Results 291 to 300 of about 107,657 (326)

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

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
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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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Positive Allosteric Modulators of Opioid Receptors

2016
Activation of opioid receptors produces powerful analgesia; and µ-opioid receptor agonists such as morphine and oxycodone remain the “gold standard” for pain therapy, despite their abuse liability and dangerous side effect profile. Safer pain medications are urgently needed.
Kristin L. Rockwell, Andrew Alt
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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
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First in Human Trial of a Type I Positive Allosteric Modulator of Alpha7-Nicotinic Receptors: Pharmacokinetics, Safety, and Evidence for Neurocognitive Effect of AVL-3288

Journal of Psychopharmacology, 2017
Type I positive allosteric modulators (PAMs) of the alpha7-nicotinic receptor enhance its cholinergic activation while preserving the spatiotemporal features of synaptic transmission and the receptor’s characteristic rapid desensitization kinetics ...
K. Gee, A. Olincy, R. Kanner, L. Johnson, D. Hogenkamp, Josette G. Harris, M. Tran, Stephen A Edmonds, R. Yoshimura, T. Johnstone, R. Freedman   +10 more
semanticscholar   +1 more source

Large library docking identifies positive allosteric modulators of the calcium-sensing receptor

Science
Positive allosteric modulator (PAM) drugs enhance the activation of the calcium-sensing receptor (CaSR) and suppress parathyroid hormone (PTH) secretion.
Fangyu Liu, Cheng-Guo Wu, Chia-Ling Tu, Isabella S. Glenn, Justin Meyerowitz, Anat Levit Kaplan, Jiankun Lyu, Zhiqiang Cheng, Olga O. Tarkhanova, Yurii S. Moroz, J. Irwin, Wenhan Chang, B. Shoichet, G. Skiniotis   +13 more
semanticscholar   +1 more source

In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor

European Journal of Pharmacology, 2004
The present study was aimed at assessing the in vivo effectiveness of the positive allosteric modulator of the gamma-aminobutyric acidB (GABAB) receptor, CGP7930 [2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol]. The synergistic potentiation of GABAB receptor functioning, previously observed in different in vitro assays, has been confirmed ...
Carai MAM, Colombo G, Froestl W, Gessa GL   +3 more
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Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

Bioorganic & Medicinal Chemistry Letters, 2016
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA receptor function, suggesting the potential utility of mGluR5 positive allosteric modulators (PAMs) in ...
Andrew P. Degnan, Darrell Maxwell, Anand Balakrishnan, Jeffrey M. Brown, Amy Easton, Michael Gulianello, Umesh Hanumegowda, Melissa Hill-Drzewi, Regina Miller, Kenneth S. Santone, Arun Senapati, Eric E. Shields, Digavalli V. Sivarao, Ryan Westphal, Valerie J. Whiterock, Xiaoliang Zhuo, Joanne J. Bronson, John E. Macor   +17 more
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An mGlu4‐Positive Allosteric Modulator Alleviates Parkinsonism in Primates

Movement Disorders, 2018
Background: Levodopa remains the gold‐standard treatment for PD. However, it becomes less effective as the disease progresses and produces debilitating side effects, such as motor fluctuations and l‐dopa‐induced dyskinesia.
D. Charvin, T. Di Paolo, E. Bézard, L. Grégoire, A. Takano, G. Duvey, E. Pioli, C. Halldin, R. Medori, F. Conquet   +9 more
semanticscholar   +1 more source