Results 31 to 40 of about 11,411 (182)

Functional Selectivity Does Not Predict Antinociceptive/Locomotor Impairing Potencies of NOP Receptor Agonists

Frontiers in Neuroscience, 2021
Nociceptin/orphanin FQ controls several functions, including pain transmission, via stimulation of the N/OFQ peptide (NOP) receptor. Here we tested the hypothesis that NOP biased agonism may be instrumental for identifying innovative analgesics. In vitro
Joaquim Azevedo Neto, Chiara Ruzza, Chiara Ruzza, Chiara Sturaro, Davide Malfacini, Salvatore Pacifico, Nurulain T. Zaveri, Girolamo Calò   +7 more
doaj   +1 more source

Pharmacological Insights Into Safety and Efficacy Determinants for the Development of Adenosine Receptor Biased Agonists in the Treatment of Heart Failure

Frontiers in Pharmacology, 2021
Adenosine A1 receptors (A1R) are a potential target for cardiac injury treatment due to their cardioprotective/antihypertrophic actions, but drug development has been hampered by on-target side effects such as bradycardia and altered renal hemodynamics ...
Patricia Rueda, Jon Merlin, Stefano Chimenti, Michel Feletou, Jerome Paysant, Paul J. White, Arthur Christopoulos, Patrick M. Sexton, Roger J. Summers, William N. Charman, Lauren T. May, Christopher J. Langmead   +11 more
doaj   +1 more source

Bias-inducing allosteric binding site in mu-opioid receptor signaling

SN Applied Sciences, 2021
G-protein-biased agonism of the mu-opioid receptor (μ-OR) is emerging as a promising strategy in analgesia. A deep understanding of how biased agonists modulate and differentiate G-protein-coupled receptors (GPCR) signaling pathways and how this is ...
Andrés F. Marmolejo-Valencia, Abraham Madariaga-Mazón, Karina Martinez-Mayorga   +2 more
doaj   +1 more source

Biased agonism [PDF]

F1000 Biology Reports, 2009
Seven-transmembrane receptors are commonly coupled to multiple signaling pathways in cells. The simple model describing agonists for these receptors as producing a common active state to induce uniform activation of the pathways linked to the receptor has been shown to be untenable in light of a large body of data that suggest that some agonists ...
openaire   +2 more sources

A novel mechanism of action for angiotensin-(1-7) via the angiotensin type 1 receptor [PDF]

, 2016
No abstract ...
Nicklin, Stuart A.
core   +1 more source

Fingerprinting heterocellular β-adrenoceptor functional expression in the brain using agonist activity profiles

Frontiers in Molecular Biosciences, 2023
Noradrenergic projections from the brainstem locus coeruleus drive arousal, attentiveness, mood, and memory, but specific adrenoceptor (AR) function across the varied brain cell types has not been extensively characterized, especially with agonists. This
Rachel A. Matt, Frederick G. Westhorpe, Rosemary F. Romuar, Payal Rana, Joel R. Gever, Anthony P. Ford   +5 more
doaj   +1 more source

Multidisciplinary Consideration of Potential Pathophysiologic Mechanisms of Paradoxical Erythema with Topical Brimonidine Therapy. [PDF]

, 2016
Rosacea is a chronic inflammatory disease with transient and non-transient redness as key characteristics. Brimonidine is a selective α2-adrenergic receptor (AR) agonist approved for persistent facial erythema of rosacea based on significant efficacy and
Detmar, Michael, Di Nardo, Anna, Docherty, James R, Holmes, Anna, Lorton, Dianne, Schäfer, Gregor, Steinhoff, Martin   +6 more
core   +2 more sources

Structural Basis of the Diversity of Adrenergic Receptors

Cell Reports, 2019
Summary: Adrenergic receptors are highly homologous while at the same time display a wide diversity of ligand and G-protein binding, and understanding this diversity is key for designing selective or biased drugs for them.
Lu Qu, Qingtong Zhou, Yueming Xu, Yu Guo, Xiaoyu Chen, Deqiang Yao, Gye Won Han, Zhi-Jie Liu, Raymond C. Stevens, Guisheng Zhong, Dong Wu, Suwen Zhao   +11 more
doaj   +1 more source

Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias

Frontiers in Pharmacology, 2021
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos   +7 more
doaj   +1 more source

Rates of agonism among female primates: a cross-taxon perspective [PDF]

, 2013
Agonism is common in group-living animals, shaping dominance relationships and ultimately impacting individual tness. Rates of agonism vary considerably among taxa, however, and explaining this variation has been central in ecological models of female ...
Altmann, Altmann, Andreas Koenig, Arnold, Asensio, Aureli, Barta, Barton, Barton, Bertram, Blumstein, Boinski, Borries, Brandon C. Wheeler, Broom, Burnham, Chancellor, Chancellor, Cheney, Clara J. Scarry, Clutton-Brock, Clutton-Brock, Clutton-Brock, Cords, Cowlishaw, Crockett, Crombie, Côté, Davies, De Ruiter, Di Bitetti, Drews, Dubois, Dubuc, Emlen, Enquist, Erhart, Felsenstein, Frank, Freckleton, Freckleton, Freckleton, Goldberg, Goss-Custard, Goss-Custard, Harcourt, Harcourt, Heesen, Hill, Hirsch, Hirsch, Hoogland, Huchard, Isbell, Isbell, IUCN, Janson, Janson, Janson, Janson, Janson, Janson, Janson, Jones, Keller, Klein, Knox, Koenig, Koenig, Koenig, Koenig, Koenig, Koenig, Korstjens, Krause, Kuester, Lee, Lu, Majolo, Marmet, Martin, Maynard-Smith, McKenna, Miller, Mitchell, Monaghan, Moore, Nicholson, Orme, Pagel, Phillips, Pruetz, Pusey, R Development Core Team, Range, Rayor, Revell, Risenhoover, Ron, Say, Sayers, Seyfarth, Silk, Sirot, Small, Snaith, Sokal, Steenbeek, Sterck, Sterck, Sterck, Strier, Sussman, Sussman, Symonds, Thouless, Tiddi, Treves, Trivers, van Hooff, van Schaik, van Schaik, Vogel, Vogel, Vogel, Vogel, Watts, Whitten, Wrangham, Wrangham, Yeager, Zinner   +131 more
core   +1 more source