AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and ProcessesDisciplines and Occupations
GABA AgonistsMuscimolGABA-A Receptor AgonistsBaclofenGABA Antagonistsgamma-Aminobutyric AcidReceptors, GABA-AGABA-B Receptor AgonistsBicucullineIsoxazolesDopamine AgonistsPurinergic P1 Receptor AgonistsPicrotoxinRats, Sprague-DawleySerotonin 5-HT1 Receptor AgonistsSerotonin 5-HT2 Receptor AgonistsMicroinjectionsGABA AgentsSerotonin Receptor AgonistsAdenosine A1 Receptor AgonistsGABA ModulatorsNeuronsDose-Response Relationship, DrugAdrenergic alpha-2 Receptor AgonistsReceptors, GABA-BPurinergic P2 Receptor AgonistsCannabinoid Receptor AgonistsSerotonin 5-HT4 Receptor AgonistsMuscarinic AgonistsHistamine AgonistsGABA Plasma Membrane Transport ProteinsNicotinic AgonistsReceptors, Opioid, kappaAdenosine A2 Receptor AgonistsAdrenergic AgonistsAdenosine A3 Receptor AgonistsReceptors, Opioid, muExcitatory Amino Acid AgonistsAdenosineAdrenergic beta-3 Receptor AgonistsAdrenergic beta-AgonistsRats, WistarSerotonin AntagonistsReceptors, Dopamine D2Receptors, Opioid, deltaAdrenergic alpha-Agonists2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepineAdrenergic alpha-1 Receptor AgonistsCholinergic AgonistsPhenethylaminesGABA-A Receptor AntagonistsGABA Uptake InhibitorsPiperidinesReceptors, Purinergic P1QuinpiroleEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Radioligand AssayReceptors, Dopamine D1BenzazepinesCannabinoidsReceptors, OpioidCells, CulturedReceptor, Adenosine A2APatch-Clamp TechniquesPhosphinic AcidsDrug InteractionsPyrrolidinesCalciumSerotoninNaphthalenesCyclic AMPLigandsNipecotic AcidsSynaptic TransmissionEnkephalin, D-Penicillamine (2,5)-Adenosine-5'-(N-ethylcarboxamide)GABA-B Receptor AntagonistsNeural InhibitionReceptor, Cannabinoid, CB1Guinea PigsDopamine AntagonistsBehavior, AnimalBenzoxazinesReceptor, Cannabinoid, CB2Serotonin 5-HT3 Receptor AgonistsSignal TransductionCarbacholTetrahydronaphthalenesPurinergic P2X Receptor AgonistsPurinergic P1 Receptor Antagonists8-Hydroxy-2-(di-n-propylamino)tetralinApomorphineReceptors, GlucagonErgolinesNarcotic AntagonistsGlutamic AcidReceptors, Dopamine D3DopaminePurinergic P2Y Receptor AgonistsBenzeneacetamides
NeuronsAntagonistPotent agonistBindsAntagonistsGlutamateMuscimolInhibitory neurotransmitterInhibitNeurotransmitter gamma-aminPositive allosteric modulatorsSerotoninSelectiveAmygdalaModulationGABAergicOpioidCurrentsBrainConcentrationsAcetylcholineSpinal cordBaclofenSynaptic cleftPotentiationChlorideFunctionalPresynapticActivationBehaviorInhibitsExcitatoryHypnoticsEffectsCompoundsAlcoholBenzodiazepineProteinAnxietyBiologicalDrugsBlockerAssessRegulationMiceActs
Neurons12
  • Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
  • The activation of GABAA receptors with muscimol, as well as bath application of glutamate, lead to increases in [Ca2+]i in pioneer neurons. (nih.gov)
  • Consistent with such results, immunocytochemical studies showed a prominent expression of GABAA and NMDA receptors in pioneer neurons. (nih.gov)
  • The activation of such receptors may be implicated in the remodelling of pioneer neurons during development. (nih.gov)
  • However, opioid receptor-effector uncoupling cannot account fully for physical dependence, which is characterized by withdrawal signs, or abnormal rebound responses in single neurons after administration of an opiate antagonist. (jneurosci.org)
  • The gelsemine actions were determined by electrophysiological recordings of recombinant GABARs expressed in HEK293 cells, and of native receptors in cortical neurons. (iasp-pain.org)
  • The actions of the endogenous ORL 1 -receptor ligand nociceptin on the membrane properties and synaptic currents in rat periaqueductal gray (PAG) neurons were examined by the use of whole-cell patch-clamp recording in brain slices. (jneurosci.org)
  • Ethanol binds to postsynaptic GABAA receptors (inhibitory neurons). (medscape.com)
  • Mu-opioid receptor (MOR) agonists potently inhibited MThal inputs without affecting ACC inputs to individual striatal medium spiny neurons (MSNs). (elifesciences.org)
  • The decrease in the frequency of mIPSCs of SCN neurons produced by the selective 5-HT 1B receptor agonist CP-93,129 is consistent with the interpretation that 5-HT 1B receptors are located on GABA terminals in the SCN and that 5-HT inhibits GABA release via a 5-HT 1B presynaptic receptor-mediated mechanism. (unl.edu)
  • Nonlethal concentrations of EO increased agonist binding and decreased antagonist binding in cortical neurons. (hindawi.com)
  • In such cases, the dendrites (a neuron's receiving branches) on the postsynaptic neurons release neurotransmitters that affect receptors on the presynaptic neurons. (msdmanuals.com)
Antagonist3
  • Engel JA , Nylander I, Jerlhag E. A ghrelin receptor (GHS-R1A) antagonist attenuates the rewarding properties of morphine and increases opioid peptide levels in reward areas in mice. (neurotree.org)
  • Engel JA , Jerlhag E, Svensson L, Smith RG, Egecioglu E. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. (neurotree.org)
  • Using CsCl-containing microelectrodes with QX314, we isolated mPSCs that were sensitive to the GABA A receptor antagonist, bicuculline. (unl.edu)
Potent agonist1
  • Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies. (bvsalud.org)
Binds3
  • Positive allosteric modulators work by increasing the frequency with which the chloride channel opens when an agonist binds to its own site on the GABA receptor. (wikipedia.org)
  • It is believed to act as a GABA agonist, meaning it binds to GABA receptors and increases the activity of GABA in the brain. (nationallabday.org)
  • The toxin in these mushrooms is muscarine, a thermostable muscarinic receptor agonist that binds to acetylcholine receptors in the peripheral nervous system. (msdvetmanual.com)
Antagonists4
  • Furthermore, we treated the ARC with GABA-A/B receptor antagonists separately, and IOP was evaluated, as well as retinal ganglion cell apoptosis in the chronic high IOP rat model. (molvis.org)
  • Antagonists of GABA receptors inhibit the action of GABA. (otavachemicals.com)
  • Agonists and antagonists of GABA A and GABA B were taken from ChEMBL database. (otavachemicals.com)
  • The newest class of sleeping pills, orexin receptor antagonists inhibit orexin, a neurotransmitter in the brain that promotes wakefulness. (sleepreviewmag.com)
Glutamate6
  • The main groups include sodium channel blockers, calcium current inhibitors, gamma-aminobutyric acid (GABA) enhancers, glutamate blockers, carbonic anhydrase inhibitors, hormones, and drugs with unknown mechanisms of action (see the image below). (medscape.com)
  • 1998). We have analysed the functional activity of glutamate and GABA receptors in such cells by measuring changes in intracellular calcium concentrations ([Ca2+]i). (nih.gov)
  • The stimulatory action of glutamate is mostly produced through the NMDA-type of ionotropic receptors. (nih.gov)
  • Metabotropic glutamate receptor activation has no effect on [Ca2+]i. (nih.gov)
  • Most of the clinical effects can be explained by the interaction of ethanol with various neurotransmitters and neuroreceptors in the brain, including those interacting with gamma-aminobutyric acid (GABA), glutamate (NMDA), and opiates. (medscape.com)
  • Keppra or levetiracetam does not act on glutamate receptors. (accessmedicinenetwork.com)
Muscimol3
  • The influence of γ-aminobutyric type-A (GABA A ) receptors agonist (muscimol hydrobromide, 0.1 µg/0.5 µl) injections into the right or left basolateral amygdala (BLA) on the behavior of high-an- xiety (HA) and low-anxiety (LA) rats subjected to the elevated plus-maze (EPM) test was investigated. (scirp.org)
  • its decarboxylated derivative, muscimol, is an agonist at gamma-aminobutyric acid (GABA) receptors. (medscape.com)
  • Many of the central nervous system (CNS) effects of muscimol (eg, sedation) are ascribed to its ability to act as a GABA agonist. (medscape.com)
Inhibitory neurotransmitter4
  • GABA is the major inhibitory neurotransmitter in the brain, and GABA-like drugs are used to suppress spasms. (wikipedia.org)
  • For example, if a patient has tried and failed a sodium channel blocker, it might be time to try a calcium channel blocker or something that increases the levels of GABA (the major inhibitory neurotransmitter). (accessmedicinenetwork.com)
  • This is effective because GABA is the major inhibitory neurotransmitter in the brain, helping to decrease the uncontrolled activity seen in seizures. (accessmedicinenetwork.com)
  • Phenibut is a synthetic derivative of the naturally occurring inhibitory neurotransmitter gamma-aminobutyric acid (GABA). (nationallabday.org)
Inhibit2
  • The GABA-β receptor belongs to the class of G-Protein coupled receptors that inhibit adenylyl cyclase, therefore leading to decreased cyclic adenosine monophosphate (cAMP). (wikipedia.org)
  • The signal may stimulate or inhibit the receiving cell, depending on the neurotransmitter and receptor involved. (msdmanuals.com)
Neurotransmitter gamma-amin2
Positive allosteric modulators2
  • These drugs act instead as positive allosteric modulators (PAMs) and while they do bind to the GABA receptors, they bind to an allosteric site on the receptor and cannot induce a response from the neuron without an actual agonist being present. (wikipedia.org)
  • However, some general anaesthetics like propofol and high doses of barbiturates may not only be positive allosteric modulators of GABA-A receptors but also direct agonists of these receptors. (wikipedia.org)
Serotonin2
  • It has been considered to increase the synaptic concentration of serotonin and/or norepinephrine by reuptake inhibition, but also appears to work by down regulation of beta-adrenergic receptors and serotonin receptors and desensitization of adenyl cyclase. (cmelist.com)
  • The suprachiasmatic nucleus (SCN) receives a dense serotonergic innervation that modulates photic input to the SCN via serotonin 1B (5-HT 1B ) presynaptic receptors on retinal glutamatergic terminals. (unl.edu)
Selective4
  • Pagoclone is a novel member of the cyclopyrrolone class of compounds and acts as a gamma amino butyric acid (GABA) selective receptor modulator. (fiercebiotech.com)
  • Pagoclone is a novel, non-benzodiazepine, selective GABA-A receptor agonist. (fiercebiotech.com)
  • Ovid Therapeutics), a delta (δ)-selective GABA A receptor agonist, for the treatment of Fragile X syndrome. (empr.com)
  • We therefore tested the hypothesis that 5-HT 1B receptors might also be located on SCN GABAergic terminals by examining the effects of the highly selective 5-HT 1B receptor agonist CP-93,129 on SCN miniature inhibitory postsynaptic currents (mIPSCs). (unl.edu)
Amygdala2
  • Based on the analysis of literature data, as well as our previous findings, we hypothesize that the level of GABA and, probably, its difference between the right and the left amygdala, may determine the differences in the anxiety levels in animals. (scirp.org)
  • GABA-B receptors are present in the brain (especially the cerebral cortex, thalamic nuclei, cerebellum, and amygdala). (emcrit.org)
Modulation3
  • Modulation of GABA receptors and of GABAergic synapses by the natural alkaloid gelsemine. (iasp-pain.org)
  • The results demonstrate, for the first time, that EO can improve GABAergic neurotransmission via interactions with GABA A receptor and modulation of GABA uptake. (hindawi.com)
  • Considering that PTZ blocks the chloride channel coupled to the GABA A receptor complex, the present study aimed to analyze the possible modulation of GABAergic homeostasis within synaptic clefts in vitro . (hindawi.com)
GABAergic1
  • This study investigated the effects of EO on the main GABAergic targets for anticonvulsant drugs, analyzing the effect on the GABA receptor's benzodiazepine and picrotoxinin binding sites and the GABA uptake. (hindawi.com)
Opioid2
  • Opioid withdrawal is treated with a long-acting opioid agonist, such as methadone 20-35 mg/d or buprenorphine 4-16 mg/d, and then tapered over days to weeks. (medscape.com)
  • In contrast, delta-opioid receptor (DOR) agonists disinhibited ACC pyramidal neuron responses to MThal inputs by suppressing local feed-forward GABA signaling from parvalbumin-positive interneurons. (elifesciences.org)
Currents1
  • Gelsemine inhibited the agonist-evoked currents of recombinant and native receptors. (iasp-pain.org)
Brain8
  • Alcohol is believed to mimic GABA's effect in the brain, binding to GABA receptors and inhibiting neuronal signaling. (wikipedia.org)
  • Benzodiazepine receptor agonists (BZRAs) target a specific part of the brain and may increase a neurotransmitter called gamma-aminobutyric acid (GABA). (medicalnewstoday.com)
  • The brain naturally releases GABA to promote sleep at nighttime. (medicalnewstoday.com)
  • GABA-B receptors occur outside the blood-brain barrier, within the sympathetic nervous system and some visceral tissues (including the heart). (emcrit.org)
  • Depakote or valproic acid increases the levels of GABA in the brain and also works through sodium channels. (accessmedicinenetwork.com)
  • It is a derivative of the neurotransmitter GABA and is believed to have a calming effect on the brain. (nationallabday.org)
  • Phenibut is a synthetic derivative of GABA, a neurotransmitter that is naturally produced in the brain. (nationallabday.org)
  • These target and activate the GABA receptors in the brain, which promote sleepiness, she says. (sleepreviewmag.com)
Concentrations1
  • Low concentrations significantly inhibited GABA uptake, especially in astrocytes, suggesting an accumulation of endogenous GABA in the synaptic cleft. (hindawi.com)
Acetylcholine2
  • Unlike acetylcholine, muscarine is not degraded by acetylcholinesterase, and toxicity results from unregulated stimulation at the receptors. (msdvetmanual.com)
  • Muscarine competes with acetylcholine at cholinergic receptor binding sites, leading to excessive stimulation of postganglionic cholinergic fibers and the subsequent observed clinical signs (cholinergic excess). (msdvetmanual.com)
Spinal cord1
  • GABA-B receptors are also found in the ventral and dorsal horns of the spinal cord. (emcrit.org)
Baclofen2
Synaptic cleft1
  • Neurotransmitters diffuse across the synaptic cleft and bind briefly to specific receptors on the adjoining neuron or effector cell. (msdmanuals.com)
Potentiation1
  • Drugs that fall into this class exert their pharmacodynamic action by increasing the effects that an agonist has when potentiation is achieved. (wikipedia.org)
Chloride1
  • The two receptors GABA-α and GABA-ρ are ion channels that are permeable to chloride ions which reduces neuronal excitability. (wikipedia.org)
Functional1
  • In mice lacking functional 5-HT 1B receptors, CP-93,129 (1 mM) had no clear effect on the frequency or the amplitude of mIPSCs recorded in any of the cells tested ( n = 4). (unl.edu)
Presynaptic1
  • 5-HT 1B Receptor-Mediated Presynaptic Inhibition of GABA Rel" by Jayne R. Bramley, Patricia J. Sollars et al. (unl.edu)
Activation1
  • Activation of these receptors enhances the effects of GABA. (medscape.com)
Behavior1
  • Zawilska and Wojcieszak, 2014 ), but use of WIN can clarify the effects of cannabinoid receptor agonist SA on behavior. (nature.com)
Inhibits1
Excitatory1
  • Depending on the receptor, the response may be excitatory or inhibitory. (msdmanuals.com)
Hypnotics1
  • The newer GABA-effective hypnotics are the only medications with demonstrated effectiveness in treating chronic insomnia with the majority of evidence supporting treatment efficacy for cognitive-behavioral therapy and short acting GABA-receptor agonists. (springer.com)
Effects6
  • A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. (wikipedia.org)
  • GABA-α and GABA-ρ receptors produce sedative and hypnotic effects and have anti-convulsion properties. (wikipedia.org)
  • GABA-β receptors also produce sedative effects. (wikipedia.org)
  • Therefore, the current study sought to develop a rodent model of adolescent cannabinoid self-administration (SA), using the synthetic cannabinoid receptor agonist WIN55,212-2 (WIN), in order to assess measures of relapse/reinstatement of drug seeking and long-term effects on cognitive function assessed in a delay-match-to-sample working memory task and a spatial recognition task. (nature.com)
  • GABA receptors agonists produce typically sedative effects, and may also cause other effects such as anticonvulsant, anxiolytic and muscle relaxant effects. (otavachemicals.com)
  • It is believed to act as a GABA agonist, leading to a variety of effects, including relaxation, improved mood, and improved cognitive performance. (nationallabday.org)
Compounds2
  • Therefore, small molecule compounds modulating GABA receptors activity may have significant therapeutic potential. (otavachemicals.com)
  • The designed libraries comprise drug-like compounds only (PAINS compounds are filtered off) and provide an excellent basis for drug discovery projects related with GABA receptors. (otavachemicals.com)
Alcohol5
  • Alcohol is an indirect GABA agonist. (wikipedia.org)
  • Sedative-hypnotic drugs are the primary agents for treatment of alcohol withdrawal syndrome because they are cross-tolerant drugs that modulate GABA functions. (medscape.com)
  • Suchankova P, Engel JA , Jerlhag E. Sub-chronic Ghrelin Receptor Blockade Attenuates Alcohol- and Amphetamine-Induced Locomotor Stimulation in Mice. (neurotree.org)
  • Vallöf D, Maccioni P, Colombo G, Mandrapa M, Jörnulf JW, Egecioglu E, Engel JA , Jerlhag E. The glucagon-like peptide 1 receptor agonist liraglutide attenuates the reinforcing properties of alcohol in rodents. (neurotree.org)
  • Suchankova P, Nilsson S, von der Pahlen B, Santtila P, Sandnabba K, Johansson A, Jern P , Engel JA , Jerlhag E. Genetic variation of the growth hormone secretagogue receptor gene is associated with alcohol use disorders identification test scores and smoking. (neurotree.org)
Benzodiazepine1
  • Restoril is a benzodiazepine and Ambien is a type A GABA receptor agonist . (rxlist.com)
Protein1
  • Mutations occur in the FMR1 gene which can block expression of the Fragile X Mental Retardation Protein (FMRP), an important protein in GABA synthesis. (empr.com)
Anxiety1
  • These findings suggest an important role in anxiety regulation of the amygdalar GABA levels, and the assumed GABA hemispheric lateralization. (scirp.org)
Biological1
  • The behavioral activity profile of gelsemine suggests the involvement of GABA receptors (GABARs), which are the main biological targets of benzodiazepines (BDZs), a group of drugs with anxiolytic, hypnotic, and analgesic properties. (iasp-pain.org)
Drugs1
  • Many commonly used sedative and anxiolytic drugs that affect the GABA receptor complex are not agonists. (wikipedia.org)
Blocker1
  • Clarified Euterpe oleracea (EO) juice showed anticonvulsant properties similar to diazepam in an in vivo model with pentylenetetrazol, a GABA A receptor blocker. (hindawi.com)
Assess1
  • To assess the expression of GABA-A/B receptors within the ARC under persistent high IOP, we performed immunofluorescence (IF) and immunohistochemical (IHC) staining at 2 weeks and 4 weeks. (molvis.org)
Regulation1
  • GABA-A/B receptors in the ARC may be involved in regulation of IOP, and pathologically high IOP affects the expression of GABA-A/B receptors in the ARC. (molvis.org)
Mice1
  • In the following induced high IOP animal model, the expression of GABA-A/B receptors within the ARC was evaluated in DBA/2J mice which developed progressive eye abnormalities spontaneously that closely mimic human hereditary glaucoma. (molvis.org)
Acts1