Results 201 to 210 of about 111,646 (306)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Unique Biology and Single-Channel Properties of GluN2A- and GluN2C-Containing Triheteromeric N-Methyl-D-Aspartate Receptors. [PDF]

J Exp Neurosci, 2018
Bhattacharya S, Traynelis SF.
europepmc   +1 more source

Muscarinic agonists for schizophrenia: Bridging preclinical evidence and clinical enthusiasm

British Journal of Pharmacology, EarlyView.
Abstract Antipsychotic drugs targeting dopamine receptors have been used to treat schizophrenia for decades, primarily alleviating positive symptoms such as hallucinations and delusions. However, they provide limited benefit for cognitive and negative symptoms—major contributors to poor outcomes—and are frequently associated with significant side ...
Brian J. Morris, Judith A. Pratt
wiley   +1 more source

N-Methyl-D-Aspartate Receptors: "C"ing the Culprits Behind Cocaine-Induced Metaplasticity. [PDF]

Biol Psychiatry, 2016
Wright WJ, Dong Y.
europepmc   +1 more source

Comprehensive in vitro profiling of traditional and emerging stimulants at monoamine transporters and the 5‐HT2A receptor

British Journal of Pharmacology, EarlyView.
A pharmacological profiling of 58 synthetic stimulants of various classes at dopamine, norepinephrine, and serotonin transporters and the 5‐HT2A receptor, most showing distinct class‐dependent profiles, with some indicating a high abuse potential. Background and Purpose New psychoactive substances (NPSs) often emerge on the illicit drug market with ...
Darta Stalberga, Robert Kronstrand, Bianca Schranz, Nick van Zijl, Sebastian Karlman, Soma Aref, Tobias Rautio, Svante Vikingsson, Mattias Persson, Henrik Green   +9 more
wiley   +1 more source

Multiple Mechanisms of Ketamine Blockade of N‐methyl‐D‐aspartate Receptors

Anesthesiology, 1997
B. Orser, P. Pennefather, J. Macdonald
semanticscholar   +1 more source

Adiponectin promotes AMPA receptor trafficking and enhances excitatory synaptic transmission at hippocampal synapses via AMP‐activated protein kinase signalling

British Journal of Pharmacology, EarlyView.
Background and Purpose Peripherally derived adiponectin crosses the blood–brain barrier and targets severa0l brain regions. Adiponectin receptors are highly expressed in the hippocampus, and play a pro‐cognitive role as adiponectin markedly influences the functioning of hippocampal synapses.
Alexandra Soca, Patricia Raposo Afonso, Valentin Morfin, James Cantley, Jenni Harvey   +4 more
wiley   +1 more source

Transcriptomic and metabolomic analyses reveal that lobeglitazone ameliorates hepatic steatosis in rats concurrent with regulation of mitochondrial pyruvate metabolism

British Journal of Pharmacology, EarlyView.
Background and Purpose Lobeglitazone is a thiazolidinedione and PPARγ agonist that improves metabolic parameters and hepatic steatosis, but its mechanisms are not fully understood. This study investigated the effects of lobeglitazone on hepatic transcriptomic and metabolic profiles in a rat model of obesity and Type 2 diabetes mellitus.
Hyekyung Yang, Su Young Son, Youngmi Song, Hyewon Choi, In‐Gu Do, Choong Hwan Lee, Cheol‐Young Park   +6 more
wiley   +1 more source

Glutamate Induces Blood-Brain Barrier Permeability through Activation of N-Methyl-D-Aspartate Receptors. [PDF]

J Neurosci, 2016
Xhima K, Weber-Adrian D, Silburt J.
europepmc   +1 more source