Results 81 to 90 of about 11,641 (225)

The Serotonin 2B (5‐HT2B) Receptor: A Narrative Review of Preclinical and Clinical Evidence on the Safety Considerations and Therapeutic Potential for the Treatment of Depression

Clinical Pharmacology &Therapeutics, EarlyView.
Major depressive disorder (MDD) and treatment‐resistant depression (TRD) remain leading causes of disability, providing the impetus for receptor‐level treatment strategies beyond monoamine reuptake. The serotonin 5‐HT2B receptor (5‐HT2BR) is uniquely positioned at the interface of central‐antidepressant mechanisms and peripheral cardiac risks.
Gia Han Le, Sabrina Wong, Danica E. Johnson, Diana K. Orsini, Yang Jing Zheng, Kayla M. Teopiz, Christine E. Dri, Joshua D. Rosenblat, Roger S. McIntyre   +8 more
wiley   +1 more source

A GLP-1 analogue optimized for cAMP-biased signaling improves weight loss in obese mice

Molecular Metabolism
Objective: Glucagon-like peptide 1 (GLP-1) receptor (GLP-1R) agonism is foundational to modern obesity pharmacotherapies. These compounds were engineered for maximal G protein alpha(s) (Gsα) signaling potency and downstream cAMP production. However, this
Jonathan D. Douros, Aaron Novikoff, Barent DuBois, Rebecca Rohlfs, Jacek Mokrosinski, Wouter F.J. Hogendorf, Robert Augustin, Myrte Merkestein, Lene Brandt Egaa Martini, Lars Linderoth, Elliot Gerrard, Janos Tibor Kodra, Jenny Norlin, Nikolaj Kulahin Roed, Anouk Oldenburger, Stephanie A. Mowery, Maria Waldhoer, Diego Perez-Tilve, Brian Finan, Steffen Reedtz-Runge, Timo D. Müller, Patrick J. Knerr   +21 more
doaj   +1 more source

Structural basis for GPR40 allosteric agonism and incretin stimulation

Nature Communications, 2018
GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of human GPR40 with an agonist bound to an allosteric site located near the lipid-rich region ...
Joseph D. Ho, Betty Chau, Logan Rodgers, Frances Lu, Kelly L. Wilbur, Keith A. Otto, Yanyun Chen, Min Song, Jonathan P. Riley, Hsiu-Chiung Yang, Nichole A. Reynolds, Steven D. Kahl, Anjana Patel Lewis, Christopher Groshong, Russell E. Madsen, Kris Conners, Jayana P. Lineswala, Tarun Gheyi, Melbert-Brian Decipulo Saflor, Matthew R. Lee, Jordi Benach, Kenton A. Baker, Chahrzad Montrose-Rafizadeh, Michael J. Genin, Anne R. Miller, Chafiq Hamdouchi   +25 more
doaj   +1 more source

An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse effects

Pharmacological Research, 2022
Kappa opioid receptor (κOR) agonists lack the abuse liability and respiratory depression effects of clinically used mu opioid receptor (μOR) analgesics and are hypothesized to be safer alternatives.
Alexander R. French, Richard M. van Rijn
doaj   +1 more source

The Pathogenic TSH β-Subunit Variant C105Vfs114X Causes a Modified Signaling Profile at TSHR [PDF]

, 2019
1) Background: Central congenital hypothyroidism (CCH) is a rare endocrine disorder that can be caused by mutations in the β-subunit of thyrotropin (TSHB).
Biebermann, Heike, Grüters-Kieslich, Annette, Kalveram, Laura, Kleinau, Gunnar, Rivero-Müller, Adolfo, Scheerer, Patrick, Szymańska, Kamila   +6 more
core   +1 more source

Resveratrol Ameliorates Allergic Rhinitis by Activating SIRT1 to Disrupt the Mitochondrial ROS‐Inflammation Vicious Cycle

Flavour and Fragrance Journal, EarlyView.
This study demonstrates that resveratrol alleviates allergic rhinitis by activating SIRT1, thereby disrupting the mitochondrial ROS‐inflammatory cycle, improving mitochondrial function, promoting anti‐inflammatory M2 macrophage polarisation, and reducing epithelial oxidative damage.
Xinyu Zhou, Yi Yue, Wenwen Qi, Wenqing Zhu, Xinran Liu, Rongcui Sui, Xuanchen Zhou   +6 more
wiley   +1 more source

Desensitization of cAMP Accumulation via Human β3-Adrenoceptors Expressed in Human Embryonic Kidney Cells by Full, Partial, and Biased Agonists

Frontiers in Pharmacology, 2019
β3-Adrenoceptors couple not only to cAMP formation but, at least in some cell types, also to alternative signaling pathways such as phosphorylation of extracellular signal-regulated kinase (ERK). β3-Adrenoceptor agonists are used in long-term symptomatic
Katerina Okeke, Katerina Okeke, Martina B. Michel-Reher, Stavros Gravas, Martin C. Michel   +4 more
doaj   +1 more source

Retrospective analysis reveals significant association of hypoglycemia with tramadol and methadone in contrast to other opioids. [PDF]

, 2019
Tramadol is one of the most commonly used analgesics worldwide, classified as having a low abuse potential by U.S. Drug Enforcement Agency, and often recommended in pain management guidelines.
Abagyan, Ruben, Atayee, Rabia S, Makunts, Tigran, U, Andrew   +3 more
core   +1 more source

Complex Pharmacology of Free Fatty Acid Receptors [PDF]

, 2017
G protein-coupled receptors (GPCRs) are historically the most successful family of drug targets. In recent times it has become clear that the pharmacology of these receptors is far more complex than previously imagined.
Bharat Shimpukade, Brian D. Hudson, Carpentier Y. A., Graeme Milligan, Kalliomaki M., Liu D., Lutz M., Tazoe H., Trond Ulven, Yousefi S., Zhu Y.   +10 more
core   +3 more sources

Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit beta-Arrestin-2. [PDF]

, 2016
Natural products found in Mitragyna speciosa, commonly known as kratom, represent diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing opportunities to better understand opioid pharmacology.
Borics, Attila, Marrone, Gina F., Narayan, Ankita, Palmer, Travis C., Szabó, Márton Richárd, Váradi, András   +5 more
core   +1 more source