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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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Positive Allosteric Modulation of the Mu Opioid Receptor
The FASEB Journal, 2022Opioid therapeutics, such as morphine, that act at the mu‐opioid receptor (MOR) are the clinical standard for patients struggling to manage symptoms associated with pain. It is widely understood that although opioids are effective at treating pain, their use leads to the development of severe adverse effects, such as constipation, addiction, and ...
Kelsey Kochan, John Traynor
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mGluR2 positive allosteric modulators: a patent review (2009 – present)
Expert Opinion on Therapeutic Patents, 2013The mGlu2 receptor, which belongs to the group II subfamily of metabotropic glutamate receptors (mGlu) along with the mGlu3 receptor, has proven to be of particular importance in neuropharmacology. Preferentially expressed on presynaptic nerve terminals, the mGlu2 receptor negatively modulates glutamate and GABA release and is widely distributed in the
Andrés A, Trabanco, José María, Cid
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Positive Allosteric Modulators of Opioid Receptors
2016Activation 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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Positive Allosteric Modulator of the Human 5-HT2C Receptor
Molecular Pharmacology, 2003The human 5-hydroxytryptamine-2C (5-HT2C) receptor has been the target of potential anxiolytics and antiobesity drugs, and its positive allosteric modulator was discovered to be l-threo-alpha-d-galacto-octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[[(4-undecyl-2-piperidinyl)carbonyl]amino]-1-thiomonohydrochloride (2S-cis) (PNU-69176E).
Wha Bin, Im +3 more
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QSAR design of triazolopyridine mGlu2 receptor positive allosteric modulators
Journal of Molecular Graphics and Modelling, 2014Two QSAR approaches were applied to assist the design and to prioritise the synthesis of new active mGlu2 receptor positive allosteric modulators (PAMs). With the aim to explore a particular point of substitution the models successfully prioritised molecules originating from chemistry ideas and a large virtual library. The two methods, 3D topomer CoMFA
Gary, Tresadern +2 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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6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters, 2022The systemic use of GABAB orthosteric agonist baclofen might be limited due to its detrimental properties: sedation and motor impairment. In contrast, GABAB positive allosteric modulators produce less adverse effects. Using BHF-177 as a starting point, we found a new active scaffold: the 6-aryl-quinazoline scaffold. Further elaborating the scaffold, we
József, Huszár +9 more
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Positive allosteric modulation of α4β2 nAChR agonist induced behaviour
Brain Research, 2012Neuronal cholinergic transmission is a prerequisite for proper CNS function. Consequently, disturbance of this system is associated with a number of pathophysiological conditions such as Parkinson's disease, Alzheimer's disease, schizophrenia and ADHD.
F, Rode +7 more
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Positive Allosteric Modulation of Antithrombin's Inhibitory Activity by RNA Aptamers
Nucleic Acid Therapeutics, 2023The leading cause of death in adults in the United States is cardiovascular disease, with mortality and morbidity mainly attributed to thromboembolism. Heparin is the most common therapy used for treating venous and arterial thrombosis. Heparin effectively accelerates the inhibition of coagulation proteases thrombin and factor Xa through the serine ...
Khalequz Zaman +3 more
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