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https://www.readbyqxmd.com/read/28343895/pharmacokinetic-profile-of-promising-acetylcholinesterase-reactivators-k027-and-k203-in-experimental-pigs
#1
Jana Zdarova Karasova, Jaroslav Kvetina, Ilja Tacheci, Vera Radochova, Kamil Musilek, Kamil Kuca, Jan Bures
Standard treatment of organophosphorus compounds (OPs) poisoning includes administration of an anti-muscarinic (atropine), anticonvulsive (diazepam) and acetylcholinesterase reactivator (oxime). From a wide group of newly synthesized oximes, oxime K027 and oxime K203 seem to be perspective compounds in some specific OPs intoxication. The available in vitro and in vivo preclinical data indicate that both oximes may be considered for potential human use. The main aim of this study was to established plasmatic concentration curves of both oximes after intramuscular (i...
March 23, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28342980/muscarinic-receptor-mediated-signaling-pathways-in-hepatocytes-from-ccl4-induced-liver-fibrotic-rat
#2
Lin Luo, Chenghao Xi, Tingting Xu, Gaoshan Zhang, E Qun, Wei Zhang
The pathological changes of parasympathetic nerves are considered as an independent prognostic factor of the survival rate for patients with chronic liver disease. The non-selective muscarinic acetylcholine receptors (mAchR) agonists and antagonists can affect the proliferation of hepatocytes, but little is known about the role of mAChR in hepatocytes and hepatic fibrosis and the signaling pathway of this receptor in regulation of hepatocytes remains elusive. Here, 3ml/kg 40% carbon tetrachloride (CCL4) was given to induce hepatic fibrosis in rats and the hepatocytes were isolated to investigate the expression of mAchR and the cell signaling pathways which were involved in...
March 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28341945/translational-value-of-drug-discrimination-with-typical-and-atypical-antipsychotic-drugs
#3
Joseph H Porter, Kevin A Webster, Adam J Prus
This chapter focuses on the translational value of drug discrimination as a preclinical assay for drug development. In particular, the importance of two factors, i.e., training dose and species, for drug discrimination studies with the atypical antipsychotic clozapine is examined. Serotonin receptors appear to be an important pharmacological mechanism mediating clozapine's discriminative cue in both rats and mice, although differences are clearly evident as antagonism of cholinergic muscarinic receptors is important in rats at a higher training dose (5...
March 25, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28340862/symptom-variability-and-control-in-copd-advantages-of-dual-bronchodilation-therapy
#4
REVIEW
Fabiano Di Marco, Pierachille Santus, Nicola Scichilone, Paolo Solidoro, Marco Contoli, Fulvio Braido, Angelo Guido Corsico
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is a heterogeneous disorder characterized by usually progressive development of airflow obstruction that is not fully reversible. While most patients will experience symptoms throughout the day or in the morning upon awakening, many patients do not experience their symptoms as constant but report variability in symptoms during the course of the day or over time. Symptom variability adversely affects patients' health status and increases the risk of COPD exacerbations...
April 2017: Respiratory Medicine
https://www.readbyqxmd.com/read/28337126/competition-between-persistent-na-and-muscarine-sensitive-k-currents-shapes-perithreshold-resonance-and-spike-tuning-in-ca1-pyramidal-neurons
#5
Jorge Vera, Julio Alcayaga, Magdalena Sanhueza
Neurons from many brain regions display intrinsic subthreshold theta-resonance, responding preferentially to theta-frequency oscillatory stimuli. Resonance may contribute to selective communication among neurons and to orchestrate brain rhythms. CA1 pyramidal neurons receive theta activity, generating place fields. In these neurons the expression of perithreshold frequency preference is controversial, particularly in the spiking regime, with evidence favoring either non-resonant (integrator-like) or resonant behavior...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28336323/m1-muscarinic-activation-induces-long-lasting-increase-in-intrinsic-excitability-of-striatal-projection-neurons
#6
Xiaohui Lv, Jonathan W Dickerson, Jerri M Rook, Craig W Lindsley, P Jeffrey Conn, Zixiu Xiang
The dorsolateral striatum is critically involved in movement control and motor learning. Striatal function is regulated by a variety of neuromodulators including acetylcholine. Previous studies have shown that cholinergic activation excites striatal principal projection neurons, medium spiny neurons (MSNs), and this action is mediated by muscarinic acetylcholine subtype 1 receptors (M1) through modulating multiple potassium channels. In the present study, we used electrophysiology techniques in conjunction with optogenetic and pharmacological tools to determine the long-term effects of striatal cholinergic activation on MSN intrinsic excitability...
March 20, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28334727/discovering-the-relative-efficacy-of-inhaled-medications-for-chronic-obstructive-pulmonary-disease-multiple-treatment-comparisons
#7
Ying Zhu, Tong Zhang, Haiyan Li, Yang Yang, Qiong Chen, Lei Kong, Bo Tai
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is managed by three major classes of inhaled medications: inhaled corticosteroids (ICS), long-acting Beta 2-agonist (LABA), long-acting muscarinic antagonist (LAMA). Single inhaled medication is usually replaced by combined inhaled medications for efficacy enhancement. However, this practice should be supported by clinical evidence for large-scale implementations. METHODS: The relative efficacy of inhaled medications is determined by three endpoints: changes in the trough forced expiratory volume in 1 second (tFEV1), changes in the St George's Respiratory Questionnaire (SGRQ) score and the proportion of SGRQ responders which represents a reduction in SGRQ total score at week 24 of ≥4...
March 27, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28334356/transient-cell-intrinsic-activity-regulates-the-migration-and-laminar-positioning-of-cortical-projection-neurons
#8
Nicolas Hurni, Marta Kolodziejczak, Ugo Tomasello, Joan Badia, Moritz Jacobshagen, Julien Prados, Alexandre Dayer
Neocortical microcircuits are built during development and require the coordinated assembly of excitatory glutamatergic projection neurons (PNs) into functional networks. Neuronal migration is an essential step in this process. In addition to cell-intrinsic mechanisms, external cues including neurotransmitters regulate cortical neuron migration, suggesting that early activity could influence this process. Here, we aimed to investigate the role of cell-intrinsic activity in migrating PNs in vivo using a designer receptor exclusively activated by a designer drug (DREADD) chemogenetic approach...
March 17, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28332063/decreased-interaction-between-zo-1-and-occludin-is-involved-in-alteration-of-tight-junctions-in-transplanted-epiphora-submandibular-glands
#9
Chong Ding, Xin Cong, Xue-Ming Zhang, Sheng-Lin Li, Li-Ling Wu, Guang-Yan Yu
Tight junctions (TJs) in salivary epithelium play an important role in regulating saliva secretion. Autologous transplantation of submandibular glands (SMGs) is an effective method to treat severe dry eye syndrome. However, epiphora occurs in some patients 6 months after transplantation. We previously found that the acinar TJs are enlarged in rabbit SMGs after long-term transplantation, but the exact TJ components involved in the epiphora are still unknown. Here, we found that the mRNA and protein expression of ZO-1 and occludin were increased in the transplanted SMGs obtained from epiphora patients, while other TJs were unchanged...
March 22, 2017: Journal of Molecular Histology
https://www.readbyqxmd.com/read/28328743/acetylcholine-atropine-interactions-paradoxical-effects-on-atrial-fibrillation-inducibility
#10
Yu Liu, Benjamin J Scherlag, Youqi Fan, Wenfang Xia, He Huang, Sunny S Po
Atropine (ATr) is well known as a cholinergic antagonist, however, at low concentrations ATr could paradoxically accentuate the parasympathetic actions of acetylcholine (ACh). In 22 pentobarbital anesthetized dogs, via a left and right thoracotomy, a leak proof barrier was attached to isolate the atrial appendages (AAs) from the rest of the atria. In Group 1(Ach+ATr+Ach), ACh, 100 mM, was placed on the AA followed by the application of ATr, 2mg/cc. The average AFdur was 17±7 minutes. After ATr was applied to the AA and ACh again tested, the AFdur was markedly attenuated (2±2 minutes, p<0...
March 21, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28328190/effects-of-nitric-oxide-inhibitors-in-mice-with-bladder-outlet-obstruction
#11
Marcy Lancia Pereira, Carlos Arturo Levi D'ancona, Julio Alejandro Rojas-Moscoso, Antonio Celso Saragossa Ramos, Fabiola Zakia Monica, Edson Antunes
PURPOSE: To investigate the lower urinary tract changes in mice treated with L-NAME, a non-selective competitive inhibitor of nitric oxide synthase (NOS), or aminoguanidine, a competitive inhibitor of inducible nitric oxide synthase (iNOS), after 5 weeks of partial bladder outlet obstruction (BOO), in order to evaluate the role of constitutive and non-constitutive NOS in the pathogenesis of this experimental condition. MATERIALS AND METHODS: C57BL6 male mice were partially obstructed and randomly allocated into 6 groups: Sham, Sham + L-NAME, Sham + aminoguanidine, BOO, BOO + L-NAME and BOO + aminoguanidine...
March 2017: International Braz J Urol: Official Journal of the Brazilian Society of Urology
https://www.readbyqxmd.com/read/28326934/activations-of-muscarinic-m1-receptors-in-the-anterior-cingulate-cortex-contribute-to-the-antinociceptive-effect-via-gabaergic-transmission
#12
Kohei Koga, Yu Matsuzaki, Kenji Honda, Fumihiro Eto, Tomonori Furukawa, Keisuke Migita, Keiichi Irie, Kenichi Mishima, Shinya Ueno
Background Cholinergic systems regulate the synaptic transmission resulting in the contribution of the nociceptive behaviors. Anterior cingulate cortex is a key cortical area to play roles in nociception and chronic pain. However, the effect of the activation of cholinergic system for nociception is still unknown in the cortical area. Here, we tested whether the activation of cholinergic receptors can regulate nociceptive behaviors in adult rat anterior cingulate cortex by integrative methods including behavior, immunohistochemical, and electrophysiological methods...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28326549/the-three-finger-toxin-fold-a-multifunctional-structural-scaffold-able-to-modulate-cholinergic-functions
#13
REVIEW
Pascal Kessler, Pascale Marchot, Marcela Silva, Denis Servent
Three-finger fold toxins are miniproteins frequently found in Elapidae snake venoms. This fold is characterized by three distinct loops rich in β-strands and emerging from a dense, globular core reticulated by four highly conserved disulfide bridges. The number and diversity of receptors, channels, and enzymes identified as targets of three-finger fold toxins is increasing continuously. Such manifold diversity highlights the specific adaptability of this fold for generating pleiotropic functions. Although this toxin superfamily disturbs many biological functions by interacting with a large diversity of molecular targets, the most significant target is the cholinergic system...
March 21, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28324647/metabolism-and-distribution-of-clozapine-n-oxide-implications-for-nonhuman-primate-chemogenetics
#14
Jessica Raper, J Scott Daniels, Ryan D Morrison, Leonard Howell, Jocelyne Bachevalier, Thomas Wichmann, Adriana Galvan
The use of Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) in neuroscience has rapidly expanded in rodent studies, but has lagged behind in nonhuman primate (NHP) experiments, slowing the development of this method for therapeutic use in humans. One reason for the slow adoption of DREADD technology in primates is that the pharmacokinetic properties and bioavailability of clozapine-n-oxide (CNO), the most commonly used ligand for human muscarinic (hM) DREADDs, are not fully described in primates...
March 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28315343/inhibition-of-agonist-induced-smooth-muscle-contraction-by-picotamide-in-the-male-human-lower-urinary-tract-outflow-region
#15
Martin Hennenberg, Alexander Tamalunas, Yiming Wang, Patrick Keller, Melanie Schott, Frank Strittmatter, Annika Herlemann, Qingfeng Yu, Beata Rutz, Anna Ciotkowska, Christian G Stief, Christian Gratzke
Male lower urinary tract symptoms (LUTS) due to bladder outlet obstruction are characterized by abnormal smooth muscle contractions in the lower urinary tract. Alpha1-adrenoceptor antagonists may induce smooth muscle relaxation in the outflow region and represent the current goldstandard of medical treatment. However, results may be unsatisfactory or inadequate. Apart from α1-adrenoceptor agonists, smooth muscle contraction in the outflow region may be induced by thromboxane A2 (TXA2), endothelins, or muscarinic receptor agonists...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315276/the-sigma-1-receptor-a-therapeutic-target-for-the-treatment-of-als
#16
Timur A Mavlyutov, Erin M Baker, Tasher M Losenegger, Jaimie R Kim, Brian Torres, Miles L Epstein, Arnold E Ruoho
The membrane bound 223 amino acid Sigma-1 Receptor (S1R) serves as a molecular chaperone and functional regulator of many signaling proteins. Spinal cord motor neuron activation occurs, in part, via large ventral horn cholinergic synapses called C-boutons/C-terminals. Chronic excitation of motor neurons and alterations in C-terminals has been associated with Amyotrophic Lateral Sclerosis (ALS ). The S1R has an important role in regulating motor neuron function. High levels of the S1R are localized in postsynaptic endoplasmic reticulum (ER) subsurface cisternae within 10-20 nm of the plasma membrane that contain muscarinic type 2 acetylcholine receptors (M2AChR), calcium activated potassium channels (Kv2...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28302036/pharmacological-effects-of-turmeric-on-learning-memory-and-expression-of-muscarinic-receptor-genes-m1-m3-and-m5-in-stress-induced-mouse-model
#17
Aliya Khalid, Rabia Shakeel, Saira Justin, Ghazala Iqbal, Syed Adnan Ali Shah, Saadia Zahid, Touqeer Ahmed
Stress is involved in memory impairment by multiple mechanisms including activation of Hypothalamic-Pituitary Axis, which in turn activates release of corticosterone in blood. Cholinergic system blockade by muscarinic antagonist like scopolamine, also impairs memory. AIM: This study aimed to investigate the effect of turmeric (20mg/kg) on learning and memory and cholinergic system in a mouse model of stress along with cholinergic blockade. METHODS: Restrained stress was induced and cholinergic receptors were blocked using scopolamine in mice...
March 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28301610/the-effects-of-substance-p-and-acetylcholine-on-human-tenocyte-proliferation-converge-mechanistically-via-tgf-%C3%AE-1
#18
Gloria Fong, Ludvig J Backman, Håkan Alfredson, Alex Scott, Patrik Danielson
Previous in vitro studies on human tendon cells (tenocytes) have demonstrated that the exogenous administration of substance P (SP) and acetylcholine (ACh) independently result in tenocyte proliferation, which is a prominent feature of tendinosis. Interestingly, the possible link between SP and ACh has not yet been explored in human tenocytes. Recent studies in other cell types demonstrate that both SP and ACh independently upregulate TGF-β1 expression via their respective receptors, the neurokinin 1 receptor (NK-1R) and muscarinic ACh receptors (mAChRs)...
2017: PloS One
https://www.readbyqxmd.com/read/28300854/randomized-placebo-and-active-controlled-crossover-study-of-the-safety-and-efficacy-of-thvd-102-a-fixed-dose-combination-of-oxybutynin-and-pilocarpine-in-subjects-with-primary-focal-hyperhidrosis
#19
David M Pariser, Janakan Krishnaraja, Thomas M Tremblay, R Michael Rubison, Ted W Love, Benjamin F McGraw
BACKGROUND: While muscarinic antagonists (anticholinergics) have shown efficacy in treating primary focal hyperhidrosis (PFH), side effects - most commonly dry mouth - are intolerable for most patients. THVD-102, a fixed-dose combination product has been developed combining oxybutynin, a muscarinic antagonist, and pilocarpine, a muscarinic agonist. The pilocarpine is at a dose level and release profile optimized to correct salivary flow impaired by oxybutynin yet not interfere with the therapeutic muscarinic antagonist effect of oxybutynin upon the sweat glands...
February 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28299422/homeostatic-regulation-through-gaba-and-acetylcholine-muscarinic-receptors-of-motor-trigeminal-neurons-following-sleep-deprivation
#20
Hanieh Toossi, Esther Del Cid-Pellitero, Barbara E Jones
Muscle tone is regulated across sleep-wake states, being maximal in waking, reduced in slow wave sleep (SWS) and absent in paradoxical or REM sleep (PS or REMS). Such changes in tone have been recorded in the masseter muscles and shown to correspond to changes in activity and polarization of the trigeminal motor 5 (Mo5) neurons. The muscle hypotonia and atonia during sleep depend in part on GABA acting upon both GABAA and GABAB receptors (Rs) and acetylcholine (ACh) acting upon muscarinic 2 (AChM2) Rs. Here, we examined whether Mo5 neurons undergo homeostatic regulation through changes in these inhibitory receptors following prolonged activity with enforced waking...
March 15, 2017: Brain Structure & Function
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