Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3...
Gαq after carbachol-induced activation by the M1 muscarinic receptor and found that at a saturating concentration of carbachol ... Characterization of M3 Receptor-Expressing CHO Cell Line. Specific [3H]NMS binding to muscarinic receptors in CHO-M3 membranes ... Competition between [3H]NMS and increasing concentrations of muscarinic agonists for muscarinic M3 receptors in CHO cell ... Regulation of phospholipase C-β1 by Gq and m1 muscarinic cholinergic receptor. Steady-state balance of receptor-mediated ...http://molpharm.aspetjournals.org/content/76/3/543.full
KAKEN - Research Projects | Receptor-mediated restoration of exocytotic capacity (KAKENHI-PROJECT-07672393)
1996, Research Category：Grant-in-Aid for Scientific Research (C), Section：一般, Research Field：Biological pharmacy ... M. K.: 'Carbachol-induced desensitization of rat basophilic leukemia (RBL-2H3) cells transfected with human m3 muscarinic ... Carbachol-induced desensitization of rat basophilic leukemia (RBL-2H3) cells transfected with human m3 muscarinic acetylcholine ... Exposure of RBL-m3 cells for 30 min to 100 muM carbachol in Ca^,2+,-free medium inhibited both secretion induce … More d by ...https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-07672393/
... of carbachol (CCh) (Auerbach and Segal, 1994). This muscarinic LTP (LTPm) is mediated by an M2 muscarinic receptor and is ... A non-NMDA receptor-mediated LTP can be induced in area CA1 of the hippocampus in the presence of the NMDA antagonist 2-APV by ... if the M3 muscarinic receptor, which mediates the muscarinic depression of the EPSP slope, and GABAergic inhibition are blocked ... does H2O2 affect the muscarinic receptor, a second messenger associated with this receptor, or some downstream process shared ...http://www.jneurosci.org/content/17/22/8695
Regulation of phospholipase D activity in neuroblastoma cells
Carbachol induced phospholipase D activity in SH-SY5Y cells. Muscarinic antagonists inhibited the response with potencies ... Muscarinic antagonists inhibited the response with potencies suggesting that muscarinic M1 receptors are responsible for the ... Carbachol induced phospholipase D activity in SH-SY5Y cells. Muscarinic antagonists inhibited the response with potencies ... Calmidazolium, Muscarinic receptors, Phosphatidylethanol, Phosphatidic acid, Phospholipase D, Signal transduction. in Journal ...https://lup.lub.lu.se/search/publication/1109867
Activation of Muscarinic Acetylcholine Receptors Enhances the Release of Endogenous Cannabinoids in the Hippocampus | Journal...
1999) Muscarinic facilitation of the occurrence of depolarization-induced suppression of inhibition in rat hippocampus. ... We found that low concentrations (0.2-0.5 μm) of carbachol (CCh) enhanced DSI without affecting basal evoked IPSCs (eIPSCs) by ... 1995) Muscarinic receptors modulate N-, P-, and L-type Ca2+ currents in rat striatal neurons through parallel pathways. J ... 2002) Muscarinic induction of hippocampal gamma oscillations requires coupling of the M1 receptor to two mixed cation currents. ...http://www.jneurosci.org/content/22/23/10182
Olanzapine - Wikipedia
I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods and ... "Inhibitory Effects of Antipsychotics on Carbachol-Enhanced Insulin Secretion from Perifused Rat Islets: Role of Muscarinic ... due to its high affinity for the D1 receptor over the D2 receptor. Antagonizing H1 histamine receptors causes sedation and may ... Antagonism of muscarinic acetylcholine receptors is associated with anticholinergic side effects such as dry mouth and ...https://en.wikipedia.org/wiki/Olanzapine
CiNii 論文 - Paeoniflorin, a Major Constituent of Peony Root, Reverses Muscarinic M 1-Receptor...
Paeoniflorin, a Major Constituent of Peony Root, Reverses Muscarinic M_1-Receptor Antagonist-Induced Suppression of Long-Term ... Involvement of M_2 receptor in an enhancement of long-term potentiation by carbachol in Schaffer collateral-CA1 synapses of ... induced spatial cognitive impairment in rats.In this study, we examined the effects of paeoniflorin and muscarinic receptor ... induced LTP suppression.These results suggest that paeoniflorin reversal of the muscarinic M,SUB,1,/SUB,−receptor−mediated ...http://ci.nii.ac.jp/naid/10008184273
Beta-Adrenoceptor-medicated down-regulation of M2 muscarinic receptors: role of cyclic adenosine 5'-monophosphate-dependent...
Procaterol-induced down-regulation of M2 receptors was fully blocked by N-[2-(methylamino)ethyl]-5'-isoquinoline-sulfonamide ... In control cells and those treated with procaterol for , / = 2 hr, cAMP generation was significantly inhibited by carbachol. ... Chronic (24 hr) treatment with 8-bromo-cAMP also had no effect on m2 muscarinic receptor mRNA, whereas forskolin caused a 50% ... In contrast, total muscarinic receptor number, measured with the lipophilic antagonist [3H]quinuclidinylbenzilate, decreased ...http://molpharm.aspetjournals.org/content/49/4/629
NICM | Dennis Chang
Chang D, Einstein R, 1999, Pacing-induced heart failure and muscarinic receptors. Journal of Molecular and Cellular Cardiology ... Reduced of carbachol-induced negative inotropic response in cardiac muscle from dogs with pacing-induced heart failure. ... Chang D, Einstein R, 1995, Decreased cardiac muscarinic receptor responsiveness in pacing-induced heart failure. Proceedings of ... Berberine alleviates ox-LDL induced inflammatory factors by up-regulation of autophagy via AMPK/mTOR signaling pathway. J ...http://nicm.edu.au/about_us/people/researchers/dennis_chang
Neurotransmitters of the suprachiasmatic nuclei
The effect is mediated by muscarinic receptors of the M1 subtype . Intraventricular administration of carbachol, which ... The master clock, as it is often called, is reset by light or photic stimuli  as well as by arousal-inducing or non-photic ... GABA receptors and receptor subunits are expressed in the SCN [116,139,140]. Although no variation in concentration of GABA in ... Use of the acetylcholine receptor agonist carbachol, a non-specific agonist, to mimic the effects of light  also added to ...https://www.jcircadianrhythms.com/articles/10.1186/1740-3391-4-2/print/
Antipsychotic-Induced Insulin Resistance and Postprandial Hormonal Dysregulation Independent of Weight Gain or Psychiatric...
Olanzapine has been shown to be a high-affinity muscarinic receptor antagonist (40) and in vitro can block acetylcholine ... Inhibitory effects of antipsychotics on carbachol-enhanced insulin secretion from perifused rat islets: role of muscarinic ... Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry 2008;13:27-35 ... Atypical antipsychotics and effects of muscarinic, serotonergic, dopaminergic and histaminergic receptor binding on insulin ...http://diabetes.diabetesjournals.org/content/62/9/3232
Store-operated influx of Ca2+ in pancreatic β-cells exhibits graded dependence on the filling of the endoplasmic reticulum |...
0.3-100 μM carbachol was introduced as shown by the lower bars. B shows the dose-response relationship for carbachol-induced ... Evidence for an opposing effect of muscarinic receptor activation. Biochem. J. 233, 865-870. ... In addition, the carbachol- and CPA-induced influx of Mn2+ depended on store filling in a graded manner. The store-operated ... 2B shows the dose-response relationship for carbachol-induced elevation of [Ca2+]i in the presence of 10 mM Ca2+. Half-maximal ...http://jcs.biologists.org/content/114/11/2179
Differential Contribution of Angiotensinergic and Cholinergic Receptors in the Hypothalamic Paraventricular Nucleus to...
Effect of periventricular muscarinic or nicotinic receptor blockade on i.c.v. hyperosmolar saline-induced AVP release.. ... such as carbachol and ACh, act centrally to stimulate AVP release viamuscarinic rather than nicotinic receptors (Bhargava et al ... muscarinic receptors are facilitatory and nicotinic receptors inhibitory in nature. The inhibitory and stimulatory receptors ... Effect of blockade of cholinergic (muscarinic and nicotinic) receptors in the PVN on i.c.v. hyperosmolar saline-induced AVP ...http://jpet.aspetjournals.org/content/285/3/1012
A Neurochemical Perspective on States of Consciousness | SpringerLink
Muscarinic-2 and orexin-2 receptors on GABAergic and other neurons in the rat mesopontine tegmentum and their potential role in ... The carbachol-induced enhancement of desynchronized sleep signs is dose dependent and antagonized by centrally administered ... Muscarinic acetylcholine receptors. Curr Pharm Des 12:3573-3581.PubMedGoogle Scholar ... M2 muscarinic receptors in pontine reticular formation of C57BL/6 J mouse contribute to rapid eye movement sleep generation. ...https://link.springer.com/chapter/10.1007/978-1-60761-462-3_3
Cholinergic Stimulation of Amylase Secretion from Pancreatic Acinar Cells Studied with Muscarinic Acetylcholine Receptor Mutant...
... carbachol-induced amylase secretion is abolished in acinar preparations from M1/M3 receptor double KO mice. B, bombesin-induced ... Evaluation of muscarinic agonist-induced analgesia in muscarinic acetylcholine receptor knockout mice. Mol Pharmacol 62: 1084- ... Carbachol-Induced Amylase Secretion from Dispersed Pancreatic Acini Prepared from WT and M1 and M3 Receptor Single KO Mice. To ... Carbachol-Induced Pancreatic Amylase Secretion Is Abolished in M1/M3 Receptor Double KO Mice. To examine whether the activation ...http://jpet.aspetjournals.org/content/313/3/995
Inhibitory effect of amiodarone on the muscarinic acetylcholine receptor-operated potassium current in guinea pig atrial cells....
Amiodarone also reversed the carbachol- and adenosine-induced action potential shortening in a concentration-dependent manner. ... However, effects of amiodarone on the muscarinic acetylcholine receptor-operated K+ current (IK.ACh), which plays an important ... Inhibitory effect of amiodarone on the muscarinic acetylcholine receptor-operated potassium current in guinea pig atrial cells. ... Inhibitory effect of amiodarone on the muscarinic acetylcholine receptor-operated potassium current in guinea pig atrial cells. ...http://jpet.aspetjournals.org/content/279/2/617
Positive Inotropy Mediated by Diacylglycerol in Rat Ventricular Myocytes | Circulation Research
Other agonists, including adenosine,13 14 acetylcholine (muscarinic),13 15 and angiotensin II (in some species)16 17 cause PI ... Mechanisms for cardiac depression induced by phorbol myristate acetate in working rat hearts. Br J Pharmacol.. 1990;100:826-830 ... κ and δ opioid receptor stimulation affects cardiac myocyte function and Ca2+ release from an intracellular pool in myocytes ... Kohl C, Linck B, Schmitz W, Scholz H, Scholz J, Mathias T. Effects of carbachol and (−)-N6-phenylisopropyladenosine on ...http://circres.ahajournals.org/content/81/1/92
Canine Cardiac Muscarinic Receptors, G Proteins, and Adenylate Cyclase after Long-Term Morphine | Journal of Pharmacology and...
1985) Carbachol induces desensitization of cardiac β-adrenergic receptors through muscarinic M1 receptors. Biochem Biophys Res ... Muscarinic Receptors.. The density and equilibrium dissociation constant (KD) of muscarinic receptors in left ventricular and ... for the antagonist and maximal muscarinic receptor binding (Bmax). Because there are few, if any, m1 muscarinic receptors in ... 1979) Muscarinic acetylcholine receptor regulation by accelerated rate of receptor loss. Biochem Biophys Res Commun 90:506-512. ...http://jpet.aspetjournals.org/content/291/2/725
Table of Contents - October 01, 1996, 50 (4) | Molecular Pharmacology
m3 Muscarinic receptor-induced and Gi-mediated heterologous potentiation of phospholipase C stimulation: role of ... Pituitary adenylate cyclase-activating peptide, carbachol, and glucose stimulate insulin release in the absence of an increase ... Inhibition by toxin B of inositol phosphate formation induced by G protein-coupled and tyrosine kinase receptors in N1E-115 ... Opioid mu, delta, and kappa receptor-induced activation of phospholipase C-beta 3 and inhibition of adenylyl cyclase is ...http://molpharm.aspetjournals.org/content/50/4
Responses of Sodium-Hydrogen Exchange to Nitric Oxide in Porcine Cultured Nonpigmented Ciliary Epithelium | IOVS | ARVO Journals
Orman B Reina S Borda E Sterin-Borda L . Signal transduction underlying carbachol-induced PGE2 generation and cox-1 mRNA ... Correlations between neuronal nitric oxide synthase and muscarinic M3/M1 receptors in the rat retina. Exp Eye Res. 2005;80:391- ... SNP-induced inhibition of pHi recovery was suppressed to a similar degree by ODQ, an inhibitor of soluble guanylate cyclase, ... SNP causes inhibition of the rate of pHi recovery from an ammonium chloride-induced acid load. SNP is an NO donor and the ...http://iovs.arvojournals.org/article.aspx?articleid=2185406
Development of the sympatho-vagal balance in the cardiovascular system in zebrafish (Danio rerio) characterized by power...
They pharmacologically analyzed the role of this receptor and observed a response to carbachol at 3 d.p.f. Carbachol, at a high ... Hsieh, D. J. and Liao, C. F. (2002). Zebrafish M2 muscarinic acetylcholine receptor: cloning, pharmacological characterization ... In contrast, atropine application induced a significant decrease in frequency bandwidth between 13 and 15 d.p.f. (0.375 Hz and ... 2A). We therefore conclude that functional cholinergic receptors are present at 5 d.p.f., but adrenergic receptors become ...http://jeb.biologists.org/content/209/6/1093
Pharmacological Assessment of M1 Muscarinic Acetylcholine Receptor-Gq/11 Protein Coupling in Membranes Prepared from Postmortem...
... of the oxotremorine-M-induced response, respectively. These data indicate that the M1 receptor is the predominant mAChR subtype ... rat brain membranes has previously been shown to have no significant effect on the affinity state of the M1 mAChR for carbachol ... 1994) Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors. J Pharmacol Exp Ther 269: ... Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using ...http://jpet.aspetjournals.org/content/325/3/869
... when exposed to group I metabotropic glutamate receptor agonists, or when exposed to muscarinic cholinergic receptor agonists. ... Responses of GIN cells to stimulation of cholinergic receptors. We also applied two cholinergic agonists, carbachol (1-20 μM) ... Werk CM, Chapman CA. Long-term potentiation of polysynaptic responses in layer V of the sensorimotor cortex induced by theta- ... receptors; APV (50 μM), to block N-methyl-d-aspartate (NMDA) receptors; PTX (20 μM), to block γ-aminobutyric acid type A (GABAA ...http://jn.physiology.org/content/100/5/2640
The High-Fat Diet-Fed Mouse | Diabetes
Dissociated insulinotropic sensitivity to glucose and carbachol in high-fat diet-induced insulin resistance in C57BL/6J mice. ... Evidence that the diabetes gene encodes the leptin receptor: identification of a mutation in the leptin receptor gene in db/db ... Ahrén B, Sundkvist G, Mulder H, Sundler F: Blockade of muscarinic transmission increases the frequency of diabetes after low- ... Surwit RS, Kuhn CM, Cochrane C, McCubbin JA, Feinglos MN: Diet-induced type II diabetes in C57BL/6J mice. Diabetes37 :1163 - ...http://diabetes.diabetesjournals.org/content/53/suppl_3/S215.full?cited-by=yes&legid=diabetes
Role of IL-4, IL-13, and STAT6 in inflammation-induced hypercontractility of murine smooth muscle cells | Gastrointestinal and...
These observations suggest that the increased affinity of the muscarinic receptor for Carbachol on murine muscle cells is ... Inflammation-induced changes in muscarinic receptors have also been reported in the airways. Fryer et al. (17) reported that in ... These neuronal M2 receptors inhibit acetylcholine release. Thus the reduced expression of these receptors induces ... increase the affinity of the muscarinic receptor through STAT6 dependent and independent pathways, and 3) to induce hypertrophy ...http://ajpgi.physiology.org/content/282/2/G226
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