Results 41 to 50 of about 3,750,504 (279)

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 [PDF]

Bioorganic & Medicinal Chemistry Letters, 2013
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacement for the piperazine ring found in the initial hit compound. Characterization of selected compounds in
Jason T, Manka, Alice L, Rodriguez, Ryan D, Morrison, Daryl F, Venable, Hyekyung P, Cho, Anna L, Blobaum, J Scott, Daniels, Colleen M, Niswender, P Jeffrey, Conn, Craig W, Lindsley, Kyle A, Emmitte   +10 more
openaire   +2 more sources

A Novel Family of Negative and Positive Allosteric Modulators of NMDA Receptors [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2010
The N-methyl-D-aspartate (NMDA) receptor family regulates various central nervous system functions, such as synaptic plasticity. However, hypo- or hyperactivation of NMDA receptors is critically involved in many neurological and psychiatric conditions, such as pain, stroke, epilepsy, neurodegeneration, schizophrenia, and depression.
Costa, BM, Irvine, MW, Fang, G, Eaves, RJ, Mayo-Martin, MB, Skifter, DA, Jane, DE, Monaghan, DT   +7 more
openaire   +3 more sources

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

eLife, 2017
Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type
Joan Font, Marc López-Cano, Serena Notartomaso, Pamela Scarselli, Paola Di Pietro, Roger Bresolí-Obach, Giuseppe Battaglia, Fanny Malhaire, Xavier Rovira, Juanlo Catena, Jesús Giraldo, Jean-Philippe Pin, Víctor Fernández-Dueñas, Cyril Goudet, Santi Nonell, Ferdinando Nicoletti, Amadeu Llebaria, Francisco Ciruela   +17 more
doaj   +1 more source

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]

Bioorganic & Medicinal Chemistry Letters, 2016
Les modulateurs allostériques négatifs (MNA) CB1 existants appartiennent à une gamme limitée de classes structurelles. Malgré le potentiel théorique des NAM CB1, les études in vivo publiées n'ont généralement pas été en mesure de démontrer les effets thérapeutiques attendus médiés par CB1.
Iain R. Greig, Gemma L. Baillie, Mostafa H. Abdelrahman, Laurent Trembleau, Ruth A. Ross   +4 more
openaire   +3 more sources

An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]

, 2020
Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio, Kobilka, Brian K, Liu, Xiangyu, Magdalena Korczynska, Xu, Xinyu, Stanek, Markus, Matt, Rachel Ann, Shoichet, Brian K, Stößel, Anne, Jake Mahoney, Xiangyu Liu, Brian K. Shoichet, Clark, Mary J, Harald Hübner, Kaindl, Jonas, Hübner, Harald, Peter Gmeiner, Sunahara, Roger K, Markus Stanek, Daniela Dengler, Korczynska, Magdalena, Dengler, Daniela, Kunio Hirata, Roger K. Sunahara, Mahoney, Jake, Xinyu Xu, Gmeiner, Peter, Anne Stößel, Brian K. Kobilka, Jonas Kaindl, Rachel Ann Matt, Mary J. Clark   +31 more
core   +1 more source

Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters

Data in Brief, 2017
The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative ...
Carolina L. Haass-Koffler, Kimberly Goodyear, Victoria M. Long, Harrison H. Tran, Antonella Loche, Roberto Cacciaglia, Robert M. Swift, Lorenzo Leggio   +7 more
doaj   +1 more source

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Communications Biology, 2020
Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other ...
Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker   +17 more
doaj   +1 more source

Sodium functions as a negative allosteric modulator of the oxytocin receptor

Biochimica et Biophysica Acta (BBA) - Biomembranes, 2018
The oxytocin receptor, a class A G protein coupled receptor (GPCR), is essentially involved in the physiology of reproduction. Two parameters are crucially important to support high-affinity agonist binding of the receptor: Mg2+ and cholesterol, both acting as positive modulators.
Andrea, Schiffmann, Gerald, Gimpl
openaire   +2 more sources

Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine [v1; ref status: indexed, http://f1000r.es/o0]

F1000Research, 2013
We investigated the role of metabotropic glutamate receptor type 5 (mGluR5) in methamphetamine-induced behavioral sensitization. The mGluR5 positive allosteric modulator (3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamide (CDPPB) and negative allosteric ...
Peter R Kufahl, Natali E Nemirovsky, Lucas R Watterson, Nicholas Zautra, M Foster Olive   +4 more
doaj   +1 more source

Distinctive binding properties of the negative allosteric modulator, [3H]SB269,652, at recombinant dopamine D3 receptors [PDF]

, 2018
Recently, employing radioligand displacement and functional coupling studies, we demonstrated that SB269,652 (N-[(1r,4r)-4-[2-(7-cyano-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-1H-indole-2-carboxamide) interacts in an atypical manner with ...
Mannoury la Cour, Clotilde, Irene Fasciani, Fasciani, Irene, Clotilde Mannoury la Cour, Aloisi, Gabriella, Ilaria Pietrantoni, Mario Rossi, Roberto Maggio, Millan, Mark J., Mark J. Millan, Gabriella Aloisi, Francesco Marampon, Marco Scarselli, Maggio, Roberto, Rossi, Mario, Millan, Mark J, Marampon, Francesco, Scarselli, Marco, Pietrantoni, Ilaria   +18 more
core   +1 more source