• They show that treating cultured mouse neurons expressing human APP with the acetylcholine receptor agonist carbachol increased the production of α-secretase cleavage products, but no such effect occurred in cells from M1 knockout mice. (alzforum.org)
  • The glutamate receptor agonist kainic acid [21] and the cholinergic agonist pilocarpine [22] are commonly used in SE models. (jle.com)
  • Although nicotine is an agonist of ionotropic acetylcholine receptors, we found that nicotine-induced polyspermy was neither mimicked by acetylcholine and carbachol nor inhibited by specific antagonists of nicotinic acetylcholine receptors. (mdpi.com)
  • Selective breeding for diisopropyl fluorophosphatesensitivity: Behavioural effects of cholinergic agonists and antagonists. (bvsalud.org)
  • The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. (pharmacycode.com)
  • Pilocarpine is used in the treatment of Xerostomia and belongs to the drug class cholinergic agonists . (drugs.com)
  • In the form of pilocarpine, muscarinic receptor agonists have been used medically for a short time. (wikipedia.org)
  • Beta-agonists, corticosteroids, and theophylline are mainstays in the treatment of status asthmaticus. (medscape.com)
  • It is interesting to note that, except for anticonvulsants, benzodiazepine receptor agonists, and corticosteroids, most drugs can be safely tapered over a 4-to-6-week period. (cdc.gov)
  • Cevimeline is a cholinergic agonist which binds to muscarinic receptors. (nih.gov)
  • Activation of muscarinic acetylcholine receptors is known to steer APP down the non-amyloidogenic, α-secretase pathway, but it has been difficult to pin the effect on a specific receptor subtype: There are five different muscarinic receptors (M1-M5) and knowing which one is involved is critical for making selective drugs and minimizing cholinergic side effects. (alzforum.org)
  • In Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. (wikipedia.org)
  • Initial focus has been the class of cholinergic receptors. (europa.eu)
  • It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. (bvsalud.org)
  • We used whole-cell patch-clamp recordings in in vitro rat brain slices to investigate the effect of adenosine on identified cholinergic and noncholinergic neurons of the magnocellular preoptic nucleus and substantia innominata. (nih.gov)
  • These results demonstrate that, in the magnocellular preoptic nucleus and substantia innominata region of the basal forebrain, adenosine inhibits both cholinergic neurons and a subset of noncholinergic neurons. (nih.gov)
  • To test this hypothesis, rats were given bilateral IgG-192-saporin injections, which predominantly targets cholinergic BF neurons. (sri.com)
  • Nine alkaloids constitute the active ingredients of betel nut ( Reference Farnworth Farnworth, 1976 ), the most abundant of which is arecoline - a potent muscarinic agonist that rapidly crosses the blood-brain barrier and induces a range of parasympathetic effects ( Reference Asthana, Greig and Holloway Asthana et al , 1996 ). (cambridge.org)
  • Unlike non-specific nicotinic agonists, GTS inhibited serum protein TNF levels in both normal and splenectomized, haemorrhagic animals. (utmb.edu)
  • Our studies suggest that GTS provides significant advantages as compared with non-specific nicotinic agonists, and it could be a promising anti-inflammatory supplement to improve survival during resuscitation. (utmb.edu)
  • It will also help determine whether nicotine and/or nicotinic agonists are of benefit in the treatment of dyskinesias that occur with levodopa treatment for Parkinson's disease. (michaeljfox.org)
  • Evoxac (cevimeline hydrochloride) is a cholinergic agonist that works by stimulating certain nerves to increase the amount of saliva produced used to treat dry mouth in people with Sjogren's Syndrome. (rxlist.com)
  • The proposed studies represent a new research direction for the treatment of levodopa-induced dyskinesias using nicotine or nicotinic receptor agonists. (michaeljfox.org)
  • The agonist ligand nicotine shows an up to 30-fold higher affinity to nACHRs than acetylcholine (ACh). (weeksmd.com)
  • Studies in the presence of l-NAME confirmed the effect of the ghrelin agonists on cholinergic excitatory motor responses. (wikigenes.org)
  • Experimentally, SE can be induced by acute systemic exposure to epileptogenic agents, including drugs that block GABAergic inhibition or facilitate glutamatergic or cholinergic excitatory transmission. (jle.com)
  • A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. (wikipedia.org)
  • Muscarine Muscarinic acetylcholine receptor Muscarinic antagonist Nicotinic acetylcholine receptor Nicotinic agonist Nicotinic antagonist Fisher A, Brandeis R, Bar-Ner RH, Kliger-Spatz M, Natan N, Sonego H, Marcovitch I, Pittel Z (2002). (wikipedia.org)
  • Alpha 7 nicotinic acetylcholine receptor (α7nAChR) agonists have been developed to treat schizophrenia but failed in clinical trials due to rapid desensitization. (bvsalud.org)
  • Their work, published in the March 24 Journal of Neuroscience, offers support for the ongoing development of M1-selective agonists as modulators of amyloid load. (alzforum.org)
  • Prodrug metabolized to desglymidodrine, a selective alpha1-adrenoreceptor agonist. (medscape.com)
  • To demonstrate the test battery, the acute effects of mecamylamine and the reversal of these effects by two agonist drugs are described. (jove.com)
  • I have shown that cholinergic agonists induce a tolerant phenotype in innate immune cells, and increase microbe and particle uptake, whilst reducing inflammatory responses. (europa.eu)
  • Hyperthyroidism: Choline esters (muscarinic agonists) can induce atrial fibrillation in hyperthyroid patients. (pharmacology2000.com)
  • Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts. (nih.gov)
  • Peptic ulcer: Choline esters (muscarinic agonists), by increasing gastric acid secretion, may exacerbate ulcer symptoms. (pharmacology2000.com)
  • BFx and intact rats were then given oral ALM, the benzodiazepine agonist zolpidem (ZOL) or vehicle (VEH) at lights-out. (sri.com)
  • Here, we report that the alpha7nAChR-agonist, GTS, restrains systemic inflammation and improves survival during resuscitation. (utmb.edu)
  • GAT107, a type 2 allosteric agonist-positive allosteric modulator (ago-PAM) to the α7 nAChR was designed to activate the α7 nAChR while reducing desensitization. (bvsalud.org)
  • We therefore propose to test the effect of nAChR agonists that preferentially stimulate brain nAChRs and not those in the peripheral nervous system. (michaeljfox.org)
  • Dr. Quik found that the targeted nAChR agonist varenicline resulted in significant declines in levodopa-induced AIMs at a relatively low dose of the agonist, with no worsening of parkinsonism. (michaeljfox.org)
  • The nAChR is the principal structure of cholinergic neuromodulation and is responsible for coordinated neuronal network interaction. (weeksmd.com)
  • We therefore hypothesize that this molecule could displace the virus from nAChR attachment and pave the way for unimpaired cholinergic signal transmission. (weeksmd.com)
  • Adenosine (0.5-100 microM) reduced the magnocellular preoptic nucleus and substantia innominata cholinergic neuronal firing rate by activating an inwardly rectifying potassium current that reversed at -82 mV and was blocked by barium (100 microM). (nih.gov)
  • Only the GABAergic marker was affected after the single treatment, whereas the GABAergic, cholinergic and astrocytic markers were decreased after the repeated treatments. (unige.ch)
  • Pretreatment with CP-99994, a neurokinin type 1 receptor antagonist, partially abolished the O(3)-induced reactivity to cholinergic agonists and electrical field stimulation. (cdc.gov)
  • At a cellular level it is found that cholinergic agonists generally negatively influence the immune response to pathogens. (europa.eu)
  • Dose-dependent effects of GAT107, a novel allosteric agonist-positive allosteric modulator (ago-PAM) for the α7 nicotinic cholinergic receptor: a BOLD phMRI and connectivity study on awake rats. (bvsalud.org)
  • Coronary vascular disease: Choline esters (muscarinic agonists), as a result of their hypotensive effects, can further compromise coronary blood flow. (pharmacology2000.com)
  • Selectivity is important on both counts: Non-specific muscarinic receptor agonists can produce side effects due to peripheral cholinergic effects including gastrointestinal disturbances, changes in blood pressure, and excessive sweating. (alzforum.org)
  • Reactivity of isolated tracheal smooth muscle to cholinergic agonists was significantly increased after O(3) exposure, as were contractions to electrical field stimulation at 10 Hz. (cdc.gov)
  • A synergistic effect may be expected with concomitant administration of succinylcholine, similar neuromuscular blocking agents, or cholinergic agonists ( 7.2 ). (nih.gov)
  • Finally, the activation of opioidergic and cholinergic systems appears to play a crucial role in (-)-linalool-induced antinociception. (researchgate.net)
  • Smooth muscle relaxing effect distal to cholinergic receptor site. (medscape.com)
  • Cholinergic agonists are used in patients with detrusor areflexia. (medscape.com)
  • Expression profiling in mouse and human macrophages has indicated that cholinergic receptor expression varies amongst species. (europa.eu)
  • Hypokalemia may result from either corticosteroid use or beta-agonist use. (medscape.com)
  • We anticipate that these studies will increase our basic understanding of the role of the nigrostriatal nicotinic cholinergic system in the development of levodopa-induced dyskinesias. (michaeljfox.org)
  • Under normal conditions, the ghrelin agonists reduced the on-relaxations in fundic strips and increased the cholinergic off-contractions in antral and fundic strips. (wikigenes.org)
  • The results suggest that an M1-specific agonist could be doubly beneficial in AD by making up for the loss of acetylcholine and by decreasing Aβ production. (alzforum.org)