Results 1 to 10 of about 121,181 (303)

Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator [PDF]

Cells, 2022
The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li, Yiqiong Bao, Ran Xu, Miaomiao Li, Lili Xi, Jingjing Guo   +5 more
doaj   +6 more sources

Mechanism and function of GPR3 regulated by a negative allosteric modulator [PDF]

Nature Communications
Allosteric modulators have gained substantial interest in current GPCR drug discovery. Here, we present a mechanism of allosteric modulation involving the dimerization of GPR3, a promising drug target for metabolic diseases and central nervous system ...
Geng Chen, Jana Bláhová, Nico Staffen, Harald Hübner, Nadja Nunhöfer, Chen Qiu, Peter Gmeiner, Dorothee Weikert, Yang Du, Jun Xu   +9 more
doaj   +7 more sources

Capsaicin Is a Negative Allosteric Modulator of the 5-HT3 Receptor [PDF]

Frontiers in Pharmacology, 2020
In this study, effects of capsaicin, an active ingredient of the capsicum plant, were investigated on human 5-hydroxytryptamine type 3 (5-HT3) receptors.
Eslam El Nebrisi, Eslam El Nebrisi, Tatiana Prytkova, Dietrich Ernst Lorke, Dietrich Ernst Lorke, Luke Howarth, Asma Hassan Alzaabi, Keun-Hang Susan Yang, Frank C. Howarth, Murat Oz   +9 more
doaj   +9 more sources

COR758, a negative allosteric modulator of GABAB receptors [PDF]

Neuropharmacology, 2021
Allosteric modulators of G protein coupled receptors (GPCRs), including GABABRs (GABABRs), are promising therapeutic candidates. While several positive allosteric modulators (PAM) of GABABRs have been characterized, only recently the first negative ...
Miriam Melis, Valeria Sogos, Sarah Beggiato   +2 more
exaly   +9 more sources

Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator. [PDF]

ACS Med Chem Lett, 2023
Glutamate plays a key role in cognition and mood, and it has been shown that inhibiting ionotropic glutamate receptors disrupts cognition, while enhancing ionotropic receptor activity is pro-cognitive.
Rudd MT, Manley PJ, Hanney B, Meng Z, Shu Y, de Leon P, Frie JL, Han Y, Wai JM, Yang ZQ, Perkins JJ, Hurzy DM, Manikowski JJ, Zhu H, Bungard CJ, Converso A, Meissner RS, Cosden ML, Hayashi I, Ma L, O'Brien J, Uebele VN, Schachter JB, Bhandari N, Ward GJ, Fillgrove KL, Lu B, Liang Y, Dubost DC, Puri V, Eddins DM, Vardigan JD, Drolet RE, Kern JT, Uslaner JM.   +34 more
europepmc   +5 more sources

Radiprodil, a NR2B negative allosteric modulator, from bench to bedside in infantile spasm syndrome [PDF]

Annals of Clinical and Translational Neurology, 2020
Objective Infantile spasm syndrome (ISS) is an epileptic encephalopathy without established treatment after the failure to standard of care based on steroids and vigabatrin.
Stéphane Auvin, Blandine Dozières‐Puyravel, Andreja Avbersek, David Sciberras, Jo Collier, Karine Leclercq, Pavel Mares, Rafal M. Kaminski, Pierandrea Muglia   +8 more
doaj   +3 more sources

Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor. [PDF]

Br J Pharmacol, 2015
Background and Purpose Cannabidiol has been reported to act as an antagonist at cannabinoid CB 1 receptors. We hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB
Laprairie RB, Bagher AM, Kelly ME, Denovan-Wright EM.   +3 more
europepmc   +5 more sources

An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups [PDF]

eLife, 2018
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to ...
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis   +10 more
doaj   +3 more sources

Identification of a β-arrestin-biased negative allosteric modulator for the β₂-adrenergic receptor. [PDF]

Proc Natl Acad Sci U S A, 2023
Significance Biased ligand pharmacology seeks to develop agents that can activate a subset of a receptor’s signaling capabilities. The β2AR (β2-adrenergic receptor) exhibits pleiotropic signaling and efforts to develop biased ligands have focused on ...
Ippolito M, De Pascali F, Hopfinger N, Komolov KE, Laurinavichyute D, Reddy PAN, Sakkal LA, Rajkowski KZ, Nayak AP, Lee J, Lee J, Cao G, Donover PS, Reichman M, An SS, Salvino JM, Penn RB, Armen RS, Scott CP, Benovic JL.   +19 more
europepmc   +2 more sources

Effect of the Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulator Dipraglurant on Motor and Non-Motor Symptoms of Parkinson's Disease. [PDF]

Cells, 2023
Parkinson’s disease (PD) patients suffer not only from the primary motor symptoms of the disease but also from a range of non-motor symptoms (NMS) that cause disability and low quality of life.
Epping-Jordan MP, Girard F, Bessis AS, Mutel V, Boléa C, Derouet F, Bessif A, Mingard B, Barbier S, Paradis JS, Rocher JP, Lütjens R, Kalinichev M, Poli S.   +13 more
europepmc   +2 more sources