Results 91 to 100 of about 46,183 (248)

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E, Mahoney, Jacob P, Manglik, Aashish, Sunahara, Roger K, Traynor, John R   +4 more
core  

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

Minocycline and bone marrow–derived mononuclear cells as potential therapeutics for hereditary retinal degenerations

Acta Ophthalmologica, EarlyView.
Abstract Purpose To assess in Royal College of Surgeons (RCS) rats if the combination of two previously documented neuroprotective strategies: minocycline administration and bone marrow–derived mononuclear cells (BM‐MNCs) intravitreal transplantation, offers enhanced neuroprotection compared with each treatment alone.
Alba Videla‐Ristol, Ana Martínez‐Vacas, David García‐Bernal, Manuel Vidal‐Sanz, María Paz Villegas‐Pérez, Diego García‐Ayuso, Johnny Di Pierdomenico   +6 more
wiley   +1 more source

Itch/β-arrestin2-dependent non-proteolytic ubiquitylation of SuFu controls Hedgehog signalling and medulloblastoma tumorigenesis [PDF]

, 2018
Suppressor of Fused (SuFu), a tumour suppressor mutated in medulloblastoma, is a central player of Hh signalling, a pathway crucial for development and deregulated in cancer.
Alfonsi, Romina, Bernardi, Flavia, Bufalieri, Francesca, Canettieri, Gianluca, Capalbo, Carlo, Coni, Sonia, De Smaele, Enrico, Di Marcotullio, Lucia, Faedda, Roberta, Ferretti, Elisabetta, Guardavaccaro, Daniele, Gulino, Alberto, Infante, Paola, Kool, Marcel, Lospinoso Severini, Ludovica, Maroder, Marella, Mazzà, Daniela, Mori, Mattia, Petroni, Marialaura, Pfister, Stefan M., Po, Agnese, Screpanti, Isabella, Siler, Mariangela   +22 more
core   +5 more sources

Preclinical models for evaluating psychedelics in the treatment of major depressive disorder

British Journal of Pharmacology, EarlyView.
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander, Dasha Anderson, Luke Baxter, Matthew Claydon, James Rucker, Emma S. J. Robinson   +5 more
wiley   +1 more source

Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists

British Journal of Pharmacology, EarlyView.
Psychedelic drugs such as LSD and psilocin were once relegated to the fringes of medical research because of their association with counterculture movements and a perceived concern about harm through recreational use, and their consequent legal prohibition in the early 1970s.
Trevor Sharp, Aurelija Ippolito
wiley   +1 more source

Pharmacogenetics of analgesic drugs [PDF]

, 2013
• Individual variability in pain perception and differences in the efficacy of analgesic drugs are complex phenomena and are partly genetically predetermined.
Branford, R, Cregg, R, Gubbay, A, Russo, G, Sato, H   +4 more
core   +1 more source

Evidence that 5‐HT2A receptor signalling efficacy and not biased agonism differentiates serotonergic psychedelic from non‐psychedelic drugs

British Journal of Pharmacology, EarlyView.
Background and Purpose Serotonergic psychedelic drugs are under investigation as therapies for various psychiatric disorders, including major depression. Although serotonergic psychedelic drugs are 5‐HT2A receptor agonists, some such agonists are not psychedelic, potentially due to differences in 5‐HT2A receptor ligand bias or signalling efficacy. Here,
Aurelija Ippolito, Sridhar Vasudevan, Shaun Hurley, Gary Gilmour, Frederick Westhorpe, Grant Churchill, Trevor Sharp   +6 more
wiley   +1 more source

Functional map of arrestin binding to phosphorylated opsin, with and without agonist [PDF]

, 2016
Arrestins desensitize G protein-coupled receptors (GPCRs) and act as mediators of signalling. Here we investigated the interactions of arrestin-1 with two functionally distinct forms of the dim-light photoreceptor rhodopsin.
Lally, Ciara C. M., Ostermaier, Martin K., Peterhans, Christian, Sommer, Martha E., Standfuss, Joerg   +4 more
core   +1 more source

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

British Journal of Pharmacology, EarlyView.
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi, Jamie Cowley, Ashley Pegg, Alison J. Cooper, John Gordon, Catherine A. Brady, Antonio Belli, Sam Butterworth, Rachel Upthegrove, Nick Andrews, Nicholas M. Barnes   +10 more
wiley   +1 more source