Results 101 to 110 of about 19,182 (246)

Simultaneous Modeling of In Vivo and In Vitro Effects of Nondepolarizing Neuromuscular Blocking Drugs [PDF]

arXiv, 2023
Nondepolarizing neuromuscular blocking drugs (NDNBs) are clinically used to produce muscle relaxation during general anesthesia. This paper explores a suitable model structure to simultaneously describe in vivo and in vitro effects of three clinically used NDNBs, cisatracurium, vecuronium, and rocuronium. In particular, it is discussed how to reconcile
arxiv  

Red-emitting dibenzodiazepinone derivatives as fluorescent dualsteric probes for the muscarinic acetylcholine M2 receptor.

Journal of Medicinal Chemistry, 2020
Fluorescently labeled dibenzodiazepinone-type muscarinic acetylcholine receptor (MR) antagonists, including dimeric ligands, were prepared using red-emitting cyanine dyes.
Xueke She, Andrea Pegoli, Corinna G Gruber, David Wifling, J. Carpenter, H. Hübner, Meng-Tsz Chen, Jianfei Wan, G. Bernhardt, P. Gmeiner, N. Holliday, M. Keller   +11 more
semanticscholar   +1 more source

Hippocampal Inhibitory Interneuron‐Specific DREADDs Treatment Alters mTORC1‐4E‐BP Signaling and Impairs Memory Formation

Journal of Neurochemistry, Volume 169, Issue 3, March 2025.
We used advanced tools called DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) to control the activity of inhibitory neurons versus excitatory neurons in the hippocampus, a region of the brain critical for learning and memory. By activating or inactivating these neurons after training, we found that disrupting their normal activity ...
Ziying Huang, Niaz Mahmood, Jean‐Claude Lacaille, Shane Wiebe, Nahum Sonenberg   +4 more
wiley   +1 more source

Calcium Mobilization by Activation of M3/M5 Muscarinic Receptors in the Human Retinoblastoma

Journal of Pharmacological Sciences, 2007
Activation of muscarinic acetylcholine receptors (mAChR) is one of the most important signal transduction pathways in the human body. In this study, we investigated the role of mAChR activation in relation to its subtypes in human retinoblastoma cell ...
Dae-Ran Kim, Sang Hoon Rah, Joon Hyung Sohn, Byung-Il Yeh, Chang Mann Ko, Jeong Sook Park, Min-Jeong Kim, Joong Woo Lee, In Deok Kong   +8 more
doaj  

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

Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]

, 2007
Muscarinic acetylcholine receptors (mAChRs) are prototypical Family A G protein coupled-receptors. The five mAChR subtypes are widespread throughout the periphery and the central nervous system and, accordingly, are widely involved in a variety of both ...
Christopoulos, Arthur, Gregory, Karen J, Sexton, Patrick M   +2 more
core   +2 more sources

Muscarinic receptor blockade with oxybutynin reduces spontaneous and induced uterine muscle contractions

Pregnancy, Volume 1, Issue 1, January 2025.
Abstract Objective The uterus and the bladder have striking physiologic and anatomic similarities. Anticholinergic medications are commonly used to treat “overactive bladder” by targeting M2 and M3 muscarinic receptors. The uterus also contains M2 and M3 muscarinic receptors; however, current management of preterm labor does not target these receptors.
Anthony G. Visco, Zachary R. Visco, Chad A. Grotegut, Cristina Linde, Timothy Westfall, Friederike L. Jayes   +5 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  

Anticholinergic drugs and dementia risk: Using stem cell–based studies to complement pharmacoepidemiology

Alzheimer's &Dementia: Translational Research &Clinical Interventions, Volume 11, Issue 1, January-March 2025.
Abstract BACKGROUND Anticholinergic (AC) use remains common in older adults despite evidence of safety risks, including increased risk in dementia. Pharmacoepidemiology studies from various populations report associations between specific anticholinergic classes – antidepressants and bladder antimuscarinics – and increased dementia incidence.
Tiara A. Schwarze‐Taufiq, Inez K. A. Pranoto, Katherine Hui, Chizuru Kinoshita, Onchee Yu, Paul K. Crane, Shelly L. Gray, Jessica E. Young   +7 more
wiley   +1 more source

In vitro and in vivo study of butyrylfentanyl and 4‐fluorobutyrylfentanyl in female and male mice: Role of the CRF1 receptor in cardiorespiratory impairment

British Journal of Pharmacology, Volume 182, Issue 1, Page 104-130, January 2025.
Abstract Background and Purpose Fentanyl analogues have been implicated in many cases of intoxication and death with overdose worldwide. The aim of this study is to investigate the pharmaco‐toxicology of two fentanyl analogues: butyrylfentanyl (BUF) and 4‐fluorobutyrylfentanyl (4F‐BUF).
Sabrine Bilel, Joaquim Azevedo Neto, Micaela Tirri, Giorgia Corli, Marta Bassi, Anna Fantinati, Giovanni Serpelloni, Davide Malfacini, Claudio Trapella, Girolamo Calo', Matteo Marti   +10 more
wiley   +1 more source