Results 101 to 110 of about 687,004 (308)

Novel drugs approved by the EMA, the FDA and the MHRA in 2025: A year in review

British Journal of Pharmacology, EarlyView.
Abstract In the 2025 novel drug mini‐review, one can take a full measure of the ingenuity that underlies current drug design and development, despite the year's smaller harvest (46 novel drugs) compared to 2024 (53) and 2023 (70). 54% of the novel drugs are first‐in‐class (FIC).
Andreas Papapetropoulos, Stavros Topouzis, Steve P. H. Alexander, Miriam M. Cortese‐Krott, Zsuzsanna Helyes, Kirill Martemyanov, Claudio Mauro, Nithyanandan Nagercoil, Reynold A. Panettieri Jr, Hemal H. Patel, Rainer Schulz, Barbara Stefanska, Gary J. Stephens, Nathalie Vergnolle, Xin Wang, Stephen Ward, Péter Ferdinandy   +16 more
wiley   +1 more source

PHARMACOLOGICAL APPROACH IN EXERCISE-INDUCED ASTHMA [PDF]

Sport Mont, 2012
Exercise-induced asthma is a transient airflow obstruction, which occurs after the strenuous exercise. It is a complex pathophysiological phenomenon, present in all levels of exercise, from children to professional athletes, so the therapy is specific ...
Biljana Vitošević, Radoslav Mitić, Iva Nikolić   +2 more
doaj  

Quantitative surface field analysis: learning causal models to predict ligand binding affinity and pose. [PDF]

, 2018
We introduce the QuanSA method for inducing physically meaningful field-based models of ligand binding pockets based on structure-activity data alone. The method is closely related to the QMOD approach, substituting a learned scoring field for a pocket ...
Cleves, Ann E, Jain, Ajay N
core  

Insights into GABA receptor signalling in TM3 Leydig cells [PDF]

, 2005
gamma-Aminobutyric acid (GABA) is an emerging signalling molecule in endocrine organs, since it is produced by endocrine cells and acts via GABA(A) receptors in a paracrine/autocrine fashion.
Artur Mayerhofer, Behar TN, Ben Ari Y, Berman JA, Christof Geigerseder, Erdo SL, Frungieri MB, Fukura H, Gilon P, Haydar TF, Karl Föhr, Kriegstein AR, Lars Kunz, Lauder JM, Lee W, Leinekugel X, Malherbe P, Maric D, Mayerhofer A, Mayerhofer A, Mayerhofer A, Monica B. Frungieri, Owens DF, Owens DF, Ricardo S. Calandra, Richard F.G. Doepner, Ritta MN, Romi Raemsch, Silvia I. Gonzalez-Calvar   +28 more
core   +2 more sources

The amino terminal domain of the human α7 nicotinic acetylcholine receptor subunit leads to the functional expression of human/insect receptors

British Journal of Pharmacology, EarlyView.
Human α7 receptors have been characterised in terms of pharmacological properties. Insertion of the N‐terminal domain of the human α7 subunit leads to honeybee and cockroach chimeric receptors activated by ACh and inhibited by α‐Bgt. Insertion of the human cys‐loop leads to cockroach chimeric receptors modulated by PNU.
Alison Cartereau, Chloé Veront, Alexandra Cremades, Priscilla Martin, Remi Gojard, Nicolas Galland, Emiliane Taillebois, Dieudonnée Togbé, Jean‐Yves Le Questel, Steeve H. Thany   +9 more
wiley   +1 more source

Adreno-Muscarinic Synergy of Contractile Responses From Human Hyperplastic Prostate [PDF]

International Neurourology Journal
Purpose Adreno-muscarinic synergy, a supra-additional contractile response to simultaneous application of α-adrenoreceptor and muscarinic receptor agonists, is a feature of several lower urinary tract regions that have dual sympathetic and ...
Ben T. Blake-James, Basu Chakrabarty, Christopher H. Fry   +2 more
doaj   +1 more source

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]

, 2013
G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D., Milligan, Graeme, Ulven, Trond   +2 more
core   +1 more source

ADAM17 and its proteolytic targets in disease pathogenesis

The FEBS Journal, EarlyView.
ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
wiley   +1 more source

M2 Muscarinic acetylcholine receptor modulates rat airway smooth muscle cell proliferation

World Allergy Organization Journal, 2013
Airways chronic inflammatory conditions in asthma and COPD are characterized by tissue remodeling, being smooth muscle hyperplasia, the most important feature.
Fabiola A. Placeres-Uray, Christopher A. Febres-Aldana, Ruth Fernandez-Ruiz, Ramona Gonzalez de Alfonzo, Itala A. Lippo de Becemberg, Marcelo J. Alfonzo   +5 more
doaj   +1 more source

Induction of Anti-Hebbian LTP in CA1 Stratum Oriens Interneurons: Interactions between Group I Metabotropic Glutamate Receptors and M1 Muscarinic Receptors [PDF]

, 2015
An anti-Hebbian form of LTP is observed at excitatory synapses made with some hippocampal interneurons. LTP induction is facilitated when postsynaptic interneurons are hyperpolarized, presumably because Ca(2+) entry through Ca(2+)-permeable glutamate ...
Kullmann, DM, Le Duigou, C, Miles, R, Savary, E   +3 more
core   +1 more source