ReceptorsAcetylcholineAntagonistsNeuronsSynapticAntagonistCarbacholMuscarinicBasal forebrainInhibitionNeurotransmissionSelectiveCortical cholinergicModulationAlzheimer'sDrugsNeuronalSubtypesLigandModulatorsDopaminergic transmissionGABAMediateInhibitsEndogenousEffectsMolecularMechanismsMechanismMeSHNeuromuscularDosesPlay a crucial roleCognitiveRegulationPathwayCortexBiosynthesisPotentialsEfficacy
Receptors21
- 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)
- 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)
- Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). (cdrewu.edu)
- Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. (cdrewu.edu)
- Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission. (cdrewu.edu)
- Central cholinergic regulation of respiration: nicotinic receptors. (cdrewu.edu)
- Drugs that bind to nicotinic cholinergic receptors ( RECEPTORS, NICOTINIC ) and block the actions of acetylcholine or cholinergic agonists. (nih.gov)
- It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. (bvsalud.org)
- The improvement of therapeutic approaches using specific mAChR modulators is further impeded by a lack of established and validated protocol to screen efficacy of different mAChR agonist/antagonist at native receptors in neocortical slices. (biomedcentral.com)
- It has been shown that cholinergic receptors are present in the superficial and deep dorsal horn of the spinal cord, and activation of spinal nicotinic or muscarinic acetylcholine receptors produces analgesia [ 12 ]. (biomedcentral.com)
- An alternative approach is to directly activate cholinergic receptors responsible for learning and memory. (ox.ac.uk)
- Peptide-induced modulation of synaptic transmission and escape response in Drosophila requires two G-protein-coupled receptors. (neurotree.org)
- It can be not clear why stimulation GSK-3 inhibition of 5 HT4 receptors in some but not in other circumstances, induces an enhancement of each cholinergic and non cholinergic transmission. (others-signal.com)
- In addition to its choline uptake enhancer, coluracetam has been identified as an agonist of AMPA receptors. (rcd.bio)
- AMPA receptors play a crucial role in facilitating glutamatergic synaptic transmission and plasticity, which are needed for the molecular processes underlying memory and learning. (rcd.bio)
- 15. The role of G-protein coupled receptor kinases in the regulation of muscarinic cholinergic receptors. (elsevier.com)
- These results suggest that BRC-induced yawning may be mediated via presynaptic dopaminergic neuron activity and that BRC, in addition to the stimulation of dopamine 4J-2 receptors, appears to require endogenous dopamine or receptor activation by another dopamine agonist (D-1 agonist) for the induction of yawning, stereotypy and upright lighting responses. (baillement.com)
- Naturally expressed nicotinic acetylcholine receptors composed of α4 and β2 subunits (α4β2-nAChR) are the predominant form of high affinity nicotine binding site in the brain implicated in nicotine reward, mediation of nicotinic cholinergic transmission, modulation of signaling through other chemical messages, and a number of neuropsychiatric disorders. (barrowneuro.org)
- A ripiprazole, a partial agonist at central D 2 receptors, is a widely prescribed atypical antipsychotic drug. (psychiatrist.com)
- 3 Moreover, the partial agonistic effect on D 2 receptors and the serotonin uptake blockage also could have contributed to the urinary symptoms by decreasing dopaminergic transmission and indirectly increasing cholinergic activity in the detrusor muscle, respectively. (psychiatrist.com)
- The lack of affinity of amisulpride for adrenergic or cholinergic receptors might explain the absence of urinary symptoms in our case. (psychiatrist.com)
Acetylcholine9
- The agonist ligand nicotine shows an up to 30-fold higher affinity to nACHRs than acetylcholine (ACh). (weeksmd.com)
- 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 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)
- In this sense, previous studies identified cholinergic terminals within the mPFC, and stressful stimuli increased local acetylcholine release. (bvsalud.org)
- Several mechanisms such as the hyperpolarization of neurons, reduction in the release of pronociceptive neurotransmitters, or activation of the nitric oxide-cyclic guanosine monophosphate pathway might mediate this peripheral cholinergic antinociception by elevating endogenous acetylcholine. (asahq.org)
- Considerable evidence indicates a crucial role of acetylcholine (ACh)-mediated transmission in learning and memory. (biomedcentral.com)
- Current therapies for Alzheimer's disease seek to correct for defective cholinergic transmission by preventing the breakdown of acetylcholine through inhibition of acetylcholinesterase, these however have limited clinical efficacy. (ox.ac.uk)
- This appears to result in increased concentrations of acetylcholine available for synaptic transmission in the central nervous system. (syrianclinic.com)
- The aim of the project is to determine how disruption of cholinergic activation of striatal GABAergic interneurons alters striatal signalling and striatum-based behaviour by using a mouse model with deletion of the β2 nicotinic acetylcholine receptor subunit in striatal GABAergic interneurons. (cas.cz)
Antagonists8
- Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses. (nih.gov)
- We investigated the effects of the cholinergic agonist carbachol (CCh) and various agonists and antagonists on neuronal activity in rat neocortical slices using intracellular (sharp microelectrode) and field potential recordings. (biomedcentral.com)
- However, the similarity in ligand-binding sites between mAChR subtypes, the paucity of selective agonists/antagonists as well as the expression of different subtypes of mAChRs in a given area constitute major obstacles to delineate cellular effects of a given subtype [ 1 ]. (biomedcentral.com)
- 5 HT3 or 5 HT4 agonists and antagonists have organspecific and species dependent results on gastrointestinal motility. (others-signal.com)
- The neurokinin type 3 (NK 3 ) receptor antagonists SB-223412 and SR-142801 inhibited vagally mediated cholinergic contractions of bronchi in vitro at stimulation voltages threshold for preganglionic nerve activation but had no effect on vagally mediated contractions evoked at optimal voltage or field stimulation-induced contractions. (johnshopkins.edu)
- The neurokinin type 3 (NK3) receptor antagonists SB-223412 and SR-142801 inhibited vagally mediated cholinergic contractions of bronchi in vitro at stimulation voltages threshold for preganglionic nerve activation but had no effect on vagally mediated contractions evoked at optimal voltage or field stimulation-induced contractions. (johnshopkins.edu)
- 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)
- H-EBDN binding competition studies reveal high affinity for nicotinic agonists and lower affinity for nicotinic antagonists. (barrowneuro.org)
Neurons6
- 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)
- Another notable aspect of coluracetam's mechanism is its possibility to protect neurons from damage caused by cholinergic neurotoxins. (rcd.bio)
- 1983). Biochemical studies have demonstrated that BRC has both agonist and antagonist properties at preand postsynaptic dopaminergic neurons, and that it decreases synaptosomal tyrosine hydroxylase activity (Goldstein et al. (baillement.com)
- We study physiology, biochemistry and pharmacology of cholinergic neurons at the molecular level and molecular pharmacology of other GPCRs. (cas.cz)
- Retrograde transmission can inhibit presynaptic neurons from releasing additional neurotransmitters and help control the level of activity and communication among neurons. (msdmanuals.com)
Synaptic5
- CCh increased neuronal firing but reduced synaptic transmission. (biomedcentral.com)
- Frequenin/NCS-1 and the Ca2+-channel alpha1-subunit co-regulate synaptic transmission and nerve-terminal growth. (neurotree.org)
- Romero-Pozuelo J, Dason JS , Atwood HL , Ferrús A. Chronic and acute alterations in the functional levels of Frequenins 1 and 2 reveal their roles in synaptic transmission and axon terminal morphology. (neurotree.org)
- 1. Molecular properties and cellular distribution of cholinergic synaptic proteins. (elsevier.com)
- Additionally, it was revealed that the most relevant genes are involved in biological processes related to signal transduction, positive regulation of transcription from RNA polymerase II promoters, chemical synaptic transmission, response to drugs, ion transmembrane transport, nervous system development, cell adhesion, and neuron migration. (biomedcentral.com)
Antagonist4
- Using saccharin as a taste stimulus in a taste preference paradigm, we examined the effects of injecting the GABA A receptor agonist muscimol or the GABA A receptor antagonist bicuculline into the IC or NBM during learning or retrieval of an appetitive taste memory on taste preference in male Sprague Dawley rats. (jneurosci.org)
- Furthermore, neither DAergic agonist nor antagonist affected PS deprivation induced inhibition of yawning. (baillement.com)
- It also highlights the status of the agonist and antagonist of brain RAS in the treatment of various neurological disorders. (hindawi.com)
- These small currents were linked to ACh release since anticholinesterases (neostigmine) increased their effects, while cholinergic receptor antagonist (tubocurarine, a nicotinic receptor blocker) blocked. (pharmacology2000.com)
Carbachol1
- Zhang W, Tan YF, Atwood HL , Martin Wojtowicz J. Biphasic effects of the cholinergic agonist carbachol on long-term potentiation in the dentate gyrus of the mammalian hippocampus. (neurotree.org)
Muscarinic2
- 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)
- Biochemical Characterization of the Muscarinic Cholinergic Receptor in Human Brain: Alterations in Huntington's Disease. (aspetjournals.org)
Basal forebrain2
- 25. Immunolesion by 192IgG-saporin of rat basal forebrain cholinergic system: a useful tool to produce cortical cholinergic dysfunction. (elsevier.com)
- Alzheimer's disease is characterized by cholinergic deficiency in the cortex and basal forebrain, which contributes to cognitive deficits. (syrianclinic.com)
Inhibition4
- 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)
- Here, we evaluate how GABA inhibition modulates cholinergic transmission and its involvement during taste novelty processing and familiar taste memory retrieval. (jneurosci.org)
- These findings indicate that GABA inhibition modulates cholinergic transmission and that cholinergic-GABAergic system interactions are important during the transition from novel to familiar memory. (jneurosci.org)
- These data indicate that the three effects are mediated by different mAChRs, the increase in firing being mediated by M 1 mAChR, decrease of inhibition by M 2 mAChR and depression of excitatory transmission by M 4 mAChR. (biomedcentral.com)
Neurotransmission3
- Despite these pieces of evidence, the specific role of cholinergic neurotransmission in different subregions of the mPFC controlling the cardiovascular responses to stress has never been systematically evaluated. (bvsalud.org)
- Therefore, the purpose of this study was to investigate the involvement of cholinergic neurotransmission present within PL and IL in cardiovascular responses to an acute session of restraint stress in rats. (bvsalud.org)
- Taken together, these results indicate functional differences of cholinergic neurotransmission within the PL and IL in control of cardiovascular and autonomic responses to stressful stimuli. (bvsalud.org)
Selective5
- 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)
- The ability of bromocriptine (BRC), a selective dopamine D-2 receptor agonist, to induce yawning responses was studied in rats pretreated with reserpine and alpha-methyl-p-tyrosine (alpha-MPT). (baillement.com)
- A low dose of the selective D-1 dopamine receptor agonist SK&F38393 did not induce yawning but enhanced the BRC-induced response. (baillement.com)
- The exact ranking of efficacies and potencies of agonists is indispensable in the discovery of new selective agonists. (cas.cz)
- In addition, subtype-selective agonists, which bind to and activate the receptor via binding domains distinct from the orthosteric binding site have also been reported. (guidetopharmacology.org)
Cortical cholinergic4
- Questions remain regarding which neuronal circuits and neurotransmitters trigger activation or suppression of cortical cholinergic activity. (jneurosci.org)
- These results indicate that the pattern of cortical cholinergic and GABAergic neuroactivity during novel taste exposure is the opposite of that which occurs during familiar taste recognition and these differing neurotransmitter system states may enable different behavioral consequences. (jneurosci.org)
- This work demonstrates interactions between cortical cholinergic and GABAergic systems during taste learning and memory retrieval. (jneurosci.org)
- However, questions remain regarding which neuronal circuits and neurotransmitters trigger and/or accompany the activation and suppression of cortical cholinergic activity during novel and familiar stimulus recognition, respectively. (jneurosci.org)
Modulation1
- 24. Activity-related modulation of cholinergic transmission. (elsevier.com)
Alzheimer's1
- 28. The systems-level organization of cholinergic innervation in the human cerebral cortex and its alterations in Alzheimer's disease. (elsevier.com)
Drugs2
- Conversely, drugs that augment cholinergic transmission (e.g. donepezil or galatamine) have been shown to improve certain cognitive functions [ 5 , 6 ]. (biomedcentral.com)
- Ectopic agonists represent a new class of drugs that bind out of the orthosteric site and display unique functional selectivity through mechanisms yet to be defined. (cas.cz)
Neuronal2
- 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)
- The nAChR is the principal structure of cholinergic neuromodulation and is responsible for coordinated neuronal network interaction. (weeksmd.com)
Subtypes1
- The benefit of β2-adrenergic agonists alone or combined with pyridostigmine or 3,4-Dyaminopiridine is increasingly being reported for different subtypes of CMS including AChR-deficiency and glycosylation abnormalities, thus expanding the therapeutic repertoire available. (ox.ac.uk)
Ligand1
- A biased agonist is a ligand which stabilizes a particular active conformation of a receptor, thus stimulating some responses but not others. (cas.cz)
Modulators1
- Thus, the potential therapeutic benefit of allosteric modulators/agonists is that they show subtype selectivity in a manner that has not be achievable with orthosteric ligands. (guidetopharmacology.org)
Dopaminergic transmission1
- 1975). Decreased tonic dopaminergic transmission consequently induces yawning (Yamada and Furukawa 1980, 1981). (baillement.com)
GABA1
- This sting injects significant quantities of γ amino-butyric acid (GABA) and complementary agonists taurine and β alanine. (wikipedia.org)
Mediate1
- This study was performed to determine whether spinal cholinergic systems mediate the relieving effects of electroacupuncture (EA) on cold and warm allodynia in a rat model of neuropathic pain. (biomedcentral.com)
Inhibits1
- Furthermore, BRC acts like a dopamine D-2 agonist and inhibits dopamine-stimulated synthesis of cyclic adenosine 3',S'-monophosphate (cyclic AMP) (Trabucchi et al. (baillement.com)
Endogenous1
- Jenkins and Jackson (1985) reported that BRC, in behavioral terms, has no effect per se at the postsynaptic dopamine receptor and that BRC requires either endogenous dopamine or the administration of an exogenous agonist such as apomorphine for the expression of its effects. (baillement.com)
Effects5
- Concomitant treatment of PS deprived animals with DA agonists reverses PS deprivation effects on stereotypy and aggressiveness. (baillement.com)
- Bexarotene (Bxt) is a retinoid-X receptor agonist used in the treatment of cutaneous lymphoma with a favorable safety profile whose effects have been recently investigated in other neurodegenerative diseases. (frontiersin.org)
- peptides injection into the cholinergic nuclei: morphological, neurochemical and behavioral effects. (elsevier.com)
- BRC cannot be considered a directly acting agonist like apomorphine, since reserpine and -MPT inhibit or completely abolish most of the behavioral effects induced by BRC (Johnson et al. (baillement.com)
- Biased agonists might represent a novel and uniquely effective type of therapeutic agent with reduced side-effects. (cas.cz)
Molecular1
- We perform a detailed analysis of receptor activation induced by ectopic and classical agonists with the aim to reveal molecular mechanisms underlying functional selectivity. (cas.cz)
Mechanisms1
- These discoveries throw new light on many areas of cholinergic mechanisms. (elsevier.com)
Mechanism1
- However, the spinal cholinergic mechanism of EA-induced antiallodynia remains to be elucidated. (biomedcentral.com)
MeSH1
- Nicotinic Agonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (cdrewu.edu)
Neuromuscular1
- Congenital myasthenic syndromes (CMS) are genetic disorders characterised by impaired neuromuscular transmission. (ox.ac.uk)
Doses1
- Yawning can be elicited by several cholinergic (AChergic) agonists, by low doses of dopaminergic (DAergic) agonists, and by polypeptides such as a-MSH and ACTH. (baillement.com)
Play a crucial role1
- Finally, the activation of opioidergic and cholinergic systems appears to play a crucial role in (-)-linalool-induced antinociception. (researchgate.net)
Cognitive1
- Here we aimed to design the drug properties needed for a well-tolerated M1-agonist with the potential to alleviate cognitive loss by taking a stepwise translational approach from atomic structure, cell/tissue-based assays, evaluation in preclinical species, clinical safety testing, and finally establishing activity in memory centers in humans. (ox.ac.uk)
Regulation1
- 5. The VAChT/ChAT "cholinergic gene locus": new aspects of genetic and vesicular regulation of cholinergic function. (elsevier.com)
Pathway1
- As an agonist of the retinoic-X receptor (RXR) pathway, Bxt notably increased the nuclear expression of the RXRα throughout transcriptionally active euchromatin domains. (frontiersin.org)
Cortex1
- Vi fann ett antal samband mellan mRNA uttryck och etanolintag i speciellt prefrontala cortex, en region i hjärnan som är inblandad i bl.a. bearbetning av nya intryck, minne och kontroll av beteende. (5dok.org)
Biosynthesis1
- 4. Biosynthesis and integration of acetylcholinesterase in the cholinergic synapse. (elsevier.com)
Potentials1
- The concoction temporarily blocks the motor action potentials in the prothoracic ganglion by depressing cholinergic transmission through the increased chloride conductance across nerve synapses. (wikipedia.org)
Efficacy1
- We tried to define simple paradigms to quantify routinely the efficacy of different mAChR agonists. (biomedcentral.com)