Results 211 to 220 of about 107,657 (326)

Is there a role for cannabidiol in obesity, metabolic syndrome and binge eating?

British Journal of Pharmacology, EarlyView.
Cannabidiol (CBD) is one of the most abundant phytocannabinoids isolated from the Cannabis sativa plant. CBD is a lipophilic, non‐intoxicating substance that differently from Δ9‐tetrahydrocannabinol (Δ9‐THC) does not present the typical profile of a drug of abuse.
Luca Botticelli, Emanuela Micioni Di Bonaventura, Giacomo Einaudi, Gustavo Provensi, Alessia Costa, Claudio D'Addario, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura   +7 more
wiley   +1 more source

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M₄ Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust <i>In Vivo</i> Efficacy. [PDF]

ACS Chem Neurosci
Gregro AR, Park C, Long MF, Baker LA, Bollinger KA, Ringuette AE, Peng L, Luscombe VB, Billard NB, Rodriguez AL, Niswender CM, Peng W, Dickerson JW, Rook JM, O'Neill J, Chang S, Boonen HCM, Jensen T, Thomsen MS, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ.   +24 more
europepmc   +1 more source

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Application of Deuterium in an M₁ Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422. [PDF]

ACS Chem Neurosci
Engers JL, Li J, Han C, Long MF, Gregro AR, Presley CC, Dickerson JW, Peng W, Cho HP, Rodriguez AL, Xiang Z, Boutaud O, O'Carroll C, Dey PM, Burstein ES, Niswender CM, Rook JM, Conn PJ, Engers DW, Lindsley CW.   +19 more
europepmc   +1 more source

The In Vivo Effects of the CB1-Positive Allosteric Modulator GAT229 on Intraocular Pressure in Ocular Normotensive and Hypertensive Mice

Journal of Ocular Pharmacology and Therapeutics, 2017
Elizabeth A Cairns, A. Szcześniak, A. Straiker, P. Kulkarni, R. Pertwee, G. Thakur, W. Baldridge, M. Kelly   +7 more
semanticscholar   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

A Positive Allosteric Modulator of the SERCA Pump Rescues Hippocampal Neuronal Circuits Dysfunction and Cognitive Defects in a Mouse Model of Alzheimer's Disease. [PDF]

J Neurosci
Gerasimov E, Rakovskaya A, Pchitskaya E, Vlasova O, Dahl R, Bezprozvanny I.   +5 more
europepmc   +1 more source

Therapeutic Advantage of the Positive Allosteric Modulators of the GABA-B Receptor [PDF]

ACS Medicinal Chemistry Letters, 2017
openaire   +2 more sources

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