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1. Combined nutritional stress and a new systemic pesticide (flupyradifurone, Sivanto®) reduce bee survival, food consumption, flight success, and thermoregulation

Author:
Tong, Linda; Nieh, James C.; Tosi, Simone
Source:
Chemosphere 2019 v.237 pp. 124408
ISSN:
0045-6535
Subject:
acetylcholine,   etc   ; Apis mellifera; adverse effects; agonists; beneficial insects; flight; food consumption; honey bees; hypothermia; lethal dose 50; malnutrition; mortality; nectar; neonicotinoid insecticides; risk assessment; thermoregulation;     Show all 16 Subjects
Abstract:
... Flupyradifurone (FPF, Sivanto®) is a new butenolide insecticide that, like the neonicotinoids, is a systemic nicotinic acetylcholine receptor (nAChR) agonist. However, FPF is considered bee-safe (according to standard Risk Assessment tests), and is thus a potential solution to the adverse effects of other pesticides on beneficial insects. To date, no studies have examined the impact of nutritional ...
DOI:
10.1016/j.chemosphere.2019.124408

2. Respiratory failure triggered by cholinesterase inhibitors may involve activation of a reflex sensory pathway by acetylcholine spillover

Author:
Nervo, Aurélie; Calas, André-Guilhem; Nachon, Florian; Krejci, Eric
Source:
Toxicology 2019 v.424 pp. 152232
ISSN:
0300-483X
Subject:
acetylcholine,   etc   ; acetylcholinesterase; agonists; brain; breathing; cholinesterase; cholinesterase inhibitors; cineole; enzyme inhibition; mice; muscles; nose; reflexes; sensory neurons; synapse; synaptic transmission; tissues; toxicity;     Show all 18 Subjects
Abstract:
... Respiration failure during exposure by cholinesterase inhibitors has been widely assumed to be due to inhibition of cholinesterase in the brain. Using a double chamber plethysmograph to measure various respiratory parameters, we observed long “end inspiratory pauses” (EIP) during most exposure that depressed breathing. Surprisingly, Colq KO mice that have a normal level of acetylcholinesterase (AC ...
DOI:
10.1016/j.tox.2019.06.003

3. Combined effects of mutations in loop C and the loop D-E-G triangle on neonicotinoid interactions with Drosophila Dα1/chicken β2 hybrid nAChRs

Author:
Hikida, Mai; Shimada, Shota; Kurata, Ryo; Shigetou, Sho; Ihara, Makoto; Sattelle, David B.; Matsuda, Kazuhiko
Source:
Pesticide biochemistry and physiology 2018 v.151 pp. 47-52
ISSN:
0048-3575
Subject:
acetylcholine,   etc   ; Drosophila; Xenopus laevis; agonists; binding sites; electrophysiology; hybrids; imidacloprid; mutation; nicotinic receptors; oocytes; thiacloprid;     Show all 12 Subjects
Abstract:
... Neonicotinoid insecticides interact with the orthosteric sites of nicotinic acetylcholine receptors (nAChRs) formed at the interfaces of (a) two adjacent α subunits and (b) α and non-α subunits. However, little is known of the detailed contributions of these two orthosteric sites to neonicotinoid actions. We therefore applied voltage-clamp electrophysiology to the Dα1/chicken β2 hybrid nAChR expre ...
DOI:
10.1016/j.pestbp.2018.03.008

4. Isosamidin, an extract of Peucedanum japonicum, inhibits phenylephrine‐mediated contractions of the human prostate in vitro

Author:
Suzuki, Takahisa; Otsuka, Atsushi; Ito, Yoshihiko; Yamada, Shizuo; Miyake, Hideaki; Ozono, Seiichiro
Source:
Phytotherapy research 2018 v.32 no.5 pp. 949-952
ISSN:
0951-418X
Subject:
acetylcholine,   etc   ; Peucedanum japonicum; active ingredients; agonists; bladder; clinical trials; health foods; humans; hyperplasia; males; medicinal properties; patients; phenylephrine; East Asia;     Show all 14 Subjects
Abstract:
... Isosamidin is a pharmacologically active compound extracted from Peucedanum japonicum which is used as a health food in East Asia. Our preliminary animal data suggested that isosamidin may have sufficient potency to treat patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia or overactive bladder. However, the efficacy of isosamidin in humans is unknown. Here, we ex ...
DOI:
10.1002/ptr.6039

5. Synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor

Author:
Li, Quan; Chen, Hai-Feng
Source:
RSC advances 2018 v.8 no.24 pp. 13067-13074
ISSN:
2046-2069
Subject:
acetylcholine,   etc   ; agonists; algorithms; calcium channels; cardiac output; central nervous system; humans; information exchange; metabolic diseases; molecular dynamics; muscarine receptors; mutation;     Show all 12 Subjects
Abstract:
... Muscarinic acetylcholine receptors are GPCRs that regulate the activity of a diverse array of central and peripheral functions in the human body, including the parasympathetic actions of acetylcholine. The M2 muscarinic receptor subtype plays a key role in modulating cardiac function and many important central processes. The orthosteric agonist and allosteric modulator can bind the pocket of M2. H ...
DOI:
10.1039/c8ra01545g

6. Effects of selective α2‐adrenergic receptor agonists on electrical field‐stimulated contractions of isolated bronchi in horses

Author:
Menozzi, A.; Pozzoli, C.; Poli, E.; Colla, C.; Placenza, G.; Bertini, S.
Source:
Journal of veterinary pharmacology and therapeutics 2018 v.41 no.2 pp. 246-253
ISSN:
0140-7783
Subject:
acetylcholine,   etc   ; agonists; alpha-2 adrenergic receptors; antagonists; bronchi; bronchoconstriction; carbachol; detomidine; electric field; horses; medetomidine; muscles; neurons; xylazine;     Show all 14 Subjects
Abstract:
... We investigated the effects of different selective α₂‐adrenergic receptor (AR) agonists (detomidine, medetomidine, xylazine, and brimonidine) on the contractions of horse‐isolated bronchi induced by electrical field stimulation (EFS) and by carbachol. No effects were observed on the contraction induced by carbachol, while α₂‐AR agonists reduced EFS‐evoked contractions in a concentration‐related fa ...
DOI:
10.1111/jvp.12470

7. Crosstalk between mAChRM3 and β2AR, via acetylcholine PI3/PKC/PBEP1/Raf-1 MEK1/2/ERK1/2 pathway activation, in human bronchial epithelial cells after long-term cigarette smoke exposure

Author:
Albano, Giusy Daniela; Bonanno, Anna; Moscato, Monica; Anzalone, Giulia; Di Sano, Caterina; Riccobono, Loredana; Wenzel, Sally E.; Profita, Mirella
Source:
Life sciences 2018 v.192 pp. 99-109
ISSN:
0024-3205
Subject:
acetylcholine,   etc   ; agonists; choline; choline acetyltransferase; chronic exposure; epithelial cells; humans; inflammation; interleukin-8; oxidative stress; phosphorylation; receptors;     Show all 12 Subjects
Abstract:
... Cigarette smoke extract (CSE) affects the expression of non-neuronal components of cholinergic system in bronchial epithelial cells and, as PEBP1/Raf-mediated MAPK1/2 and ERK1/2 pathway, promotes inflammation and oxidative stress.We studied whether Acetylcholine (ACh) is involved in the mechanism of crosstalk between mAChRM3 and β2Adrenergic receptors (β2AR) promoting, via PI3/PKC/PBEP1/Raf/MEK1/2 ...
DOI:
10.1016/j.lfs.2017.11.034

8. Oxotremorine-M potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms

Author:
Zwart, Ruud; Reed, Hannah; Sher, Emanuele
Source:
Biochemical and biophysical research communications 2018 v.495 no.1 pp. 481-486
ISSN:
0006-291X
Subject:
acetylcholine,   etc   ; Alzheimer disease; Xenopus; agonists; ammonium; antagonists; atropine; cognition; cortex; hippocampus; humans; memory; moieties; muscarine receptors; neuroplasticity; oocytes;     Show all 16 Subjects
Abstract:
... Muscarinic acetylcholine M1 receptors play an important role in synaptic plasticity in the hippocampus and cortex. Potentiation of NMDA receptors as a consequence of muscarinic acetylcholine M1 receptor activation is a crucial event mediating the cholinergic modulation of synaptic plasticity, which is a cellular mechanism for learning and memory. In Alzheimer's disease, the cholinergic input to th ...
DOI:
10.1016/j.bbrc.2017.11.036

9. Interactive effects of neonicotinoids and natural ultraviolet radiation on yellow perch (Perca flavescens) larvae

Author:
Paquet-Walsh, Angela; Bertolo, Andrea; Landry, Catherine; Deschamps, Lucas; Boily, Monique
Source:
The Science of the total environment 2019 v.685 pp. 690-701
ISSN:
0048-9697
Subject:
acetylcholine,   etc   ; Perca flavescens; acetylcholinesterase; agonists; agricultural land; agricultural watersheds; biomarkers; corn; enzyme activity; imidacloprid; insects; lakes; larvae; leaching; lipid peroxidation; lipids; mortality; nervous system; neurotransmitters; protein content; proteins; sublethal effects; synergism; thiamethoxam; ultraviolet radiation; vertebrates; Quebec; Saint Lawrence River;     Show all 28 Subjects
Abstract:
... Neonicotinoids (NEOCs) are insecticides that are widely used worldwide in the culture of maize and soya. Whereas they specifically target terrestrial insects by acting as agonists of the neurotransmitter acetylcholine in their nervous system, their effects on the cholinergic system of vertebrates is still unclear. Moreover, there is an increasing concern about their effects on aquatic biota becaus ...
DOI:
10.1016/j.scitotenv.2019.05.113

10. Probing for and Quantifying Agonist Hydrogen Bonds in α6β2 Nicotinic Acetylcholine Receptors

Author:
Post, Michael R.; Lester, Henry A.; Dougherty, Dennis A.
Source:
Biochemistry 2017 v.56 no.13 pp. 1836-1840
ISSN:
1520-4995
Subject:
acetylcholine,   etc   ; agonists; binding sites; hydrogen; hydrogen bonding; neurons; nicotine; nicotinic receptors;     Show all 8 Subjects
Abstract:
... Designing subtype-selective agonists for neuronal nicotinic acetylcholine receptors is a challenging and significant goal aided by intricate knowledge of each subtype’s binding patterns. We previously reported that in α6β2 receptors, acetylcholine makes a functional cation−π interaction with Trp149, but nicotine and TC299423 do not, suggesting a distinctive binding site. This work explores hydroge ...
DOI:
10.1021/acs.biochem.7b00213
PubMed:
28287260
PubMed Central:
PMC6075822

11. M3-subtype muscarinic receptor activation stimulates intracellular calcium oscillations and aldosterone production in human adrenocortical HAC15 cells

Author:
Malaiyandi, Latha M.; Sharthiya, Harsh; Surachaicharn, Nuntida; Shams, Yara; Arshad, Mohammad; Schupbach, Chad; Kopf, Phillip G.; Dineley, Kirk E.
Source:
Molecular and cellular endocrinology 2018 v.478 pp. 1-9
ISSN:
0303-7207
Subject:
acetylcholine,   etc   ; acute exposure; adrenal cortex; agonists; aldosterone; animal models; antagonists; calcium; carbachol; cattle; human cell lines; humans; image analysis; messenger RNA; muscarine receptors; neoplasm cells; secretion; steroid hormones;     Show all 18 Subjects
Abstract:
... A previous body of work in bovine and rodent models shows that cholinergic agonists modulate the secretion of steroid hormones from the adrenal cortex. In this study we used live-cell Ca²⁺ imaging to investigate cholinergic activity in the HAC15 human adrenocortical carcinoma cell line. The cholinergic agonists carbachol and acetylcholine triggered heterogeneous Ca²⁺ oscillations that were strongl ...
DOI:
10.1016/j.mce.2018.06.016

12. Substituted 2-Aminopyrimidines Selective for α7-Nicotinic Acetylcholine Receptor Activation and Association with Acetylcholine Binding Proteins

Author:
Kaczanowska, Katarzyna; Camacho Hernandez, Gisela Andrea; Bendiks, Larissa; Kohs, Larissa; Cornejo-Bravo, Jose Manuel; Harel, Michal; Finn, M. G.; Taylor, Palmer
Source:
Journal of the American Chemical Society 2017 v.139 no.10 pp. 3676-3684
ISSN:
1520-5126
Subject:
acetylcholine,   etc   ; agonists; antagonists; cholinergic receptors; complementary DNA; fluorescence; ion channels; ligands; median effective concentration; screening; serotonin receptors;     Show all 11 Subjects
Abstract:
... Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. To examine receptor interactions of this structural family on ligand-g ...
DOI:
10.1021/jacs.6b10746

13. IPPA08 allosterically enhances the action of imidacloprid on nicotinic acetylcholine receptors

Author:
Bao, Haibo; Shao, Xusheng; Zhang, Yixi; Cheng, Jiagao; Wang, Yunchao; Xu, Xiaoyong; Fang, Jichao; Liu, Zewen; Li, Zhong
Source:
Insect biochemistry and molecular biology 2016 v.79 pp. 36-41
ISSN:
0965-1748
Subject:
acetylcholine,   etc   ; Nilaparvata lugens; Xenopus; agonists; binding sites; cholinergic receptors; hybrids; imidacloprid; mutagenesis; oocytes; rats; synergism;     Show all 12 Subjects
Abstract:
... Our previous study showed that IPPA08, a cis-configuration neonicotinoid compound with unique oxabridged substructure, acted as a specific synergist to neonicotinoid insecticides targeting nicotinic acetylcholine receptors (nAChRs). Heteropentamer nAChRs have diverse characteristics and can form canonical and noncanonical subunit interfaces. While canonical interfaces have been exploited as target ...
DOI:
10.1016/j.ibmb.2016.10.010

14. Susceptibility of <em>Bemisia tabaci</em> MEAM1 (Hemiptera: Aleyrodidae) to Imidacloprid, Thiamethoxam, Dinotefuran and Flupyradifurone in South Florida

Author:
Smith, Hugh A.; Nagle, Curtis A.; MacVean, Charles A.; McKenzie, Cindy L.
Source:
Insects 2016 v.7 no.4
ISSN:
2075-4450
Subject:
acetylcholine,   etc   ; Bemisia tabaci; Gossypium; agonists; cotton; dinotefuran; imidacloprid; petioles; thiamethoxam; tomatoes; Florida;     Show all 11 Subjects
Abstract:
... Populations of Bemisa tabaci MEAM1 were established from nineteen locations in south Florida, primarily from commercial tomato fields, and were tested using a cotton leaf petiole systemic uptake method for susceptibility to the nicotinic acetylcholine agonist insecticides imidacloprid, thiamethoxam, dinotefuran and flupyradifurone. Eleven populations produced LC50s for one or more chemi ...
DOI:
10.3390/insects7040057

15. Activation and desensitization of peripheral muscle and neuronal nicotinic acetylcholine receptors by selected, naturally-occuring pyridine alkaloids

Author:
Green, Benedict T.; Lee, Stephen T.; Welch, Kevin D.; Cook, Daniel
Source:
Toxins 2016 v.8 no.7 pp. 204
ISSN:
2072-6651
Subject:
acetylcholine,   etc   ; agonists; anabasine; cholinergic receptors; fetus; muscles; neurons; nicotine; teratogenicity; teratogens; toxins;     Show all 11 Subjects
Abstract:
... Teratogenic alkaloids can cause developmental defects due to the inhibition of fetal movement that results from desensitization of fetal muscle-type nicotinic acetylcholine receptors (nAChRs). We investigated the ability of two known teratogens, the piperidinyl-pyridine anabasine and its 1,2-dehydropiperidinyl analog anabaseine, to activate and desensitize peripheral nAChRs expressed in TE-671 and ...
Handle:
10113/62924
DOI:
10.3390/toxins8070204
PubMed:
27384586
PubMed Central:
PMC4963837
CHORUS:
10.3390/toxins8070204

16. Anagyrine desensitization of peripheral nicotinic acetylcholine receptors. A potential biomarker of quinolizidine alkaloid teratogenesis in cattle

Author:
Green, Benedict T.; Lee, Stephen T.; Welch, Kevin D.; Cook, Daniel
Source:
Research in veterinary science 2017 v.115 pp. 195-200
ISSN:
0034-5288
Subject:
acetylcholine,   etc   ; Lupinus; agonists; biomarkers; blood serum; calves; cell culture; median effective concentration; membrane potential; metabolism; models; nicotinic receptors; piperidine alkaloids; sparteine; teratogenicity;     Show all 15 Subjects
Abstract:
... Anagyrine, a teratogenic quinolizidine alkaloid found in Lupinus spp., is proposed to undergo metabolism by pregnant cattle to a piperidine alkaloid which inhibits fetal movement, the putative mechanism behind crooked calf syndrome. The objective of this study was to test the hypothesis that anagyrine but not lupanine or sparteine can directly, without metabolism, desensitize nicotinic acetylcholi ...
DOI:
10.1016/j.rvsc.2017.04.019
Chorus Open Access:
10.1016/j.rvsc.2017.04.019

17. Heterologous formation of neonicotinoid-sensitive nAChRs containing UNC-38 and UNC-29 subunits from Bursaphelenchus xylophilus

Author:
Yu, Na; Liu, Yang; Wang, Xuan; Li, Jian; Bao, Haibo; Liu, Zewen
Source:
Pesticide biochemistry and physiology 2017 v.143 pp. 168-172
ISSN:
0048-3575
Subject:
acetylcholine,   etc   ; Bursaphelenchus xylophilus; Caenorhabditis elegans; Pinus; RNA; Xenopus; agonists; imidacloprid; invertebrates; median effective concentration; models; multigene family; nicotinic receptors; oocytes; pests; stoichiometry; vascular wilt;     Show all 17 Subjects
Abstract:
... Nicotinic acetylcholine receptor (nAChR) subunits are encoded by a large multigene family and generate a large number of pentameric receptors with various properties. At present, nematode species, such as Caenorhabditis elegans, have the largest number of nAChR subunits. In this study, two nAChR subunits (Bxy-Unc-38 and Bxy-Unc-29) were cloned from Bursaphelenchus xylophilus, a fatal nematode pest ...
DOI:
10.1016/j.pestbp.2017.08.001

18. Expression of muscarinic acetylcholine receptors in hepatocytes from rat fibrotic liver

Author:
Luo, Lin; Xu, Tingting; Wang, Pengbo; Mao, Liuliu; Xi, Chenghao; Huang, Jinhua; Zhang, Wei
Source:
Experimental and toxicologic pathology 2017 v.69 no.2 pp. 73-81
ISSN:
0940-2993
Subject:
acetylcholine,   etc   ; agonists; alanine transaminase; albumins; antagonists; atropine; carbon tetrachloride; chemokine CCL4; collagen; hepatocytes; hydroxyproline; liver; liver cirrhosis; muscarine receptors; nerve tissue; patients; pilocarpine; rats; survival rate; therapeutics;     Show all 20 Subjects
Abstract:
... The pathological changes of parasympathetic nerve are considered as an independent prognostic factor of the survival rate of patients with chronic liver disease. The non-selective muscarinic acetylcholine receptors (mAchR) agonists and antagonists can affect the proliferation of hepatocytes and hepatic stellate cells, but the subtypes of mAchR expressions in HCs are still uncertain. Here, we inves ...
DOI:
10.1016/j.etp.2016.11.005

19. Imidacloprid, a neonicotinoid insecticide, facilitates tyrosine hydroxylase transcription and phenylethanolamine N-methyltransferase mRNA expression to enhance catecholamine synthesis and its nicotine-evoked elevation in PC12D cells

Author:
Kawahata, Ichiro; Yamakuni, Tohru
Source:
Toxicology 2018 v.394 pp. 84-92
ISSN:
0300-483X
Subject:
acetylcholine,   etc   ; adrenal glands; agonists; biosynthesis; cAMP-dependent protein kinase; cell lines; chromaffin cells; epinephrine; gene expression; humans; hypertension; imidacloprid; insects; messenger RNA; neoplasms; nicotine; nicotinic receptors; patients; phenylethanolamine N-methyltransferase; physiological response; protein synthesis; rats; secretion; signal transduction; tachycardia; tyrosine 3-monooxygenase; vomiting;     Show all 27 Subjects
Abstract:
... Imidacloprid is a neonicotinoid insecticide acting as an agonist of nicotinic acetylcholine receptors (nAChRs) in the target insects. However, questions about the safety to mammals, including human have emerged. Overactivation of mammalian peripheral catecholaminergic systems leads to onset of tachycardia, hypertension, vomiting, etc., which have been observed in acutely imidacloprid-poisoned pati ...
DOI:
10.1016/j.tox.2017.12.004

20. The 5-HT4 receptor agonist prucalopride does not facilitate cholinergic neurotransmission in circular and longitudinal smooth muscle preparations of equine mid-jejunum

Author:
Lefebvre, Romain Adelin; Callens, Chana; Van Colen, Inge; Delesalle, Catherine John Ghislaine
Source:
Research in veterinary science 2017 v.114 pp. 153-162
ISSN:
0034-5288
Subject:
acetylcholine,   etc   ; adenosine triphosphate; agonists; atropine; clearcutting; cyclic AMP; death; electric field; electrodes; horses; in vitro studies; intestinal obstruction; jejunum; muscles; neurons; nitric oxide; platinum; receptors; second messengers; serotonin; smooth muscle;     Show all 21 Subjects
Abstract:
... Postoperative ileus (POI) remains an important cause of death in horses. The recently developed selective 5-HT4 receptor agonists such as prucalopride target 5-HT4 receptors on myenteric cholinergic neurons to enhance acetylcholine release and GI motility. No clearcut in vitro evaluation whether highly selective 5-HT4 receptor agonists enhance submaximal cholinergic neurotransmission towards the m ...
DOI:
10.1016/j.rvsc.2017.04.006