• secretion
  • free medium inhibited both secretion induce … More d by subsequent addition of carbachol and by cross-linking FcepsilonRI.RBL-m3 cells were desensitized without any modification of m3 mAChR or functional uncoupling between the receptor and phospholipase C.Our novel finding was that the heterologous desensitization of RBL-m3 cells occurred at the steps distal to the rise in concentration of intracellular calcium. (nii.ac.jp)
  • These findings indicate that carbachol-induced heterologous as well as homologous desensitization of secretion involves negative regulation of the signaling pathway leading to membrane ruffling. (nii.ac.jp)
  • We hypothesized that meal ingestion that elicits both neural and incretin-mediated hormonal responses would be more likely to reveal olanzapine-induced changes in meal-related metabolism compared with the traditional measurements used to assess insulin secretion and sensitivity, which involve intravenous glucose administration and bypass activation of the brain-gut-pancreas axis. (diabetesjournals.org)
  • However, another pancreatic secretagogue, bombesin, retained its ability to fully stimulate amylase secretion in acinar preparations from M 1 /M 3 receptor double KO mice. (aspetjournals.org)
  • These receptors are highly expressed on pancreatic beta cells and are critical regulators of glucose homoestasis by modulating insulin secretion. (wikipedia.org)
  • The muscarinic M3 receptor regulates insulin secretion from the pancreas and are an important target for understanding the mechanisms of type 2 diabetes mellitus. (wikipedia.org)
  • The M3 receptors are also located in many glands, both endocrine and exocrine glands, and help to stimulate secretion in salivary glands and other glands of the body. (wikipedia.org)
  • 1994
  • We have discovered recently a gradually developing, long-lasting potentiation induced by exposure of a hippocampal slice to a low concentration (0.5 μ m ) of carbachol (CCh) ( Auerbach and Segal, 1994 ). (jneurosci.org)
  • angiotensin
  • In the first set of experiments, periventricular angiotensin AT1, muscarinic or nicotinic receptors were blocked by i.c.v. administration of losartan (10 nmol), atropine (100 nmol) or hexamethonium (100 nmol), respectively, before i.c.v. hyperosmolar saline injections. (aspetjournals.org)
  • Blood-borne signals such as plasma hypernatremia and an increase in ANG II act on osmo/sodium or angiotensin receptors found in CVOs, such as the SFO and the OVLT, that are known to be involved in osmoregulation. (aspetjournals.org)
  • olanzapine
  • Olanzapine is believed to work by blocking, or antagonizing, the dopamine D2 receptor that is an action it shares with most antipsychotics. (wikipedia.org)
  • Like most other atypical antipsychotics, olanzapine also strongly antagonizes the 5-HT2A receptor, which may partially underpin its reduced propensity for causing movement disorders. (wikipedia.org)
  • whereas
  • The protein kinase C inhibitors, bisindolylmaleimide and staurosporine significantly inhibited the carbachol-induced Peth formation whereas H7 had no effect. (lu.se)
  • Chronic (24 hr) treatment with 8-bromo-cAMP also had no effect on m2 muscarinic receptor mRNA, whereas forskolin caused a 50% reduction in the steady state levels of m2 mRNA that could be only partially blocked by the cAMP-dependent protein kinase inhibitor H-8 and the protein kinase C inhibitor GF 109203X. (aspetjournals.org)
  • The two lower saline concentrations did not affect arterial blood pressure (non-pressure-associated AVP release), whereas 0.6 M saline induced increase in blood pressure (pressure-associated AVP release). (aspetjournals.org)
  • The 0.3 M saline-induced AVP release was blocked by atropine and hexamethonium, whereas the 0.6 M saline-induced AVP release was blocked by atropine only. (aspetjournals.org)
  • We conclude that afferents arising from periventricular osmosensitive neurons to the hypothalamic paraventricular nucleus, which are involved in non-pressure-associated osmotically induced AVP release, are both angiotensinergic and cholinergic, whereas those mediating pressure-associated AVP release are cholinergic in nature. (aspetjournals.org)
  • affinity
  • A full spectrum of efficacy can be established between these two extremes, governed by the differential in affinity for the two receptor states. (aspetjournals.org)
  • Contrary to expectations, morphine increased muscarinic receptor density in the right atrium and left ventricle by 17 and 34%, respectively, with no change in the apparent affinity of the receptor ( K D ). Morphine also increased the expression of the G protein G i α by 115 and 233%, respectively, in right atrial and left ventricular sarcolemmal membranes. (aspetjournals.org)
  • mRNA
  • Northern blot analysis showed a small and transient increase in m2-receptor mRNA levels up to 2 hr but no long term (24 hr) effect. (aspetjournals.org)
  • adrenergic
  • Adrenergic Systems in the Antagonizing Effect of Paeoniflorin on the Scopolamine-Induced Deficiti n Radial Maze Performance in Rats. (nii.ac.jp)
  • Thus, the complex interplay that can occur among opposing muscarinic, opioid, and adrenergic systems and their common second messengers provides multiple opportunities for altered autonomic function during long-term opiate administration. (aspetjournals.org)
  • atropine
  • Single KACh channel current was also recorded by use of a pipette solution containing carbachol (1 microM) or atropine (10 microM) plus theophylline (100 microM) in a cell-attached configuration. (aspetjournals.org)
  • EPSP
  • This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in exocrine glands and in the CNS. (wikipedia.org)
  • protein
  • Although there are several empirical approaches that enable the comparison of relative agonist efficacy, the molecular basis that underlies differences in the ability of G protein-coupled receptor agonists to elicit a response is still largely unexplained. (aspetjournals.org)
  • Several models have been described that incorporate the kinetics of receptor-mediated initiation of the G protein cycle, but these have not directly addressed the influence of agonist-binding kinetics. (aspetjournals.org)
  • In permeabilized SH-SY5Y cells, both the carbachol- and GTP gamma S-induced Peth formation was inhibited by GDP beta S, indicating that both responses are mediated via a G-protein. (lu.se)
  • The data provide evidence that diacylglycerol can induce a strong positive inotropic effect in mammalian ventricular muscle, possibly by activating protein kinase C. By contrast, perfusion of diC 8 extracellularly onto myocytes caused a 42±2% decline in twitch amplitude, in accordance with previous reports. (ahajournals.org)
  • Agonist binding and protein kinase C activation stimulate phosphorylation of the gastrin-releasing peptide receptor at distinct sites. (aspetjournals.org)
  • The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the CHRM4 gene. (wikipedia.org)
  • 1995
  • This potential model for narcotic tolerance was developed further by Sadee and Wang (1995) , who provided evidence that μ receptors assume constitutive activity during continuous exposure to morphine and no longer require agonist for signal transduction. (aspetjournals.org)
  • inhibitor
  • Blockade of DNA synthesis induced by platelet-derived growth factor by tranilast, an inhibitor of calcium entry, in vascular smooth muscle cells. (aspetjournals.org)
  • intracellular calcium
  • Because the M3 receptor is Gq-coupled and mediates an increase in intracellular calcium, it typically causes constriction of smooth muscle, such as that observed during bronchoconstriction. (wikipedia.org)
  • Identification
  • Ligand-binding characteristics and related structural features of the expressed goldfish kainate receptors: identification of a conserved disulfide bond and three residues important for ligand binding. (aspetjournals.org)
  • Identification, molecular cloning, and distribution of a short variant of the 5-hydroxytryptamine2C receptor produced by alternative splicing. (aspetjournals.org)
  • behaviors
  • Vagally-induced bronchoconstriction Mediating olfactory behaviors (e.g. aggression, mating) A structural homolog of M1 receptor is expressed in unicellular eukaryotes, such as Acanthamoeba castellanii. (wikipedia.org)
  • evidence
  • Despite accumulating evidence of AAP-induced metabolic impairments, there remain unresolved issues as to whether metabolic disease is part of the natural history of schizophrenia and bipolar illness or if the metabolic impairments are only secondary to weight gain. (diabetesjournals.org)
  • efficacy
  • To test this, we investigated the relationship between the efficacy of seven M 3 muscarinic receptor agonists and their rate of dissociation ( k off ) from the M 3 receptor. (aspetjournals.org)
  • When efficacy was compared with the dissociation rate constant, however, the two were highly correlated, suggesting a relationship between the duration of agonist binding at the receptor and the intrinsic efficacy. (aspetjournals.org)
  • Efficacy is defined as the ability of a ligand to elicit a response upon binding to a receptor ( Stephenson, 1956 ) and is arguably the most important parameter for optimization in novel agonist drugs. (aspetjournals.org)
  • Since then, however, models have been developed that describe efficacy in terms of the ability to stabilize an active receptor conformation. (aspetjournals.org)