Results 101 to 110 of about 8,155 (246)

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

Thermodynamic characterisation of covalent ligand binding

British Journal of Pharmacology, EarlyView.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman, Maayan Lavie, Almog Nadir, Ronen Gabizon, Nir London   +4 more
wiley   +1 more source

Rosemary metabolite carnosic acid opens Kv1.1 via its voltage sensor and corrects Kv1.1‐linked episodic ataxia in mice

British Journal of Pharmacology, EarlyView.
Background and Purpose Episodic ataxia type 1 (EA1) is an autosomal dominant neurological disorder caused primarily by loss‐of‐function mutations in the voltage‐gated potassium channel Kv1.1 (KCNA1). Small molecules that restore Kv1.1 activity hold promise as targeted therapies for EA1, yet current pharmacological strategies remain limited ...
Rían W. Manville, Ryan F. Yoshimura, Hanh A. Nguyen, Ruiming Zhao, Derk J. Hogenkamp, Steve A. N. Goldstein, Geoffrey W. Abbott   +6 more
wiley   +1 more source

Therapeutic potential of a Bax inhibitor‐1/TMBIM6 antagonist (BIA) and its analogues in Aspergillus fumigatus‐induced asthma via dual targeting of AKT and epithelial‐derived inflammatory cytokines

British Journal of Pharmacology, EarlyView.
Background and Purpose Aspergillus fumigatus (A. fumigatus) exposure causes of severe allergic asthma, characterized by airway inflammation and epithelial dysfunction. TMBIM6 (Bax inhibitor‐1) has been implicated in airway epithelial stress responses and AKT signalling.
Young‐Jin Yu, Ahsan Ullah, Jisun Kim, Mehedi Hasan Bappi, Yerim Heo, Jin Hee Ahn, Hyun‐Kyoung Kim, Han‐Jung Chae   +7 more
wiley   +1 more source

Honokiol regulates Acute respiratory distress syndrome (ARDS)‐associated pulmonary fibrosis via the miR‐19a‐3p/POSTN axis

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Acute respiratory distress syndrome (ARDS) and subsequent pulmonary fibrosis are associated with high mortality and limited treatment options. Periostin (POSTN) is a profibrotic mediator predicted to be regulated by microRNA‐19a‐3p (miR‐19a‐3p), but the relevance of this axis in ARDS‐associated pulmonary fibrosis remains
Weilun Liu, Hsiaohsuan Wang, Hsuanfu Kuo, Chiahung Yen, Modasang Hua, Chiayuan Chang, Zhiwei Xu, Ifan Liu, Chongchao Hsieh, Chihhsin Hsu, Chiayang Li, Shuchi Wang, Yunghsiang Chen, Menghsuan Cheng, Polen Liu   +14 more
wiley   +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

GMP‐compliant production, validation and dosimetry of clinical grade [18F]3‐(3‐fluoropropyl)‐2‐phenyl‐2,3‐dihydrobenzo[d]thiazole ([18F]FPBT) for oxidative stress PET imaging

British Journal of Pharmacology, EarlyView.
Background and Purpose Oxidative stress plays a critical role in the pathophysiology of various diseases, yet current methods for its non‐invasive detection remain limited. This study aimed to systematically validate a superoxide‐selective PET tracer, [18F]FPBT, for the early diagnosis and therapeutic monitoring of oxidative stress‐related conditions ...
Hua Zhang, Fangfang Sun, Chun Li, Xin Wang, Yuexuan Song, Lu Jiang, Paul Gape, Samantha Y. A. Terry, Shujun He, Ran Yan, Zhi Lu   +10 more
wiley   +1 more source

Subregion‐specific perineuronal net remodelling in the dorsal hippocampus drives vulnerability and resilience to chronic stress: The role of venlafaxine treatment

British Journal of Pharmacology, EarlyView.
Background and Purpose Neuronal plasticity enables the brain to adapt to internal and external demands by dynamically regulating synaptic connectivity and emotional circuitry. Impaired neuroplasticity represents a core pathophysiological framework of major depressive disorder, one of the leading causes of disability worldwide. Chronic stress is a major
Paola Brivio, Arianna Palumbo, Maria Teresa Gallo, Filippo Umberto Tancredi Veronesi, Giorgia Cortinovis, Piotr Gruca, Magdalena Lason, Ewa Litwa, Dominika Biala, Fabio Fumagalli, Mariusz Papp, Francesca Calabrese   +11 more
wiley   +1 more source

Intermittent cocaine use patterns, not total intake, predict cue‐induced drug seeking in rats

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Cocaine‐associated cues trigger relapse to drug use in humans and animal models. In rats, long daily cocaine access (4–6 vs. 1–2 h) increases drug self‐administration and cue‐induced cocaine seeking, suggesting that greater intake promotes relapse.
Amélie Mainville‐Berthiaume, Hajer Algallal, Salomé Dupuis, Sema Abu Shamleh, Coralie Godbout, Vincent Jacquemet, Anne‐Noël Samaha   +6 more
wiley   +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