Results 61 to 70 of about 29,139 (279)

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

Pharmacological Characterization of Itch-Associated Response Induced by Repeated Application of Oxazolone in Mice

Journal of Pharmacological Sciences, 2010
We investigated pharmacological characteristics of the itch-associated response to chronic dermatitis induced by 4-ethoxymethylene-2-phenyl-2-oxazolin-5-one (oxazolone) repeated application in mice.
Yukihito Tsukumo, Daisuke Harada, Haruhiko Manabe   +2 more
doaj  

Pro-inflammatory mechanisms of muscarinic receptor stimulation in airway smooth muscle

Respiratory Research, 2010
Background Acetylcholine, the primary parasympathetic neurotransmitter in the airways, plays an important role in bronchoconstriction and mucus production.
Zuyderduyn Suzanne, Hiemstra Pieter S, Rieks Daniëlle, Nanninga Janke E, Kolahian Saeed, Oenema Tjitske A, Halayko Andrew J, Meurs Herman, Gosens Reinoud   +8 more
doaj   +1 more source

PET mapping of receptor occupancy using joint direct parametric reconstruction [PDF]

Receptor occupancy (RO) studies using PET neuroimaging play a critical role in the development of drugs targeting the central nervous system (CNS). The conventional approach to estimate drug receptor occupancy consists in estimation of binding potential changes between two PET scans (baseline and post-drug injection).
arxiv   +1 more source

Identification of a Family of Muscarinic Acetylcholine Receptor Genes [PDF]

Science, 1987
Complementary DNAs for three different muscarinic acetylcholine receptors were isolated from a rat cerebral cortex library, and the cloned receptors were expressed in mammalian cells. Analysis of human and rat genomic clones indicates that there are at least four functional muscarinic receptor genes and that these genes lack introns in the coding ...
Bonner, T., Buckley, N., Young, A., Brann, M.   +3 more
openaire   +4 more sources

Investigation of Thiazolidine‐2,4‐Dione Derivatives as Acetylcholinesterase Inhibitors: Synthesis, In Vitro Biological Activities and In Silico Studies

ChemistryOpen, EarlyView.
Thiazolidin‐2,4‐dion derivatives were synthesized and evaluated for drug‐likeness, BBB permeability, and ADMET properties. Docking studies revealed that all derivatives (CHT1‐5) had good AChE inhibition, although CHT1 was the most effective and showed strong antioxidant activity in vitro.
Hanane Naeimi, Maryam Taheri, Hossein Ghafouri, Asadollah Mohammadi   +3 more
wiley   +1 more source

Cholesterol modulates acetylcholine receptor diffusion by tuning confinement sojourns and nanocluster stability [PDF]

arXiv, 2017
Translational motion of neurotransmitter receptors is key for determining receptor number at the synapse and hence, synaptic efficacy. We combine live-cell STORM superresolution microscopy of nicotinic acetylcholine receptor (nAChR) with single-particle tracking, mean-squared displacement (MSD), turning angle, ergodicity, and clustering analyses to ...
arxiv  

Acetylcholine-induced inhibition of presynaptic calcium signals and transmitter release in the frog neuromuscular junction

Frontiers in Physiology, 2016
Acetylcholine (ACh), released from axonal terminals of motor neurones in neuromuscular junctions regulates the efficacy of neurotransmission through activation of presynaptic nicotinic and muscarinic autoreceptors.
Eduard Khaziev, Eduard Khaziev, Eduard Khaziev, Dmitry Samigullin, Dmitry Samigullin, Dmitry Samigullin, Nikita Zhilyakov, Nikita Zhilyakov, Nijaz Fatikhov, Ellya Bukharaeva, Ellya Bukharaeva, Alexej Verkhratsky, Evgeny Nikolsky, Evgeny Nikolsky, Evgeny Nikolsky   +14 more
doaj   +1 more source

DREADDs‐Based Chemogenetics Induced Slow Transit Constipation via Inhibition of Enteric Neurons

Journal of Digestive Diseases, EarlyView.
Designer receptors exclusively activated by designer drugs (DREADDs)‐based chemogenetic tools were used to induce murine model of slow transit constipation. Adeno‐associated virus (AAV) 9‐hM4Di or normal saline (control) was injected into six sites spread out over the whole colon of mice, and the indicators of colonic motility were evaluated after ...
Xin Yi Lu, Yu Xiang Wen, Ni Jiang, Si Qi Zhou, Tian Yang, Liang Liang Shi, Hui Min Guo, Wei Zhang, Qi Peng Zhang, Ni Na Zhang   +9 more
wiley   +1 more source

Basic and Clinical Aspects of Non-neuronal Acetylcholine: Expression of Non-neuronal Acetylcholine in Lung Cancer Provides a New Target for Cancer

Journal of Pharmacological Sciences, 2008
Lung cancer is the leading cause of cancer death worldwide and new treatment strategies are clearly needed. The recent discovery that lung and other cancers synthesize and secrete acetylcholine (ACh) which acts as an autocrine growth factor suggests that
Therapy Pingfang Song, Eliot R. Spindel
doaj