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Muscarinic receptors

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https://www.readbyqxmd.com/read/28432022/a-crosstalk-between-muscarinic-and-crf2-receptors-regulates-cellular-adhesion-properties-of-human-colon-cancer-cells
#1
M Pelissier-Rota, N T Chartier, B Bonaz, M R Jacquier-Sarlin
Patients with inflammatory bowel disease often suffer from chronic and relapsing intestinal inflammation that favor the development of colitis associated cancer. An alteration of the epithelial intestinal barrier function observed in IBD is supposed to be a consequence of stress. It has been proposed that corticotrophin-releasing factor receptor (CRF2), one of the two receptors of CRF, the principal neuromediator of stress, acts on cholinergic nerves to induce stress-mediated epithelial barrier dysfunction...
April 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28431780/tolterodine-tartrate
#2
Gennady Ananchenko, Jasmina Novakovic
Tolterodine tartrate belongs to the family of muscarinic receptor antagonists and is indicated for the treatment of overactive urinary bladder syndrome. This chapter provides an overview of physical, analytical, and ADME profiles; highlights methods of chemical synthesis; and discusses stability of tolterodine as a free base and/or its l-tartrate salt in solution and in the solid state. The information presented in this chapter is based on the peer-reviewed literature, compendial reports (USP, EP), and authors' data...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28429224/combined-effects-of-m1-muscarinic-acetylcholine-receptor-agonist-tbpb-and-%C3%AE-7n-acetylcholine-receptor-activator-gts-21-on-mouse-mortality-and-blood-concentration-of-proinflammatory-cytokines-in-sepsis
#3
P F Zabrodskii, M S Gromov, V V Maslyakov
Experiments on random-bred albino mice showed that M1 muscarinic acetylcholine receptor agonist (TBPB) and α7n-acetylcholine receptor agonist (GTS-21) significantly reduced mortality of mice with experimental sepsis (intraperitoneally administration of E. coli) in 4 and 24 h after modeling by reducing blood concentration of proinflammatory cytokines TNF-α, IL-1β, and IL-6. Combined treatment with TBPB and GTS-21 determined their additive effect.
April 21, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28426939/high-throughput-agonist-shift-assay-development-for-the-analysis-of-m1-positive-allosteric-modulators
#4
Michelle F Homsher, Douglas C Beshore, Jason Cassaday, Brian Squadroni, Elizabeth Mohammed, Michelle Hartnett, Stephen Day, Lei Ma, David Pechter, Michelle D Smith, Fredrick Monsma, Paul Zuck, Michael F Finley, Victor N Uebele, Jeffrey D Hermes
Agonist shift assays feature cross-titrations of allosteric modulators and orthosteric ligands. Information generated in agonist shift assays can include a modulator's effect on the orthosteric agonist's potency (alpha) and efficacy (beta), as well as direct agonist activity of the allosteric ligand (tauB) and the intrinsic binding affinity of the modulator to the unoccupied receptor (KB). Because of the heavy resource demand and complex data handling, these allosteric parameters are determined infrequently during the course of a drug discovery program and on a relatively small subset of compounds...
April 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28422371/effects-of-m1-and-m4-activation-on-excitatory-synaptic-transmission-in-ca1
#5
Catherine Thorn, Michael Popiolek, Eda Stark, Jeremy Edgerton
Hippocampal networks are particularly susceptible to dysfunction in many neurodegenerative diseases and neuropsychiatric disorders including Alzheimer's disease, Lewy body dementia, and schizophrenia. CA1, a major output region of the hippocampus, receives glutamatergic input from both hippocampal CA3 and entorhinal cortex, via the Schaffer collateral (SC) and temporoammonic (TA) pathways, respectively. SC and TA inputs to CA1 are thought to be differentially involved in the retrieval of previously stored memories versus the encoding of novel information, and switching between these two crucial hippocampal functions is thought to critically depend on acetylcholine (ACh) acting at muscarinic receptors...
April 19, 2017: Hippocampus
https://www.readbyqxmd.com/read/28419871/short-term-inhibition-of-gabaergic-ipscs-induced-by-association-of-pre-and-postsynaptic-activation-in-the-neonatal-hippocampus
#6
Megumi Taketo, Hiroko Matsuda
Activity-dependent plasticity including short and long-term depression accompanied by a reduction in transmitter release probability has been demonstrated in both inhibitory and excitatory synapses. In the neonatal hippocampus, repetitive postsynaptic depolarization is followed by presynaptic alterations of the efficacy of GABAAergic transmission. Both facilitation and inhibition have been observed, but the mechanisms underlying this plasticity have not yet been elucidated. In the present experiment, repetitive postsynaptic depolarization by itself did not cause marked alterations of spontaneous inhibitory postsynaptic currents (sIPSCs)...
April 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28416748/differential-expression-of-m3-muscarinic-receptors-in-progressive-colon-neoplasia-and-metastasis
#7
Kunrong Cheng, Aaron C Shang, Cinthia B Drachenberg, Min Zhan, Jean-Pierre Raufman
M3 muscarinic receptor (M3R) activation promotes colon cancer cell proliferation, migration, and invasion in vitro. Although over-expression of CHRM3, the gene encoding M3R, is reported in primary colon cancers, expression of M3R itself has not been studied in colon neoplasia. We compared M3R expression in normal colon to colon adenomas, and primary and metastatic colon cancers. Compared to adjacent normal colon, CHRM3 expression was increased up to 128-fold in 10 of 18 consecutive surgical cancer specimens (56%) and associated with metastatic spread (P < 0...
March 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28415952/effective-treatment-of-ketamine-associated-cystitis-with-botulinum-toxin-type-a-injection-combined-with-bladder-hydrodistention
#8
Jianfeng Zeng, Haibiao Lai, Dongxiang Zheng, Liang Zhong, Zhifeng Huang, Shanyun Wang, Weiwei Zou, Lianbo Wei
Objective Ketamine-associated cystitis (KAC) has been described in a few case reports, but its treatment in a relatively large number of patients has not been documented. This study aimed to describe our experience of treatment of 36 patients with KAC. Methods Thirty-six patients (30 males and 6 females, aged 19-38 years) with KAC, who had previously taken a muscarinic receptor blocker and/or antibiotics, but without symptomatic relief, were treated with botulinum toxin A injection combined with bladder hydrodistention...
April 2017: Journal of International Medical Research
https://www.readbyqxmd.com/read/28414301/striatopallidal-dysfunction-underlies-repetitive-behavior-in-shank3-deficient-model-of-autism
#9
Wenting Wang, Chenchen Li, Qian Chen, Marie-Sophie van der Goes, James Hawrot, Annie Y Yao, Xian Gao, Congyi Lu, Ying Zang, Qiangge Zhang, Katherine Lyman, Dongqing Wang, Baolin Guo, Shengxi Wu, Charles R Gerfen, Zhanyan Fu, Guoping Feng
The postsynaptic scaffolding protein SH3 and multiple ankyrin repeat domains 3 (SHANK3) is critical for the development and function of glutamatergic synapses. Disruption of the SHANK3-encoding gene has been strongly implicated as a monogenic cause of autism, and Shank3 mutant mice show repetitive grooming and social interaction deficits. Although basal ganglia dysfunction has been proposed to underlie repetitive behaviors, few studies have provided direct evidence to support this notion and the exact cellular mechanisms remain largely unknown...
April 17, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28412413/activation-of-muscarinic-receptors-prevents-tnf-%C3%AE-mediated-intestinal-epithelial-barrier-disruption-through-p38-mapk
#10
Junsuke Uwada, Takashi Yazawa, Md Tariqul Islam, Md Rafiqul Islam Khan, Susanne M Krug, Michael Fromm, Shin-Ichiro Karaki, Yuichi Suzuki, Atsukazu Kuwahara, Hatsumi Yoshiki, Kiyonao Sada, Muramatsu, Takanobu Taniguchi
Intestinal epithelial cells form a tight barrier to act as selective physical barriers, repelling hostile substances. Tumor necrosis factor-α (TNF-α) is a well characterized pro-inflammatory cytokine which can compromise intestinal barrier function and the suppression of TNF-α function is important for treatment of inflammatory bowel disease (IBD). In this study, we investigated the contribution of G-protein-coupled receptor (GPCR)-induced signalling pathways to the maintenance of epithelial barrier function...
April 12, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28412329/comparison-of-pro-amnesic-efficacy-of-scopolamine-biperiden-and-phencyclidine-by-using-passive-avoidance-task-in-cd-1-mice
#11
Natalia Malikowska, Kinga Sałat, Adrian Podkowa
INTRODUCTION: Memory disorders accompany numerous diseases and therapies, and this is becoming a growing medical issue worldwide. Currently, various animal models of memory impairments are available; however, many of them require high financial outlay and/or are time-consuming. A simple way to achieve an efficient behavioral model of cognitive disorders is to inject defined drug that has pro-amnesic properties. Since the involvement of cholinergic and glutamatergic neurotransmission in cognition is well established, the utilization of a nonselective muscarinic receptor antagonist, scopolamine (SCOP), a selective M1 muscarinic receptor antagonist, biperiden (BIP), and a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist, phencyclidine (PCP) seems to be reliable tools to induce amnesia...
April 13, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28411153/antagonism-of-muscarinic-acetylcholine-receptors-in-medial-prefrontal-cortex-disrupts-the-context-preexposure-facilitation-effect
#12
P A Robinson-Drummer, N A Heroux, M E Stanton
Cholinergic function plays a role in a variant of context fear conditioning known as the context preexposure facilitation effect (CPFE; Robinson-Drummer, Dokovna, Heroux, & Stanton, 2016). In the CPFE, acquisition of a context representation, the context-shock association, and expression of context fear occur across successive phases, usually 24hr apart. Systemic administration of scopolamine, a muscarinic acetylcholine receptor antagonist, prior to each phase (context preexposure, immediate-shock training, and testing) disrupts the CPFE in juvenile rats (Robinson-Drummer et al...
April 11, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28411124/m3-muscarinic-acetylcholine-receptor-facilitates-the-endocytosis-of-mu-opioid-receptor-mediated-by-morphine-independently-of-the-formation-of-heteromeric-complexes
#13
Juan F Lopez-Gimenez, Elisa Alvarez-Curto, Graeme Milligan
Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity. We recently described that activation of Gαq/11 proteins through 5-HT2A serotonin receptors co-expressed in the same cells facilitates MOP receptor endocytosis promoted by morphine. In order to explore whether a different Gαq/11 coupled GPCR would emulate this effect, a double stable Flp-In T-REx HEK293 cell line permanently expressing MOP-YFP receptors along with FLAG-M3-Cerulean receptors expressed in an inducible manner was generated...
April 11, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28408330/muscarinic-cholinoreceptors-m1-m2-m3-and-m4-type-modulate-the-acetylcholine-secretion-in-the-frog-neuromuscular-junction
#14
Andrei N Tsentsevitsky, Irina V Kovyazina, Leniz F Nurullin, Eugeny E Nikolsky
Muscarinic cholinoreceptors regulate the neurosecretion process in vertebrate neuromuscular junctions. The diversity of muscarinic effects on acetylcholine (ACh) secretion may be attributed to the different muscarinic subtypes involved in this process. In the present study, the location of five muscarinic receptor subtypes (M1, M2, M3, M4 and M5) on the motor nerve terminals of frog cutaneous pectoris muscle was shown using specific polyclonal antibodies. The modulatory roles of these receptors were investigated via assessment of the effects of muscarine and specific muscarinic antagonists on the quantal content of endplate currents (EPCs) and the time course of secretion, which was estimated from the distribution of "real" synaptic delays of EPCs recorded in a low Ca(2+)/high Mg(2+) solution...
April 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28406538/acetylcholine-modulates-gamma-frequency-oscillations-in-the-hippocampus-by-activation-of-muscarinic-m1-receptors
#15
Ruth T Betterton, Lisa M Broad, Krasimira Tsaneva-Atanasova, Jack R Mellor
Modulation of gamma oscillations is important for the processing of information and the disruption of gamma oscillations is a prominent feature of schizophrenia and Alzheimer's disease. Gamma oscillations are generated by the interaction of excitatory and inhibitory neurons where their precise frequency and amplitude are controlled by the balance of excitation and inhibition. Acetylcholine enhances the intrinsic excitability of pyramidal neurons and supresses both excitatory and inhibitory synaptic transmission but the net modulatory effect on gamma oscillations is not known...
April 12, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28406132/role-of-tolterodine-in-the-management-of-postoperative-catheter-related-bladder-discomfort-findings-in-a-nigerian-teaching-hospital
#16
K H Tijani, N O Akanmu, J O Olatosi, R W Ojewola
BACKGROUND: Patient discomfort secondary to an indwelling urethral catheter in the post operative period can be very distressing. These symptoms resemble the overactive bladder (OAB) syndrome. Muscarinic receptor blockers have been successful in the management of OAB. However, information on the use of these drugs in the management of the postoperative catheter-related bladder discomfort (CRBD) in sub-Saharan Africa is still relatively sparse. OBJECTIVE: To assess the efficacy of preoperative oral tolterodine in the management of CRBD in surgical patients in the immediate postoperative period...
April 2017: Nigerian Journal of Clinical Practice
https://www.readbyqxmd.com/read/28404742/autonomic-nervous-system-activation-mediates-the-increase-in-whole-body-glucose-uptake-in-response-to-electroacupuncture
#17
Anna Benrick, Milana Kokosar, Min Hu, Martin Larsson, Manuel Maliqueo, Rodrigo Rodrigues Marcondes, Marzia Soligo, Virginia Protto, Elisabet Jerlhag, Antonina Sazonova, Carl Johan Behre, Kurt Højlund, Peter Thorén, Elisabet Stener-Victorin
A single bout of low-frequency electroacupuncture (EA) causing muscle contractions increases whole-body glucose uptake in insulin-resistant rats. We explored the underlying mechanism of this finding and whether it can be translated into clinical settings. Changes in glucose infusion rate (GIR) were measured by euglycemic-hyperinsulinemic clamp during and after 45 min of low-frequency EA in 21 overweight/obese women with polycystic ovary syndrome (PCOS) and 21 controls matched for age, weight, and body mass index (experiment 1) and in rats receiving autonomic receptor blockers (experiment 2)...
April 12, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28399855/characterisation-of-a-murine-model-of-the-late-asthmatic-response
#18
Katie Baker, Kristof Raemdonck, Robert J Snelgrove, Maria G Belvisi, Mark A Birrell
BACKGROUND: The incidence of asthma is increasing at an alarming rate. While the current available therapies are effective, there are associated side effects and they fail to adequately control symptoms in all patient subsets. In the search to understand disease pathogenesis and find effective therapies hypotheses are often tested in animal models before progressing into clinical studies. However, current dogma is that animal model data is often not predictive of clinical outcome. One possible reason for this is the end points measured such as antigen-challenge induced late asthmatic response (LAR) is often used in early clinical development, but seldom in animal model systems...
April 11, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28396684/muscarinic-receptors-types-1-and-2-in-the-preoptic-anterior-hypothalamic-areas-regulate-ovulation-unequally-in-the-rat-oestrous-cycle
#19
Yadira L López-Ramírez, Kayro López-Ramírez, Isabel Arrieta-Cruz, Angélica Flores, Luciano Mendoza-Garcés, Raúl A Librado-Osorio, Roger Gutiérrez-Juárez, Roberto Domínguez, María Esther Cruz
Muscarinic receptors types 1 (m1AChR) and 2 (m2AChR) in the preoptic and anterior hypothalamus areas (POA-AHA) were counted, and the effects of blocking these receptors on spontaneous ovulation were analysed throughout the rat oestrous cycle. Rats in each phase of the oestrous cycle were assigned to the following experiments: (1) an immunohistochemical study of the number of cells expressing m1AChR or m2AChR in the POA-AHA and (2) analysis of the effects of the unilateral blockade of the m1AChR (pirenzepine, PZP) or m2AChR (methoctramine, MTC) on either side of the POA-AHA on the ovulation rate...
2017: International Journal of Endocrinology
https://www.readbyqxmd.com/read/28395930/acetylcholine-attenuated-tnf-%C3%AE-induced-intracellular-ca-2-overload-by-inhibiting-the-formation-of-the-ncx1-trpc3-ip3r1-complex-in-human-umbilical-vein-endothelial-cells
#20
Ming Zhao, Hang-Huan Jia, Long-Zhu Liu, Xue-Yuan Bi, Man Xu, Xiao-Jiang Yu, Xi He, Wei-Jin Zang
The endoplasmic reticulum (ER) forms discrete junctions with the plasma membrane (PM) that play a critical role in the regulation of Ca(2+) signaling during cellular bioenergetics, apoptosis and autophagy. We have previously confirmed that acetylcholine can inhibit ER stress and apoptosis after inflammatory injury. However, limited research has focused on the effects of acetylcholine on ER-PM junctions. In this work, we evaluated the structure and function of the supramolecular sodium-calcium exchanger 1 (NCX1)-transient receptor potential canonical 3 (TRPC3)-inositol 1,4,5-trisphosphate receptor 1 (IP3R1) complex, which is involved in regulating Ca(2+) homeostasis during inflammatory injury...
April 7, 2017: Journal of Molecular and Cellular Cardiology
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