AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and ProcessesDisciplines and OccupationsAnthropology, Education, Sociology and Social PhenomenaTechnology, Industry, AgricultureHealth Care
Scopolamine HydrobromideReceptors, MuscarinicMuscarinic AntagonistsMuscarinic AgonistsReceptor, Muscarinic M3Receptor, Muscarinic M1PharmacologyN-MethylscopolaminePharmacology, ClinicalReceptor, Muscarinic M4ParasympatholyticsCarbacholScopolamine DerivativesCholinergic AntagonistsAtropineParasympathomimeticsAcetylcholineCholinergic AgentsCholinergic AgonistsButylscopolammonium BromidePhysostigmineDiaminesMuscarineCholinesterase InhibitorsCholinergic FibersDose-Response Relationship, DrugTacrineGallamine TriethiodideSialorrheaAdministration, CutaneousAvoidance LearningMecamylaminePilocarpineArecolineParasympathetic Nervous SystemRadioligand AssayMaze LearningOxotremorinePiperidinesAtropa belladonnaBethanecholMemoryAmnesiaReceptors, CholinergicDaturaGuinea PigsTropanesMotion SicknessMuscle, SmoothRats, Sprague-DawleyNicotinic AntagonistsPirenzepinePropylbenzilylcholine MustardDrug InteractionsSolanaceous AlkaloidsBenzilatesMemory DisordersRats, WistarBehavior, AnimalSerotonin AntagonistsDiagonal Band of BrocaMethacholine CompoundsAdjuvants, AnesthesiaQuinuclidinesElectric StimulationReceptors, NicotinicBrainHippocampusLorazepamCholine O-AcetyltransferaseDicyclomineCHO CellsMotor ActivityHaloperidolReceptors, SerotoninThiadiazolesGTP-Binding ProteinsBethanechol CompoundsBiperidenNeuronsIleumCalciumDopamine AntagonistsLearning DisordersCassiaNootropic AgentsRats, Inbred StrainsReceptors, Serotonin, 5-HT1Muscle ContractionRats, Long-EvansVagus NerveNicotineApomorphineAcetylcholinesteraseTime FactorsBinding, CompetitiveCricetinaeAlkaloidsSynaptic TransmissionIndans
ReceptorsAntagonistAntagonistsAnti-muscarinicAtropine and scopolamineTropanePirenzepineAgonistReceptor subtypesAnticholinergicRatsAntimuscarinicDrugsAmnesiaPretreatmentAntidoteExertEffectsCompoundsMiceAntidepressantDecreaseClinicalPilocarpineGenesDoseMolecularMemoryChapterIrisAdministrationCentralGroupBrain
Receptors23
  • Muscarinic receptors responding to the natural ligand acetylcholine have a widespread tissue distribution and are involved in the control of numerous central and peripheral physiological responses, as well as being a major drug target in human disease. (guidetopharmacology.org)
  • Hence, M2 and M4-muscarinic receptors are able to couple to the pertusiss-toxin sensitive G i/o -proteins, and M 1 , M 3 and M 5 -muscarinic receptors couple to G q/11 -proteins [ 9 , 34 ]. (guidetopharmacology.org)
  • By targeting allosteric sites of muscarinic receptors, contained on the extracellular loops and extracellular regions of the transmembrane helices [ 24 ], allosteric modulators are able to regulate the binding affinity of ligands at the orthosteric site. (guidetopharmacology.org)
  • Co-expressed with the M 3 -muscarinic receptors in smooth muscle is an often larger population of M 2 -muscarinic receptors [ 11 ] which appear to play a much smaller role in the smooth muscle contractile response [ 35 ]. (guidetopharmacology.org)
  • Muscarinic blockers block the muscarinic receptors. (howmed.net)
  • Antimuscarinic drugs block the muscarinic receptors, which can be reversed by increasing the concentration of muscarinic agonist. (howmed.net)
  • Atropine is a competitive antagonist of acetyl choline and other muscarinic agonists on muscarinic receptors, it selectively reduce s or abolishes the muscarinic effects of acetyl choline. (howmed.net)
  • All muscarinic acetylcholine receptors are G-protein coupled receptors present at various locations such as CNS, heart, many smooth muscles and exocrine glands. (egpat.com)
  • The muscarinic receptor antagonists atropine, scopolamine and PZ inhibited the binding of [3H]QNB and [3H]PZ to solubilized receptors with Hill slopes of 1, as did the muscarinic receptor agonist oxotremorine. (unboundmedicine.com)
  • Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. (lookformedical.com)
  • Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. (lookformedical.com)
  • Drugs interfering with Muscarinic Acetylcholine Receptors and Their effects on Place Navigation. (cas.cz)
  • The pharmacology of tacrine at N-methyl-D-aspartate receptors. (cas.cz)
  • The altered state of consciousness produced by common or 'classical' deliriant substances such as scopolamine , atropine and diphenhydramine is primarily mediated through the drug compounds' competitive antagonism of the peripheral and central muscarinic acetylcholine receptors . (wikipedia.org)
  • [6] Peripheral muscarinic receptors are part of the autonomic nervous system . (wikipedia.org)
  • The stereotypy mediated by the postsynaptic dopaminergic system, but not the yawning mediated by the presynaptic system, may be altered by chronic treatment with physostigmine, while long-term treatment with scopolamine seems to produce a supersensitivity to cholinergic receptors. (baillement.com)
  • Physostigmine, an anticholinesterase agent, and pilocarpine, a cholinergic agonist predominantly acting upon muscarinic receptors, have been reported to elicit yawning in infant rats (Urbá-Holmgren et al. (baillement.com)
  • Cyclopentolate blocks the receptors in the muscles of the eye (muscarinic receptors). (medicatione.com)
  • A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. (nih.gov)
  • Like other transmembrane receptors , acetylcholine receptors are classified according to their "pharmacology", or according to their relative affinities and sensitivities to different molecules. (wikidoc.org)
  • muscarinic acetylcholine receptors ( mAChR , also known as " metabotropic " acetylcholine receptors) are particularly responsive to muscarine . (wikidoc.org)
  • Molecular biology has shown that the nicotinic and muscarinic receptors belong to distinct protein superfamilies . (wikidoc.org)
  • Muscarinic acetylcholine receptors can be blocked by the drugs atropine and scopolamine . (wikidoc.org)
Antagonist6
  • Anisodine acts as a muscarinic acetylcholine receptor antagonist and α1-adrenergic receptor antagonist. (wikipedia.org)
  • In the case of pirenzepine, for example, this antagonist has a 44-fold selectivity for the M 1 -muscarinic receptor over the M 2 , but only a 17.9 and 3.5 fold selectivity for the M 3 and M 4 -muscarinic receptor subtypes respectively [ 9 ]. (guidetopharmacology.org)
  • Atropine is a muscarinic antagonist indicated for temporary blockade of severe or life threatening muscarinic effects. (nih.gov)
  • In addition, intraperitoneally administered Colivelin suppresses memory impairment caused by a muscarinic acetylcholine receptor antagonist, 3-quinuclidinyl benzilate, indicating that a substantial portion of intraperitoneally administered Colivelin passes through the blood-brain barrier and suppresses functional memory deficit. (jneurosci.org)
  • [6] Scopolamine is a nonspecific muscarinic antagonist at all four ( M 1 , M 2 , M 3 , and M 4 ) receptor sites. (wikipedia.org)
  • We also assessed the interactive effects of castration and scopolamine, a muscarinic receptor antagonist, as well as mecamylamine, a nicotinic receptor antagonist, on behavior. (lsu.edu)
Antagonists6
  • The orthosteric binding pocket of the muscarinic receptor family is highly conserved, making the development of subtype-specific agonists and antagonists very difficult. (guidetopharmacology.org)
  • Also known as muscarinic receptor antagonists . (howmed.net)
  • Together, these data suggest that muscarinic receptor sites solubilized from rat brain retain their abilities to interact selectively with muscarinic receptor agonists and antagonists. (unboundmedicine.com)
  • Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system. (lookformedical.com)
  • The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS. (lookformedical.com)
  • 4. Pretreatment (30 min) with the non-selective muscarinic antagonists scopolamine (0.1, 0.3 or 1 mg kg(-1), i.p.) and atropine (0.3, 1 or 3 mg kg(-1), s.c.) but not methylatropine (1, 3 or 10 mg kg(-1), s.c) significantly inhibited stretching induced by Ro 04-6790 (30 mg kg(-1), i.p.). 5. (lookformedical.com)
Anti-muscarinic2
Atropine and scopolamine1
  • Included in these naturally occurring substances are DMT, psilocybin and psilocin, mescaline, salvinorin A, lysergic acid amide (LSA), and atropine and scopolamine. (medscape.com)
Tropane1
Pirenzepine1
  • These are known as inverse agonists and include atropine, M1 selective drugs, Pirenzepine, methyl derivatives of Scopolamine (Hyosine) and trihexphenydle. (howmed.net)
Agonist1
Receptor subtypes1
  • For example, in the presence of the allosteric modulator thiochrome the affinity of acetylcholine at the M 4 -muscarinic receptor is increased, but the affinity of acetylcholine for the other muscarinic receptor subtypes is unaffected [ 21 ]. (guidetopharmacology.org)
Anticholinergic1
  • [3] [11] Scopolamine has also been shown to exert a greater impairment on episodic memory , event-related potentials , memory retention and free recall compared to DPH (an anticholinergic and antihistamine ). (wikipedia.org)
Rats4
  • Scopolamine disrupts place navigation in rats and humans: a translational validation of the Hidden Goal Task in the Morris water maze and a real maze for humans. (cas.cz)
  • The behavioural, cognitive and neuropathological changes observed in AD can be induced by intraperitoneal (i.p) administration of scopolamine in female rats. (ijpsr.com)
  • Castration significantly exacerbated impairments in arm-choice accuracy produced by scopolamine as well as mecamylamine, without altering the disruptive effects of the drugs on the rate at which rats entered the arms of the maze. (lsu.edu)
  • Additionally, these results suggest that the absence of testicular hormones increases the sensitivity of male rats to the impairing effects of scopolamine as well as mecamylamine on working memory. (lsu.edu)
Antimuscarinic1
  • Furey, M. L. & Drevets, W. C. Antidepressant efficacy of the antimuscarinic drug scopolamine: a randomized, placebo-controlled clinical trial. (nature.com)
Drugs2
  • Just like muscarinic agonists, anticholinergics act as examples for drugs bind to GPCR. (egpat.com)
  • With regard to alteration of receptor sensitivity by long-term administration of drugs, it has been reported that chronic treatment with atropine or scopolamine produced a supersensitivity to cholinergic agents (Takeyasu et al. (baillement.com)
Amnesia2
  • Scopolamine causes drowsiness, amnesia, fatigue and dreamless sleep. (howmed.net)
  • Furthermore, Mamiya and Ukai ( 2001 ) reported that intracerebroventricular injection of S14G-HN (HNG) prevented scopolamine-induced amnesia in mice. (jneurosci.org)
Pretreatment1
  • A single pretreatment with scopolamine (0.5 mg/kg, i.p.), however, depressed these yawning responses. (baillement.com)
Antidote1
  • Atropine Sulfate Injection, USP, is indicated for temporary blockade of severe or life threatening muscarinic effects, e.g., as an antisialagogue, an antivagal agent, an antidote for organophosphorus or muscarinic mushroom poisoning, and to treat bradyasystolic cardiac arrest. (nih.gov)
Exert1
  • The rapidly acting antidepressants ketamine and scopolamine exert behavioral effects that can last from several days to more than a week in some patients. (nature.com)
Effects5
  • Here we show that methyl-CpG-binding protein 2 (MeCP2) phosphorylation at Ser421 (pMeCP2) is essential for the sustained, but not the rapid, antidepressant effects of ketamine and scopolamine in mice. (nature.com)
  • Fig. 7: Sustained antidepressant effects of ketamine and scopolamine in a corticosterone-induced animal model of depression. (nature.com)
  • Chronic treatment with haloperidol, physostigmine and scopolamine exerted different effects on the frequency of yawning induced by apomorphine (0.25 mg/kg, i.p.), physostigmine (0.2 mg/kg, i.p.) and pilocarpine (4 mg/kg, i.p.) as compared with chronic treatment with saline. (baillement.com)
  • The present experiments were performed to clarify the possible role of the dopaminergic and cholinergic systems in mediating the effects of chronic treatment with haloperidol, physostigmine and scopolamine on yawning induced by apomorphine, physostigmine or pilocarpine. (baillement.com)
  • In the present study, we examined the memory-improving effects of the extracts of C. chinensis and C. campestris on scopolamine (SCOP)-induced memory deficit and explored their underlying mechanism in mice. (mdpi.com)
Compounds1
  • The objective of this review was to combine the literature on depression with the pharmacology of antidepressant compounds, in order to formulate a conceivable pathophysiological process, allowing proposals how to accelerate the discovery process. (mdpi.com)
Mice1
  • In a mouse model, researchers caused the condition by placing mice in a controlled environmental chamber with a relative humidity of less than 25%, air flow of 15 liters per minute, and they then applied a transdermal scopolamine patch. (iris-pharma.com)
Antidepressant2
  • Our results reveal that pMeCP2 is downstream of BDNF, a critical factor in ketamine and scopolamine antidepressant action. (nature.com)
  • Fig. 4: BDNF-dependent pMeCP2 mediates the sustained antidepressant response of scopolamine. (nature.com)
Decrease1
  • Both rodent models using scopolamine effectively induced dry eye by causing a rapid decrease in tear production and an increase in corneal defects. (iris-pharma.com)
Clinical2
Pilocarpine1
  • Scopolamine potentiated the physostigmine- and pilocarpine-induced yawning but not the apomorphine-induced yawning. (baillement.com)
Genes1
  • Neurochemical studies conducted after completing behavioral experiments demonstrated that OBX downregulated the expression levels of cholinergic marker genes encoding choline acetyltransferase and muscarinic M 1 receptor in a manner reversed by ATL and tacrine. (hindawi.com)
Dose1
  • Following acquisition, scopolamine and mecamylamine dose-effect curves were established. (lsu.edu)
Molecular1
Memory1
Chapter1
Iris1
  • In a rat model, Iris Pharma researchers induced dry eye using 21-day systemic and continuous delivery of scopolamine through an osmotic pump implanted subcutaneously. (iris-pharma.com)
Administration1
  • In addition, we show that pMeCP2 is required for the long-term regulation of synaptic strength after ketamine or scopolamine administration. (nature.com)
Central1
  • This behavior is inhibited by scopolamine, but not by methyiscopolamine, suggesting that yawning is mediated by stimulation of the central 'muscarinic' receptor (Urbá-Holmgren et al. (baillement.com)
Group1
  • Escape latency time of Group 3 (Donepezil) and Group 6 (AMEE and Estradiol) is less than group 2 (Scopolamine and letrozole). (ijpsr.com)
Brain1
  • Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography. (acs.org)