol Dokladny, Jane Smoake, Maria Martinez, David Johnson, George R. Uhl   +6 more
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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, V V, Grigor'ev, S O, Bachurin, V A, Palyulin, N S, Zefirov   +4 more
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AMPA receptor positive allosteric modulators: a patent review

Expert Opinion on Therapeutic Patents, 2013
AMPA receptors represent an interesting target to develop innovative therapeutic drugs such as positive allosteric modulators, a subclass of modulators known to potentiate the effect of glutamate through this kind of glutamatergic ionotropic receptors.
Pirotte, Bernard, Francotte, Pierre, Goffin, Eric, De Tullio, Pascal   +3 more
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Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2012
A novel series of aryl azetidinyl oxadiazoles are identified as mGluR5 positive allosteric modulators (PAMs) with improved physico-chemical properties. N-substituted cyclohexyl and exo-norbornyl carboxamides, and carbamate analogs of azetidines are moderate to potent mGluR5 PAMs.
Mathivanan, Packiarajan, Christine G Mazza, Ferreira, Sang-Phyo, Hong, Andrew D, White, Gamini, Chandrasena, Xiaosui, Pu, Robbin M, Brodbeck, Albert J, Robichaud   +7 more
openaire   +2 more sources