• agonists
  • Malcangio M and Bowery NG (1995) Possible therapeutic application of GABAB receptor agonists and antagonists. (els.net)
  • The ability of selective serotonin (5-HT) receptor agonists to reduce the extracellular concentration of 5-HT was examined in the striatum of awake, unrestrained mice by in vivo microdialysis. (aspetjournals.org)
  • The present findings suggest that, on systemic administration, both 8-OH-PIPAT and CP 94,253 are potent and selective agonists at the somatodendritic 5-HT 1A autoreceptor and terminal 5-HT 1B/1D autoreceptor, respectively, and are each able to cause decreases in extracellular levels of 5-HT in the mouse striatum by activating a distinct set of receptors. (aspetjournals.org)
  • Several H3 antagonists have been shown to act as inverse agonists and such profiles of H3 antagonists have been implicated in their pharmacological functions. (aspetjournals.org)
  • In contrast, H3 antagonists (thioperamide, ciproxifan, and GT2016) with inverse agonism displayed increased K i values against the MT6 receptors (2.5- to 5.8-fold), demonstrating more a prominent effect of inverse agonists to the constitutive active receptor. (aspetjournals.org)
  • Taken together, these data suggested that A357K mutation in the H3 receptor increased the population of active state receptors that preferably binds to agonists than inverse agonists, which could be termed as a constitutively active mutant of H3 receptor. (aspetjournals.org)
  • In contrast, a high level of receptor expression or specific mutation in receptors increases the concentration of R*, leading to the increased activities in the absence of agonists and the enhanced susceptibility to inverse agonists. (aspetjournals.org)
  • The agonists acting at AMPA receptors are AMPA and amino-3-hydroxy-5-tert-butyl-4-isoxazole propionic acid (ATPA). (rcpsych.org)
  • Kainate receptor agonists include kainate and domoic acid. (rcpsych.org)
  • At concentrations that reduced evoked EPSP/EPSCs by 40-60%, neither DAMGO, DPDPE, nor DELT decreased the amplitude of the postsynaptic current produced by brief pressure ejection of (S)-alpha-amino-3-hydroxy-5- methyl-4-isoxazole-propionic acid, suggesting a presynaptic site of action of these opioid receptor agonists. (jneurosci.org)
  • General anaesthetics are mainly GABA agonists but some (such as ketamine) are glutamate antagonists. (bio.net)
  • They include antagonists, inverse agonists, Rimonantibodies of CBRs. (wikipedia.org)
  • And Δ9-tetrahydrocannabivarin (THCV), a naturally occurring cannabinoid, modulate the effects of THC via direct blockade of cannabinoid CB1 receptors, thus behaving like first-generation CB1 receptor inverse agonists, such as rimonabant. (wikipedia.org)
  • Once cannabinoid receptors had been discovered, it became important to establish whether their agonists occur naturally in the body. (wikipedia.org)
  • Endocannabinoids are eicosanoids acting as agonists for cannabinoid receptors and they occur naturally in the body. (wikipedia.org)
  • CB1 antagonists produce inverse cannabimimetic effects that are opposite in direction from those produced by agonists for these receptors. (wikipedia.org)
  • Research in this area has been limited due to the cardiotoxicity of 5-HT2B agonists, and the lack of clear therapeutic application for 5-HT2B antagonists, but there is still a need for selective ligands for scientific research. (wikipedia.org)
  • Activation of these receptors inhibits peristaltic action which causes constipation, a major side effect of μ agonists. (wikipedia.org)
  • citation needed] Physiological processes mediated by the receptor include: CNS: neuronal excitation (most likely responsible for the psychedelic effects associated with 5-HT2A receptor agonists such as LSD, DMT, etc.), behavioural effects, learning, anxiety smooth muscle: contraction (in bronchi and gastrointestinal tract) vasoconstriction / vasodilation platelets: aggregation Activation of the 5-HT2A receptor with 2,5-Dimethoxy-4-iodoamphetamine (DOI) produces potent anti-inflammatory effects in several tissues including cardiovascular and gut. (wikipedia.org)
  • Role in memory and learning Activation of the 5-HT2A receptor is necessary for the effects of the "classic" psychedelics like LSD, psilocin and mescaline, which act as full or partial agonists at this receptor, and represent the three main classes of 5-HT2A agonists, the ergolines, tryptamines and phenethylamines, respectively. (wikipedia.org)
  • Whereas extracellular domain is the site of action of agonists and competitive antagonists, the transmembrane domain contains the central ion pore, receptor gate, and principle selectivity filter that allows ions to cross the cell membrane. (wikipedia.org)
  • NMDA
  • Sublamination requires the activity of the afferent fibers, NMDA receptors, and nitric oxide synthase (NOS). (jneurosci.org)
  • cGMP expression is upregulated in both retinal terminals and postsynaptic dLGN cells during sublamination, and this expression is controlled by the activity of both NMDA receptors and NOS. (jneurosci.org)
  • We conclude that the sGC-cGMP-PKG pathway acts downstream of NMDA receptors and nitric oxide as an effector of the activity-dependent refinement of connections at this level of the mammalian visual system. (jneurosci.org)
  • Indeed, although NMDA receptors have been postulated to play an important role in a number of developing systems, the sequence of intracellular signals after NMDA receptor activation has not been established in the developing mammalian brain. (jneurosci.org)
  • We reasoned that if cGMP were an intracellular target of NO that mediated plastic changes in the retinogeniculate projection of the ferret, it should (1) be developmentally regulated during sublamination, (2) be present both in the terminals of retinal ganglion cell axons and in dLGN cells to coordinate afferent-target connectivity, (3) have its expression regulated by the activity of NMDA receptors and NOS, and (4) when inhibited block sublamination. (jneurosci.org)
  • In addition, we exposed the tissue to a number of pharmacological agents that activate or inhibit the putative intracellular pathway at different points (see Fig. 1 ), starting with NMDA receptors and including protein kinase G (PKG), a likely target of cGMP ( Wang and Robinson, 1997 ). (jneurosci.org)
  • Double dissociation of spike timing-dependent potentiation and depression by subunit-preferring NMDA receptor antagonists in mouse barrel cortex. (biomedsearch.com)
  • Spike timing-dependent plasticity (STDP) is a strong candidate for an N-methyl-D-aspartate (NMDA) receptor-dependent form of synaptic plasticity that could underlie the development of receptive field properties in sensory neocortices. (biomedsearch.com)
  • Whilst induction of timing-dependent long-term potentiation (t-LTP) requires postsynaptic NMDA receptors, timing-dependent long-term depression (t-LTD) requires the activation of presynaptic NMDA receptors at layer 4-to-layer 2/3 synapses in barrel cortex. (biomedsearch.com)
  • Here we investigated the developmental profile of t-LTD at layer 4-to-layer 2/3 synapses of mouse barrel cortex and studied their NMDA receptor subunit dependence. (biomedsearch.com)
  • An antagonist at GluN2C/D subunit-containing NMDA receptors blocked t-LTD but not t-LTP. (biomedsearch.com)
  • These data demonstrate an NMDA receptor subunit-dependent double dissociation of t-LTD and t-LTP mechanisms at layer 4-to-layer 2/3 synapses, and suggest that t-LTD is mediated by distinct molecular mechanisms at different synapses on the same postsynaptic neuron. (biomedsearch.com)
  • There are three families of ionotropic receptors: the N-methyl- d -aspartate (NMDA), the amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) and the kainate receptors. (rcpsych.org)
  • The AMPA and the kainate receptors are collectively termed 'non-NMDA' receptors and appear to control conductance of Na + and K + through channels that exhibit rapid kinetics. (rcpsych.org)
  • The most structurally complex glutamatergic receptor is the NMDA receptor. (rcpsych.org)
  • Glycine is an 'obligate co-agonist' for glutamate, i.e. glutamate cannot act on the NMDA receptor in the absence of glycine. (rcpsych.org)
  • Excitatory postsynaptic currents (EPSCs) or potentials (EPSPs) were evoked electrically at the ipsilateral dorsal root entry zone after blocking inhibitory inputs with bicuculline and strychnine, and NMDA receptors with D-2-amino-5-phosphonopentanoic acid. (jneurosci.org)
  • PCP works primarily as an NMDA receptor antagonist. (wikipedia.org)
  • LTP is initiated when the NMDA receptors are in a local environment with a voltage potential high enough to displace the positively-charged Mg2+ ion from the channel pore. (wikipedia.org)
  • As a result of the channel being unblocked, Ca2+ ions are able to enter into the postsynaptic neuron through the NMDA receptor channel. (wikipedia.org)
  • inhibition
  • Crunelli V and Leresche N (1991) A role for GABAB receptors in excitation and inhibition of thalamorcortical cells. (els.net)
  • Thompson SM, Capogna M and Scanziani M (1993) Presynaptic inhibition in the hippocampus. (els.net)
  • Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. (wikipedia.org)
  • 1991
  • A quantal analysis of the increased synaptic activity indicates that 5-HT 3 receptors elicit this effect by activating GABAergic interneurons ( Ropert and Guy, 1991 ). (aspetjournals.org)
  • Conversely
  • Conversely, a GluN2A subunit-preferring antagonist blocked t-LTP but not t-LTD. The GluN2C/D subunit requirement for t-LTD appears to be synapse specific, as GluN2C/D antagonists did not block t-LTD at horizontal cross-columnar layer 2/3-to-layer 2/3 synapses, which was blocked by a GluN2B antagonist instead. (biomedsearch.com)
  • inhibits
  • GABAB receptor activation inhibits exocytosis in rat pancreatic beta-cells by G-protein-dependent activation of calcineurin. (abcam.com)
  • Kappa-bungarotoxin is a receptor antagonist, meaning it blocks the normal response of the receptor to acetylcholine, which inhibits neurotransmission and therefore causes neuromuscular paralysis. (wikipedia.org)
  • subunit
  • Two distinct binding surfaces, both on the N-terminal extracellular face of the receptor subunit, have been identified. (wikipedia.org)
  • This could indicate that the 5-HTR3B receptor subunit could be used as biomarker of antiemetic drug efficacy. (wikipedia.org)
  • glycine
  • where glycine receptors are rare ( Frostholm and Rotter, 1985 ), strongly support the notion that some of the toxic effects of this alkaloid can be accounted for by its action on receptors other than the glycine receptors in the CNS. (aspetjournals.org)
  • GABAB
  • Dutar P and Nicoll RA (1988) A physiological role for GABAB receptors in the central nervous system. (els.net)
  • Wojcik WJ and Neff NH (1984) GABAB receptors are negatively coupled to adenylyl cyclase and in the cerebellum these receptors may associate with granule cells. (els.net)
  • Bowery NG, Kerr DIB and Ong J (1997) GABAB receptors: role and therapeutic implications in CNS disorders. (els.net)
  • Kerr DIB and Ong J (1995) GABAB receptors. (els.net)
  • Misgeld U, Bijak M and Jarolimek W (1995) A physiological role for GABAB receptors and the effects of baclofen in the mammalian central nervous system. (els.net)
  • Wojcik JW and Holopainen I (1992) Role of central GABAB receptors in physiology and pathology. (els.net)
  • activation
  • These effects were shown to be caused by activation of presynaptic 5-HT 1A receptors because similar effects were produced by the local infusion of 8-OH-DPAT within the raphe nuclei, and administration of 5-HT 1A receptor antagonists into the raphe nuclei prevented the effects of 8-OH-DPAT when given systemically ( Kreiss and Lucki, 1994 ). (aspetjournals.org)
  • Previous studies have attributed this effect to the activation of HT-5 3 receptors located on GABAergic interneurons. (aspetjournals.org)
  • Direct evidence for the depolarization and activation of GABAergic interneurons by 5-HT 3 receptors has been obtained recently in the dentate gyrus ( Kawa, 1994 ). (aspetjournals.org)
  • When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5-Carboxamidotryptamine can be used in conjunction with selective antagonists for its other targets (principally 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT7). (wikipedia.org)
  • Surprisingly however 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels, despite its role in modulating serotonin release. (wikipedia.org)
  • Activation of the μ-opioid receptor by an agonist such as morphine causes analgesia, sedation, slightly reduced blood pressure, itching, nausea, euphoria, decreased respiration, miosis (constricted pupils), and decreased bowel motility often leading to constipation. (wikipedia.org)
  • There are many additional signal cascade components that include the formation of arachidonic acid through PLA2 activity, activation of phospholipase D, Rho/Rho kinase, and ERK pathway activation initiated by agonist stimulation of the receptor. (wikipedia.org)
  • Activation of the 5-HT2A receptor in hypothalamus causes increases in hormonal levels of oxytocin, prolactin, ACTH, corticosterone, and renin. (wikipedia.org)
  • extracellular
  • When challenged with the 5-HT 1A receptor agonist 8-hydroxy-2-(di- n -propylamino) tetralin (8-OH-DPAT), EMD 68843-induced increases in extracellular 5-HT were greatly reduced in the HPv but to a lesser extent in the FC. (aspetjournals.org)
  • adenosine
  • Instead, by using the selective A 1 antagonist 8-cyclopentyl-1,3-dipropylxanthine and a novel adenosine sensor, we demonstrate that adenosine production is reduced with repeated episodes of hypoxia. (jneurosci.org)
  • Here we used the expression of Nur77 , a transcription factor of the orphan nuclear receptor family, as readout to explore the role of dopamine, glutamate, and adenosine receptors in the effect of a dopamine D 2 antagonist in the striatum. (frontiersin.org)
  • Direct modulation of Nur77 expression by striatal glutamate and adenosine receptors was confirmed using corticostriatal organotypic cultures. (frontiersin.org)
  • The most prominent is that it reversibly blocks the action of adenosine on its receptor and consequently prevents the onset of drowsiness induced by adenosine. (wikipedia.org)
  • interneurons
  • We interpret these results to indicate that 5-HT 2 receptors activate GABAergic interneurons in the slice, leading to an increase in GABAergic synaptic activity onto pyramidal cells of the CA1 region. (aspetjournals.org)
  • ionotropic receptor
  • It is the only ionotropic receptor to control Ca 2+ conductance in addition to the conductance of Na + and K + . When the channel is activated there is an influx of Na + and Ca 2+ ions and an efflux of K + ions. (rcpsych.org)
  • activate
  • Studies of the activity of the terminal 5-HT 1B receptor have been limited by the lack of a selective 5-HT 1B receptor agonist that can activate the 5-HT 1B receptor on systemic administration. (aspetjournals.org)
  • Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. (wikipedia.org)
  • The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. (wikipedia.org)
  • selective
  • Because yohimbine has highest affinity for the α2 receptor, small doses can increase blood pressure by causing a relatively selective α2 blockade. (wikipedia.org)
  • Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused mainly on the role of adenosine receptors in the heart, and led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest. (wikipedia.org)
  • However the development of more highly selective A2A ligands has led towards other applications, with the most significant focus of research currently being the potential therapeutic role for A2A antagonists in the treatment of Parkinson's disease. (wikipedia.org)
  • localization
  • Dopamine receptor localization (red and orange bars-see key) is inferred from the D1 and D2 receptor immunohistochemistry in the present study: solid versus dotted bars indicate unambiguous versus ambiguous localization, respectively. (jneurosci.org)
  • noradrenergic
  • Baisley SK, Fallace KL, Rajbhandari AK, Bakshi VP (2012) Mutual independence of 5-HT 2 and α1 noradrenergic receptors in mediating deficits in sensorimotor gating. (springer.com)
  • neurokinin
  • Abnormal levels of Substance P have been reported in depression, which led to development of potential antidepressants that interact with neurokinin receptors. (schoolbag.info)
  • Regulation
  • Therefore, it is worthwhile to consider what presynaptic molecular mechanisms might influence the amount of glutamate released into the synaptic cleft and whether such mechanisms might be endogenously controlled to provide additional modes of synaptic regulation. (jneurosci.org)
  • The P2X7 receptor also serves as a pattern recognition receptor for extracellular ATP-mediated apoptotic cell death, regulation of receptor trafficking, mast cell degranulation, and inflammation. (wikipedia.org)
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, drug addiction and Parkinson's disease. (wikipedia.org)
  • central and peripheral
  • The receptor is found in the central and peripheral nervous systems, in microglia, in macrophages, in uterine endometrium, and in the retina. (wikipedia.org)
  • The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. (wikipedia.org)
  • The receptor is found in the central and peripheral nervous systems, in the epithelia of ducted glands and airways, in the smooth muscle of the bladder, gastrointestinal tract, uterus, and arteries, in uterine endometrium, and in fat cells. (wikipedia.org)
  • primarily
  • Consistent with the known mechanism of action of hallucinogens in humans, the behavioral effects of hallucinogens in rodents are mediated primarily by activation of 5-HT 2A receptors. (springer.com)
  • The H3 receptor is primarily localized in the central nervous system, and it acts not only as a presynaptic autoreceptor that modulates the HA release but also as a presynaptic heteroreceptor that regulates the release of other neurotransmitters such as monoamines and amino acids. (readbyqxmd.com)
  • P2X7
  • P2X7 receptors do not become desensitized readily and continued signaling leads to the aforementioned increased permeability and an increase in current amplitude. (wikipedia.org)
  • P2X7 receptors respond to BzATP more readily than ATP. (wikipedia.org)
  • P2X7 receptors are sensitive to pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS) and relatively insensitive to suramin, but the suramin analog, NF279, is much more effective. (wikipedia.org)
  • In microglia, P2X7 receptors are found mostly on the cell surface. (wikipedia.org)
  • Activation of the P2X7 receptor by ATP leads to recruitment of pannexin pores which allow small molecules such as ATP to leak out of cells. (wikipedia.org)
  • Moreover, P2X7 receptor signaling increases the release of proinflammatory molecules such as IL-1β, IL-6, and TNF-α. (wikipedia.org)
  • In addition, P2X7 receptors have been linked to increases in proinflammatory cytokines such as CXCL2 and CCL3. (wikipedia.org)
  • The permeabilizing ATP receptor, P2X7. (wikipedia.org)