Results 101 to 110 of about 11,641 (225)

G protein stoichiometry dictates biased agonism through distinct receptor-G protein partitioning

Scientific Reports, 2017
Biased agonism at G protein coupled receptors emerges as an opportunity for development of drugs with enhanced benefit/risk balance making biased ligand identification a priority.
Lauriane Onfroy, Ségolène Galandrin, Stéphanie M. Pontier, Marie-Hélène Seguelas, Du N’Guyen, Jean-Michel Sénard, Céline Galés   +6 more
doaj   +1 more source

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  

Novel mechanisms of G-protein-coupled receptors functions: AT1 angiotensin receptor acts as a signaling hub and focal point of receptor cross-talk [PDF]

, 2018
AT1 angiotensin receptor (AT1R), a prototypical G protein-coupled receptor (GPCR), is the main receptor, which mediates the effects of the renin-angiotensin system (RAS).
Balla, András, Hunyady, László, Turu, Gábor, Tóth, András D.   +3 more
core   +1 more source

Safety pharmacology of acute mescaline administration in healthy participants

British Journal of Clinical Pharmacology, EarlyView.
Aims Psychedelics, including mescaline, may serve as novel treatments for depression and anxiety. However, data is scarce on the safety of mescaline. Methods The present pooled analysis included two double‐blind, randomized, placebo‐controlled studies with a total of 48 participants and 96 mescaline administrations. Single oral‐dose administrations (n =
Aaron Klaiber, Mélusine Humbert‐Droz, Laura Ley, Yasmin Schmid, Matthias E. Liechti   +4 more
wiley   +1 more source

Cytoprotective Activated Protein C Averts Nlrp3 Inflammasome–Induced Ischemia-Reperfusion Injury Via Mtorc1 Inhibition [PDF]

, 2017
Cytoprotection by activated protein C (aPC) after ischemia-reperfusion injury (IRI) is associated with apoptosis inhibition. However, IRI is hallmarked by inflammation, and hence, cell-death forms disjunct from immunologically silent apoptosis are, in ...
Al-Dabet, Moh\u27d Mohanad, Bock, Fabian, Braun-Dullaeus, Ruediger C., Camerer, Eric, Dockendorff, Chris, Elwakiel, Ahmed, Esmon, Charles T., Gadi, Ihsan, Ghosh, Sanchita, Griffin, John H., Huber, Tobias B., Isermann, Berend, Kohli, Shrey, Manoharan, Jayakumar, Nazir, Sumra, Ranjan, Satish, Shahzad, Khurrum   +16 more
core   +2 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

‘O sibling, where art thou?’ – a review of avian sibling recognition with respect to the mammalian literature [PDF]

, 2004
Avian literature on sibling recognition is rare compared to that developed by mammalian researchers. We compare avian and mammalian research on sibling recognition to identify why avian work is rare, how approaches differ and what avian and mammalian ...
Barnard C. J., Barnard C.J., Barnard C.J., Bateson P., Bateson P., Beecher I. M., Blaustein A. R., Boyse E. A., Brown J. L., Burger J., Byers J. A., Catchpole C. K., Colgan P., Cramp S., Cramp S., Davis L. S., Dawkins R., Dewsbury D. A., Evans R. M., Farabaugh S. M., Ferkin M. H., Fletcher D. J. C., Fletcher D.J. C., Fuller C. A., Gamboa G. J., Gottlieb G., Halpin Z. T., Hamilton W. D., Hare J. F., Hare J. F., Hepper P. G., Hepper P. G., Hepper P. G., Hoglund J., Holmes W. G., Holmes W. G., Holmes W. G., Johnsgard P. A., Johnsgard P. A., Kroodsma D. E., Lenington S., McGregor P. K., McShea W. J., Medvin M. B., Miller D. E., Mock D. W., Murie J. O., Nowak R. M., Palestis B. G., Palestis B. G., Pfennig D. W., Pierotti R., Porter R. H., Porter R. H., Porter R. H., Radesater T., Schimmel L., Schubert C. A., Sherman P. W., Sherman P. W., Shields W. M., Shields W. M., Slater P.J. B., Stacey P. B., Stoddard P. K., Trainer J. M., Waldman B., Wilson E. O., Wilson E. O., Zann R. A.   +69 more
core   +2 more sources

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

Endogenous lysophosphatidic acid (LPA1) receptor agonists demonstrate ligand bias between calcium and ERK signalling pathways in human lung fibroblasts [PDF]

, 2016
Background and Purpose Human lung fibroblasts (HLF) express high levels of the LPA1 receptor, a GPCR that responds to the endogenous lipid mediator, lysophosphatidic acid (LPA).
Dowling, Mark R,, Rosethorne, Elizabeth M., Sattikar, Afrah   +2 more
core   +2 more sources

Psychedelics, entactogens and psychoplastogens for depression and related disorders

British Journal of Pharmacology, EarlyView.
Currently, the most actively investigated rapidly acting antidepressants, anxiolytics and/or anti PTSD agents, include psychedelics e.g. psilocybin, LSD, N,N‐dimethyltryptamine, ayahuasca; non‐hallucinogenic entactogens, e.g. MDMA; psychoplastogens which rapidly promote neuroplasticity, e.g.
Daniel Hoyer
wiley   +1 more source