Results 1 to 10 of about 11,132 (239)

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 more
europepmc   +2 more sources

Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]

Med Res Rev
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A, Galli G, Dallanoce C, De Amici M, Gorostiza P, Matera C.   +5 more
europepmc   +2 more sources

Evaluation of the Alterations in Central Cholinergic Neurotransmission in Aging and Amyloid Precursor Protein Knock-In Mice. [PDF]

J Neurochem
In Alzheimer's disease, reduced release of ACh is linked more to Aβ pathology than to age‐related change, highlighting an early sign of disease. ABSTRACT A progressive decline in cognitive function occurs as a result of aging and Alzheimer's disease (AD) and is primarily associated with diminished cholinergic neurotransmission.
Nagai-Arakawa I, Muramatsu I, Uwada J, Tsuda Y, Tokunaga A, Irie A, Maeda H, Madokoro Y, Sato T, Uchida Y, Saito T, Saido TC, Sada K, Masuoka T, Matsukawa N.   +14 more
europepmc   +2 more sources

Novel Electroactive Therapeutic Platforms for Cardiac Arrhythmia Management

Advanced Science, EarlyView.
Electroactive platforms offer promising applications in cardiac arrhythmia. Based on their energy sources and mechanisms, electroactive platforms are categorized into i) direct electrical stimulation, ii) self‐powered electroactive systems, iii) physical stimuli‐mediated electroactive systems, and iv) conductive systems, and their applications in ...
Juwei Yang, Longfei Li, Yiran Hu, Zhou Li, Wei Hua   +4 more
wiley   +1 more source

Deciphering the skeletal interoceptive circuitry to control bone homeostasis

BMEMat, EarlyView.
This review introduces the skeletal interoceptive circuitry, covering the ascending signals from bone tissues to the brain (sensors), the central neural circuits that integrate this information and dispatch commands (CPU), and the descending pathways that regulate bone homeostasis (effectors).
Yefeng Wu, Jiusi Guo, Zhen Chen, Fengwei Zhang, Billy Kwok Chong Chow, Zhuofan Chen, Kelvin Wai‐Kwok Yeung, Wei Qiao   +7 more
wiley   +1 more source

Benzochalcogenodiazoles, Synthesis, and Applications in Medicinal Chemistry and Photomedicine

European Journal of Organic Chemistry, EarlyView.
Benzochalcogenodiazoles (BXD) including benzoxadiazoles, benzothiadiazoles, and benzoselenadiazoles are initially mainly designed for optoelectronic materials as electron‐deficient cores. Nevertheless, they are now extending their application to biology.
Jean‐Elie Zheng, Xavier Franck, Thibault Gallavardin   +2 more
wiley   +1 more source

β3‐Adrenoceptor Agonist Effects on the Urinary Bladder Beyond Detrusor Relaxation

Neurourology and Urodynamics, EarlyView.
ABSTRACT Aims β3‐Adrenoceptor agonists such as mirabegron or vibegron reach pharmacokinetic steady‐state within a few days. However, maximum improvements in symptoms of the overactive bladder syndrome are reached at time points later than 4 weeks, that is, detrusor smooth muscle relaxation cannot fully explain clinical effects.
Martin C. Michel, Ebru Arioglu‐Inan, Martin Hennenberg   +2 more
wiley   +1 more source

Arrestin‐centred interactions at the membrane and their conformational determinants

British Journal of Pharmacology, EarlyView.
Abstract More than 30 years after their discovery, arrestins are recognised multiprotein scaffolds that play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling. Originally named for their capacity to hinder GPCR coupling to G proteins and facilitate receptor desensitisation, arrestins have emerged as key hubs for a myriad of
Owen Underwood, Raphael Silvanus Haider, Julie Sanchez, Meritxell Canals   +3 more
wiley   +1 more source

G protein‐coupled receptor‐mediated autophagy in health and disease

British Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan, Zeynep Aslıhan Durer, Beki Kan   +2 more
wiley   +1 more source

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

British Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman, Ana‐Nicoleta Bondar, Julie Dam, Zafiroula Georgoussi, Jesús Giraldo, Anemari Horvat, Christos Karoussiotis, Alba Paz‐Castro, Miriam Scarpa, Hannes Schihada, Nicole Scholz, Bilge Güvenc Tuna, Nina Vardjan   +15 more
wiley   +1 more source