Results 71 to 80 of about 57,597 (217)

In silico prediction of novel effective combinational treatment of chronic pain in individual patients: A joint white paper of the H2020 QSPainRelief consortium

British Journal of Pharmacology, EarlyView.
Abstract Opioids are prescribed widely for chronic pain despite well‐recognised risks and variable long‐term benefit, reflecting the lack of effective alternatives for many patients. Combination therapies offer a promising strategy to enhance efficacy whilst reducing side effects.
André Mouraux, Solenn Gousset, Beltrán Alvarez, Monica Baiula, Wouter Bakker, Andrea Bedini, Monir Bertayli, Divakar Budda, Robert Carr, Elisabetta Cuna, Óscar Díaz, Nina Donner, Jesús Giraldo, Geert‐Jan Groeneveld, Berfin Gülave, David Guydan, Hemme Hijma, Rafael Maldonado, Pedro Renault, Carlos Rinaudo, Jeroen Elaissaiss‐Schaap, Athan Spiros, Sara Stoeber, Petri Takkala, Daan van Valkengoed, Coen van Hasselt, Elizabeth (Liesbeth) CM de Lange   +26 more
wiley   +1 more source

Functional screen for subtype specificity of voltage sensor–targeted Kv7 potentiators

British Journal of Pharmacology, EarlyView.
Background and Purpose Voltage‐gated Kv7 (potassium channel subfamily Q [KCNQ]) potassium channels are powerful modulators of neuronal excitability. ICA‐069673 is a N‐aryl benzamide drug that targets the voltage‐sensing domain (VSD) of Kv7.2 with strong selectivity over Kv7.3 or Kv7.5, but the molecular basis of this selectivity remains poorly ...
Richard Kanyo, Thomas M. Hammond, Alice W. Wang, Caroline K. Wang, Varun Aggarwal, Shawn M. Lamothe, Harley T. Kurata   +6 more
wiley   +1 more source

AMPK‐mediated prevention of vascular dysfunction with metformin: Experimental and population‐based evidence

British Journal of Pharmacology, EarlyView.
Angiotensin II induces vascular inflammation, senescence, extracellular matrix (ECM) degradation and endothelial dysfunction, thus impairing SK+/IK+ channel function and reducing endothelial‐dependent hyperpolarisation (EDH). Metformin activates AMPK, increasing SK+/IK+ channel function and restoring vasorelaxation.
Soroush Mohammadi Jouabadi, Annika A. Jüttner, Annique Claringbould, Rene de Vries, Ingrid M. Garrelds, Usha Musterd‐Bhaggoe, Bruno H. Stricker, Maryam Kavousi, A. H. Jan Danser, Fariba Ahmadizar, Anton J. M. Roks   +10 more
wiley   +1 more source

Selective M3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model

Journal of Pharmacological Sciences, 2011
.: In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). Alteration of tumor growth
Nozomi Ami, Kazumi Koga, Hiroshi Fushiki, Yoko Ueno, Yoshio Ogino, Hisashi Ohta   +5 more
doaj   +1 more source

The discovery and development of ensifentrine: A novel inhaled dual PDE3/4 inhibitor having ‘bifunctional’ bronchodilator and anti‐inflammatory activity

British Journal of Pharmacology, EarlyView.
Abstract Ensifentrine (formerly called RPL 554) is a novel, first in class, inhaled bifunctional dual PDE3/4 inhibitor for the treatment of chronic respiratory diseases. Ensifentrine exhibits both bronchodilation via PDE3 inhibition and anti‐inflammatory activity via PDE4 inhibition.
Clive Page
wiley   +1 more source

Cholinergic Regulation of Orexin/Hypocretin Neurons Through M3Muscarinic Receptor in Mice

Journal of Pharmacological Sciences, 2008
The cholinergic system plays an important role in regulation of arousal and REM sleep. In the present study, we showed that a muscarinic receptor agonist, carbachol (CCh), activates almost 20% of orexin-producing neurons (orexin neurons), which play a ...
Kousaku Ohno, Mari Hondo, Takeshi Sakurai   +2 more
doaj   +1 more source

Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Muscarinic acetylcholine receptors are key therapeutic targets, and ligands engaging both orthosteric and allosteric sites may offer improved selectivity and efficacy. Here, we investigated whether the muscarinic antagonist KH‐5 acts as a dualsteric antagonist and defined its mode of interaction with muscarinic receptors.
Alena Janoušková‐Randáková, Eva Dolejší, Nikolai Chetverikov, Jan Jakubík   +3 more
wiley   +1 more source

Expression of Muscarinic Receptors and the Effect of Tiotropium Bromide in Aged Mouse Model of Chronic Asthma

Tuberculosis and Respiratory Diseases, 2019
Background Efficacy and safety of tiotropium bromide, a muscarinic receptor antagonist, in treatment of asthma have been reported. However, its effect on airway remodeling in chronic asthma of the elderly has not been clearly verified.
Ji Young Kang, M.D., Ph.D., In Kyoung Kim, Ph.D., Jung Hur, Ph.D., Seok Chan Kim, M.D., Ph.D., Sook Young Lee, M.D., Ph.D., Soon Seog Kwon, M.D., Ph.D., Young Kyoon Kim, M.D., Ph.D.   +6 more
doaj  

Possible involvement of acetylcholine-mediated inflammation in airway diseases

Allergology International, 2018
Inhaled bronchodilator treatment with a long acting muscarinic antagonist (LAMA) reduces symptoms and the risk of exacerbations in COPD and asthma. However, increasing evidence from cell culture and animal studies suggests that anti-muscarinic drugs ...
Akira Koarai, Masakazu Ichinose
doaj   +1 more source

Serotonin engages divergent 5‐HT receptor pathways for cell type‐resolved modulation of prefrontal layer 5 microcircuits

British Journal of Pharmacology, EarlyView.
Serotonin differentially modulates layer 5 mPFC microcircuits through cell type‐specific pre‐ and postsynaptic receptor pathways. Presynaptic 5‐HT1BRs suppress glutamate and GABA release, whereas presynaptic and postsynaptic 5‐HT3ARs enhance fast‐spiking interneuron activity, whilst distinct pyramidal neuron subtypes exhibit divergent 5‐HT1AR‐ and 5 ...
Ramya Rama, Guanxiao Qi, Gabriele Radnikow, Danqing Yang, Dirk Feldmeyer   +4 more
wiley   +1 more source