Rats gaba a receptor agonists. Medical search. Frequent questions

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 benzodiazepine antagonist flumazenil, however, fails to alter the anticonvulsant activity of loreclezole, indicating that loreclezole is not a benzodiazepine receptor agonist. (wikipedia.org)
Using CsCl-containing microelectrodes with QX314, we isolated mPSCs that were sensitive to the GABA A receptor antagonist, bicuculline. (unl.edu)
The dual HCRT receptor antagonist almorexant (ALM) decreases waking and increases sleep. (sri.com)
The type 1 neurokinin receptor (NK1R) antagonist aprepitant and its i.v. prodrug fosaprepitant have been approved for prevention of acute and delayed nausea and vomiting associated with chemotherapy. (bvsalud.org)
The effect of baclofen could be mimicked by low dose GABA and taurine, actions which were blocked by prior application of a specific GABA B antagonist. (houstonmethodist.org)
The CB1 cannabinoid receptor antagonist SR141716A (10(-6) m) prevented the inhibition produced by WIN55212-2 (10(-5) m). (cannabisuk.com)
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)
9,10 Conversely, microinjecting the GABA A receptor antagonist bicuculline into the pontine reticular formation increases REM sleep and decreases wakefulness. (silverchair.com)
The 'neutral' competitive antagonist burimamide alone was without effect but prevented ranitidine actions indicating that inverse agonist effects result from constitutive H(2)R activity independent of HA tone. (ox.ac.uk)

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)
In slices from morphine-dependent rats maintained in morphine (5 μ m ) in vitro , action potential frequencies of opioid-sensitive neurons did not differ from untreated control neurons but were greater than in control neurons maintained in morphine in vitro , indicating development of tolerance. (jneurosci.org)
Naloxone (100 n m or 1 μ m ) depolarized 25 of 51 neurons from morphine-dependent rats maintained in morphine in vitro , 19 of which previously had been classified as opioid-sensitive. (jneurosci.org)
Whole cell patch-clamp recordings of mIPSCs were obtained from rat and mouse SCN neurons in hypothalamic slices. (unl.edu)
Bath application of CP-93,129 (1 mM) decreased the frequency of mIPSCs by an average of 22% ( n = 7) in rat SCN neurons and by an average of 30% ( n = 8) in mouse SCN neurons with no clear effect on mIPSC amplitude. (unl.edu)
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)
To test this hypothesis, rats were given bilateral IgG-192-saporin injections, which predominantly targets cholinergic BF neurons. (sri.com)
Electrophysiological properties of VTA neurons in rat coronal midbrain slices were studied with the patch-clamp technique. (cannabisuk.com)
GABA(A) receptor-mediated inhibitory postsynaptic currents (IPSCs) were evoked by electrical stimulation in the vicinity of the recorded neurons. (cannabisuk.com)
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)
3 Synaptic terminals from local and distant γ-aminobutyric acid (GABA)-containing neurons 4,5 as well as GABA type A (GABA A ) receptors 6-8 are present in the pontine reticular formation and modulate behavioral arousal. (silverchair.com)
Here, we show that ethanol increases the concentration of 3alpha, 5alpha-THP as well as the amplitude of GABA(A) receptor-mediated IPSCs recorded from CA1 pyramidal neurons in isolated hippocampal slices. (unica.it)
Their stoichiometry in various microdomains will have a major role in determining A 2A and D 2 signaling in the striatopallidal GABA neurons. (johnshopkins.edu)
Mu-opioid receptor (MOR) agonists potently inhibited MThal inputs without affecting ACC inputs to individual striatal medium spiny neurons (MSNs). (elifesciences.org)
CB1 cannabinoid receptor agonist prevents NGF-induced sensitization of TRPV1 in sensory neurons. (wisc.edu)
Effects of local anesthetics on opioid inhibition of calcium current in rat dorsal root ganglion neurons. (wisc.edu)
Exogenous nerve growth factor attenuates opioid-induced inhibition of voltage-activated Ba2+ currents in rat sensory neurons. (wisc.edu)
HSP90 inhibitors alter capsaicin- and ATP-induced currents in rat dorsal root ganglion neurons. (wisc.edu)
Local anesthetic inhibition of voltage-activated potassium currents in rat dorsal root ganglion neurons. (wisc.edu)
Magnetic resonance imaging volume reconstruction and immunofluorescence analysis of grafted cell survival showed near complete injury-cavity-filling by grafted cells and development of putative GABA-ergic synapses between grafted and host neurons. (biomedcentral.com)
7. Lindvall, O., Björklund, A.: Organization of catecholamine neurons in the rat central nervous system. (lu.se)

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)
This effect was associated with decreased activation of pathways linked to neurotrophin and glutamate receptor signaling. (researchgate.net)
BF adenosine (ADO), γ-amino-butyric acid (GABA), and glutamate levels were then determined via microdialysis from intact, freely behaving rats following oral ALM, ZOL or VEH. (sri.com)
In the central nervous system, endogenous H 2 S potentiates N-methyl-D-aspartate receptor-mediated currents and long-term potentiation (LTP), enhances the effect of GABA, regulates intracellular calcium levels, and stimulates uptake of synaptic glutamate by astrocytes [ 16 , 17 ]. (biomedcentral.com)
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)
or = 20 Hz), and prevailed in the presence of antagonists of GABA, glutamate or H(3)-HA receptors. (ox.ac.uk)

Effects of steroids on gamma-aminobutyric acid receptors expressed in Xenopus oocytes by poly(A)+ RNA from mammalian brain and retina. (aspetjournals.org)
Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. (aspetjournals.org)
Baclofen a gamma-aminobutyric acid (GABA)B receptor agonist has been used clinically to treat muscle spasticity rigidity and pain. (pkc-inhibitor.com)
Many general anesthetics are thought to produce a loss of wakefulness, in part, by enhancing gamma-aminobutyric acid (GABA) neurotransmission. (silverchair.com)
Four sesquiterpenes, beta-selinene, isocurcumenol, nootkatone and aristolone and one triterpene, oleanolic acid were isolated from the ethylacetate fraction of the rhizomes of Cyperus rotundus and tested for their ability to modulate gamma-aminobutyric acid (GABA(A))-benzodiazepine receptor function by radioligand binding assays using rat cerebrocortical membranes. (lookformedical.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)
GABA responses expressed by bovine retina poly(A)+ RNA also were Cl- currents but were composed of two pharmacologically distinct components, one mediated by GABAA receptors and the other by GABA receptors with novel properties, which were resistant to bicuculline but were not activated by R(+)-baclofen, a selective agonist of GABAB receptors. (aspetjournals.org)
The discovery provided a potential mechanism to account for the widespread use of indirect-acting 5-HT receptor agonists - such as selective serotonin re-uptake inhibitors - in combination with opioids for treating pain. (buffalo.edu)
The effect of the selective human MC3 receptor agonist PG992 on high density human chondrocyte micromass cultures activated by IL-1beta. (westminster.ac.uk)
These effects are shared by the neurosteroid precursor progesterone, the peripheral benzodiazepine receptor-selective agonist CB34, and gamma-hydroxybutyrate, all of which are known to increase the formation of neuroactive steroids in plasma and in the brain. (unica.it)
Selective H(2)R antagonists (inverse agonists) ranitidine and tiotidine enhanced 5-HT release while the agonist amthamine suppressed release. (ox.ac.uk)
10. Lindvall, O., Björklund, A., Skagerberg, G.: Selective histochemical demonstration of dopamine terminal systems in rat di- and telencephalon: new evidence for dopaminergic innervation of hypothalamic neurosecretory nuclei. (lu.se)

These results suggest that isocurcumenol may serve as a benzodiazepine receptor agonist and allosterically modulate GABAergic neurotransmission via enhancement of endogenous receptor ligand binding. (lookformedical.com)

Loreclezole is a sedative and an anticonvulsant which acts as a GABAA receptor positive allosteric modulator. (wikipedia.org)
GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. (aspetjournals.org)
Threshold levels of potentiation were detectable using 1-2 nM steroid, and at concentrations of 50 and 500 nM 3 alpha-OH-DHP shifted the EC50 of cortex GABAA responses from a control value of 92 +/- 20 microM GABA to 40 +/- 4.3 microM and 13 +/- 1.8 microM, respectively. (aspetjournals.org)
However, even at concentrations as high as 50 microM, 3 alpha-OH-DHP did not itself elicit appreciable membrane current responses through direct activation of the cortex GABAA receptors. (aspetjournals.org)
4-Amino-7-hydroxy-2-methyl-5,6,7,8,-tetrahydrobenzo[b]thieno[2,3-b]pyridine-3-carboxylic acid, but-2-ynyl ester (SB-205384) and other γ-aminobutyric acidA (GABAA) receptor modulators were tested for their effects on GABA-activated chloride currents in rat cerebellar granule cells by use of the whole-cell patch clamp technique. (herts.ac.uk)
The major effect of SB-205384 on GABAA-activated current was an increase in the half-life of decay of the response once the agonist had been removed. (herts.ac.uk)
This is in contrast to many GABAA receptor modulators that have previously been shown to potentiate GABA-activated currents. (herts.ac.uk)
Neuroactive steroids such as 3alpha-hydroxy-5alpha-pregnan-20-one (3alpha, 5alpha-THP) are, in fact, potent and efficacious endogenous positive modulators of GABAA receptor function. (unica.it)

Monoacylglycerol lipase protects the presynaptic cannabinoid 1 receptor from desensitization by endocannabinoids after persistent inflammation. (iasp-pain.org)
Inhibition of GABA release by presynaptic mu opioid receptors (MORs) in the vlPAG does not desensitize with persistent inflammation. (iasp-pain.org)
These adaptations with inflammation have important implications for the development of cannabinoid-based pain therapeutics targeting MAGL and CB1Rs.Presynaptic G protein-coupled receptors are resistant to desensitization. (iasp-pain.org)
Here we find that persistent inflammation increases endocannabinoid levels, priming presynaptic cannabinoid 1 receptors for desensitization upon subsequent addition of exogenous agonists. (iasp-pain.org)
Endocannabinoids readily induce cannabinoid 1 receptor desensitization if their degradation is blocked, indicating that endocannabinoid concentrations are maintained at sub-desensitizing levels and that degradation is critical for maintaining endocannabinoid regulation of presynaptic GABA release in the ventrolateral periaqueductal gray during inflammatory states. (iasp-pain.org)
5-HT 1B Receptor-Mediated Presynaptic Inhibition of GABA Rel" by Jayne R. Bramley, Patricia J. Sollars et al. (unl.edu)
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)
The results indicate that activation of CB1 cannabinoid receptors inhibits GABAergic neurotransmission in the VTA with a presynaptic mechanism. (cannabisuk.com)
Furthermore, ethanol affects GABA(A) receptor activity through a presynaptic action, an effect that is not dependent on neurosteroid formation. (unica.it)

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)
No effect was observed upon administration of muscimol to LA rats. (scirp.org)
For example, microinjecting the GABA A receptor agonist muscimol into the pontine reticular formation increases wakefulness. (silverchair.com)

For this purpose, WIN 55,212-2 was injected in pregnant wistar rats from gestation day 5 to 20 and a detailed analysis of the levels of the neurotrophin brain-derived neurotrophic factor (BDNF) as well as of the signaling molecules extracellular signal-regulated kinase (ERK)1/2 and alpha-calcium/calmodulin-dependent protein kinase II (alpha-CaMKII) was carried out in adult offspring. (researchgate.net)

These findings suggest that clozapine potentiates the GABA B receptor and also underscores the possibility that the GABA B receptor may play a key role in the treatment of SCZ. (biomedcentral.com)

Cannabinoid receptor subtype 1 (CB1Rs) inhibition of spontaneous, miniature and evoked GABAergic postsynaptic currents (mIPSCs and eIPSCs) in the ventrolateral periaqueductal gray (vlPAG) were compared in slices from naïve and inflamed male and female Sprague-Dawley rats. (iasp-pain.org)

Lewter is studying the behavioral effects of novel positive allosteric modulators (PAMS) for alpha-2 and alpha-3 containing GABA A receptors and the potential utility of these PAMs as analgesics. (buffalo.edu)

Here we report that activation of GABA B receptors significantly inhibits Akt/GSK-3 signaling in a β-arrestin-dependent pathway. (biomedcentral.com)

Both GABA and baclofen, but not isoguvacine, altered βAR agonist binding by increasing the affinity of both the low‐ and high‐affinity binding sites and by increasing the proportion of low‐affinity receptors. (johnshopkins.edu)
The response to baclofen was stereoselective, and the effect of GABA was not inhibited by bicuculline. (johnshopkins.edu)
The results suggest that GABA B , but not GABA A , receptor activation modifies the coupling between βAR and stimulatory guanine nucleotide‐binding protein, which may in part explain the ability of baclofen to augment isoproterenol‐stim‐ulated cyclic AMP accumulation in brain slices. (johnshopkins.edu)
In the present study therefore rats were treated with either a) TP-434 vehicle b) acute baclofen (5 mg/kg) or c) chronic baclofen (5 mg/kg t.i.d. for 5 days). (pkc-inhibitor.com)
Normally minimally ineffective in stimulating PI hydrolysis in the neonatal rat cerebellum, N-methyl-d-aspartate (NMDA) increased levels of PI hydrolysis 82.3 ± 5.5% above basal values in the presence of 1 μM baclofen, a γ-aminobutyric acid B (GABA B ) receptor agonist. (houstonmethodist.org)
Smith, SS & Li, J 1991, ' GABA B receptor stimulation by baclofen and taurine enhances excitatory amino acid induced phosphatidylinositol turnover in neonatal rat cerebellum ', Neuroscience Letters , vol. 132, no. 1, pp. 59-64. (houstonmethodist.org)
As well, the GABA B receptor agonist, baclofen has been reported to have some efficacy in SCZ patients [ 4 ]. (biomedcentral.com)

In this study, postnatal day 7 (P7) Sprague-Dawley rats were randomly divided into four groups: control group (normal saline), H 2 S group (NaHS 28 μM/kg), isoflurane group (normal saline +0.75% isoflurane) and H 2 S preconditioning group (NaHS 28 μM/kg + 0.75% isoflurane). (biomedcentral.com)
Three-month-old female Sprague-Dawley rats received L3 spinal compression injury. (biomedcentral.com)

A potential benzodiazepine-like interaction with GABA receptors is suggested by the observation that the anticonvulsant effects of loreclezole can be reversed by benzodiazepine receptor inverse agonists. (wikipedia.org)

2-AG tone is detected in slices from CFA-treated rats when GRK2/3 is blocked suggesting an increase in 2-AG synthesis after persistent inflammation. (iasp-pain.org)
The interaction of isoproterenol with β‐adrenergic receptor (βAR) binding sites was measured in membranes prepared from rat brain cerebral cortical slices previously incubated in the presence or absence of γ‐aminobutyric acid (GABA) receptor agonists. (johnshopkins.edu)
Agonist stimulation of GABA B receptors enhances the phosphorylation of Akt (Thr-308) and enhances the phosphorylation of GSK-3α (Ser-21)/β (Ser-9) in both HEK-293T cells expressing GABA B receptors and rat hippocampal slices. (biomedcentral.com)
Here we have explored regulation by another HA receptor expressed in SNr, the H(2)-receptor (H(2)R), by monitoring electrically evoked 5-HT release with fast-scan cyclic voltammetry at carbon-fiber microelectrodes in SNr in rat brain slices. (ox.ac.uk)

ALM increased BF ADO (an endogenous sleep-promoting substance) and GABA (which is increased during normal sleep), and required an intact BF for maximal efficacy, whereas ZOL blocked sleep-associated BF GABA release, and required no functional contribution from the BF to induce sleep. (sri.com)
Endocannabinoid System is a biological system involving the endogenous lipid-based retrograde neurotransmitters which bind to the cannabinoid receptors, as well as the cannabinoid receptor proteins which are in the CNS and PNS. (slideshare.net)
Therefore, identification of novel endogenous targets for drug development may have beneficial properties ACTH4-10, a heptapeptide fragment derived from the hormone adrenocorticotrophin (ACTH) modulates the inflammatory response in a corticosterone-independent manner, via agonism at melanocortin type 3 receptors (MC3-R) expressed on peritoneal macrophages. (westminster.ac.uk)
As of the time of the publication of this paper, however, the interaction of endogenous taurine with GABA-A receptors in vivo remained uncertain. (life-enhancement.com)
The authors thus note, "[b]y far the strongest evidence speaks in favor of glycine receptors being the major and most specific target of endogenous taurine. (life-enhancement.com)

However, MRK-409 has greater agonist efficacy at the α3 compared with α1 subtypes (respective efficacies relative to the full agonist chlordiazepoxide of 0.45 and 0.18). (bvsalud.org)
The cannabinoid type 2 (CB2) receptor is primarily expressed on glial cells only when there is active inflammation and appears to be devoid of undesired psychotropic effects or addiction liability  Anandamide has low intrinsic activity but enhanced during pathological conditions and 2-AG acts as a full agonist. (slideshare.net)

After exposure to isoflurane for 6 h, half the numbers of rats in each group were euthanized, and the hippocampus and cerebral cortex were dissected and examined for apoptosis by the terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling (TUNEL) technique and western blot. (biomedcentral.com)
The TUNEL assay and western blot showed that when rats were preconditioned with NaHS, neuroapoptosis decreased significantly both in hippocampus and cerebral cortex compering with the isofulrane group. (biomedcentral.com)

Chloride ions in the pore of glycine and GABA channels shape the time course and voltage dependence of agonist currents. (ox.ac.uk)
In the vertebrate CNS, fast synaptic inhibition is mediated by GABA and glycine receptors. (ox.ac.uk)
Here we extend these findings to measure the effects of both extracellular and intracellular chloride on the deactivation of glycine and GABA currents at both negative and positive holding potentials. (ox.ac.uk)
Currents were elicited by fast agonist application to outside-out patches from HEK-293 cells expressing rat glycine or GABA receptors. (ox.ac.uk)
Our main finding is that glycine and GABA receptors "sense" chloride concentrations because of interactions between the M2 pore-lining domain and the permeating ions. (ox.ac.uk)
GABARs belong to the superfamily of ligand-gated ion channels that includes the glycine, nicotinic cholinergic (nAChR), and 5-hydroxytryptamine receptors. (aspetjournals.org)
Interestingly, taurine has been reported to interact with neurotransmitter receptors involved in sleep regulation, including GABA-A, GABA-B, and glycine. (life-enhancement.com)

However, the downstream molecular mechanisms related to GABA potentiation remain unexplored. (biomedcentral.com)
Most anesthetic drugs potentiate GABA A receptor-mediated inhibition, and this potentiation is thought to comprise part of the mechanism by which general anesthetics produce hypnosis. (silverchair.com)

Recent studies have suggested that dopamine D2 receptor antagonists, which are used in the clinical treatment of schizophrenia, modulate protein kinase B (Akt)/glycogen synthase kinase (GSK)-3 signaling. (biomedcentral.com)
These observations suggest that ethanol may modulate GABA(A) receptor function through an increase in de novo neurosteroid synthesis in the brain that is independent of the HPA axis. (unica.it)

The current study demonstrates that H 2 S attenuates isoflurane-induced neuroapoptosis and improves cognitive impairments in the developing rat brain. (biomedcentral.com)
This compound readily penetrates the brain in rats and occupies the benzodiazepine site of GABA(A) receptors, measured using an in vivo [(3)H]flumazenil binding assay, with an Occ(50) of 2.2 mg/kg p.o. and a corresponding plasma EC(50) of 115 ng/mL. (bvsalud.org)
γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the vertebrate brain, and fast inhibitory postsynaptic potentials are mediated by GABA A receptors (GABARs). (aspetjournals.org)
Because neurosteroids can be synthesized de novo in the brain, we have investigated whether ethanol might affect both neurosteroid synthesis and GABA(A) receptor function in isolated rat hippocampal tissue. (unica.it)
2. Lindvall, O., Björklund, A.: The organization of the ascending catecholamine neuron systems in the rat brain as revealed by the glyoxylic acid fluorescence method. (lu.se)

These data demonstrate a direct RLN3/RXFP3 action in the PVN of male and female rats, identify the associated ionic mechanisms, and reveal that hypothalamic RLN3/RXFP3 signaling regulates binge-eating behavior. (jneurosci.org)
Constitutive histamine H2 receptor activity regulates serotonin release in the substantia nigra. (ox.ac.uk)

MC3-R agonists inhibit cytokine formation and subsequent neutrophil migration, while antagonists abrogate these effects. (westminster.ac.uk)

Therefore, the ability of NMDA to stimulate PI hydrolysis in neonatal cerebellar tissue may be regulated by the degree of GABA B receptor stimulation. (houstonmethodist.org)
This is consistent with the fact that activation of GABA-A receptors counteracts the activation of NMDA receptors and generation of nitric oxide. (life-enhancement.com)

Clozapine also increased 3 H]-CGP54626A binding at GABA B R1 subunit when HEK293 cells overexpressed GABA B receptors, highlighting a potential therapeutic target for clozapine. (biomedcentral.com)
A new γ-aminobutyric acid (GABA) A receptor (GABAR) subunit class, ε, has recently been cloned and shown to form functional channels when coexpressed with both α and β subunits. (aspetjournals.org)
We report that the combination of α1β3ε subunit subtypes expressed in L929 cells produced functional chloride ion channels that were both spontaneously active and gated by the application of extracellular GABA. (aspetjournals.org)
These data extend the pharmacological characterization of ε-containing GABARs and demonstrate that incorporation of the ε subunit permits spontaneous channel gating while preserving the structural information necessary for GABA sensitivity. (aspetjournals.org)

Using native rat and cloned human GABA-A receptors, loreclezole strongly potentiated GABA-activated chloride current. (wikipedia.org)

It is principally an agonist for the γ-aminobutyric acid (GABA) type A receptor [ 8 ], thereby altering synaptic function [ 9 ]. (biomedcentral.com)

He demonstrated that rats' feeding conditions significantly modify the behavioral effects of direct- and indirect-acting serotonin (5-HT) receptor agonists. (buffalo.edu)
One identified role is the regulation of serotonin (5-HT) neurotransmission via the HA-H(3) receptor. (ox.ac.uk)

Moreover, we reveal that, in male and female rats, this action depends on M-like potassium conductance. (jneurosci.org)
Moreover, we elucidated the neuronal mechanism of RLN3/RXFP3 signaling in PVN in male and female rats and characterized sex differences in the RLN3 innervation of the PVN. (jneurosci.org)
Circuit and cell-specific contributions to decision making involving risk of explicit punishment in male and female rats. (ufl.edu)

Various neuropeptides play important roles in the regulation of feeding behavior, including relaxin-3 (RLN3), which stimulates food intake in rats through the activation of the relaxin-family peptide-3 receptor (RXFP3). (jneurosci.org)
Finally, in a model of binge-eating in female rats, RXFP3 blockade within the PVN prevented binge-eating behavior. (jneurosci.org)
Using a model of binge-eating, we demonstrated that relaxin-3/RXFP3 signaling in the hypothalamic paraventricular nucleus (PVN) is necessary for the expression of binge-eating behavior in female rats. (jneurosci.org)
Zawilska and Wojcieszak, 2014 ), but use of WIN can clarify the effects of cannabinoid receptor agonist SA on behavior. (nature.com)

Furthermore, knocking down the expression of β-arrestin2 using siRNA abolishes the GABA B receptor-mediated modulation of GSK-3 signaling. (biomedcentral.com)
Modulation of radioligand binding to the GABA(A)-benzodiazepine receptor complex by a new component from Cyperus rotundus. (lookformedical.com)

Decreasing pontine reticular formation GABA levels comprises one mechanism by which isoflurane causes loss of consciousness, altered cortical excitability, muscular hypotonia, and decreased respiratory rate. (silverchair.com)
in many instances taurine exerted its cytoprotective effects against excitotoxic and/or energy depriving insults in vitro by a mechanism involving interaction with GABA-A receptors. (life-enhancement.com)

Despite the reduced efficacy of exogenous agonists, endocannabinoids have prolonged efficacy after persistent inflammation. (iasp-pain.org)

Transcranial magnetic stimulation (TMS) indices of GABA B receptor mediated inhibitory neurotransmission can be altered through antipsychotic treatment. (biomedcentral.com)
Suchankova P, Engel JA , Jerlhag E. Sub-chronic Ghrelin Receptor Blockade Attenuates Alcohol- and Amphetamine-Induced Locomotor Stimulation in Mice. (neurotree.org)

MRK-409 binds to α1-, α2-, α3- and α5-containing human recombinant GABA(A) receptors with comparable high affinity (0.21-0.40 nM). (bvsalud.org)
However, spontaneous channel activity has been reported in recombinant α4β1 receptors as well as β1 or β3 homomeric receptors, although these isoforms are insensitive to activation by GABA. (aspetjournals.org)

Unexpectedly, while CB1R desensitization significantly reduces inhibition produced by exogenous agonists, depolarization-induced suppression of inhibition (DSI) protocols that promote 2-AG synthesis exhibit CB1R activation after inflammation. (iasp-pain.org)
He also discovered that agonists acting at 5-HT2A receptors significantly enhance the antinociceptive effects of opioid receptor agonists without enhancing the drugs' abuse-related effects. (buffalo.edu)
Relative to wakefulness, GABA levels were significantly decreased by isoflurane. (silverchair.com)

Together, these data highlight MC3-R as a potential therapeutic target and suggest that small molecule agonists directed at MC3-R with more specific actions, may be potentially novel therapeutics for treating this pathology. (westminster.ac.uk)

For hypothesis 2, rats (n = 10) were implanted with a guide cannula aimed for the pontine reticular formation. (silverchair.com)

Furthermore, a robust reduction of total and phospho-alpha-CaMKII was found in the hippocampus of rats prenatally exposed to WIN 55,212-2. (researchgate.net)

While 16α-hydroxyestrone has relatively weak affinity for estrogen receptor, it has prolonged effect due to covalent binding to the receptor. (helsinki.fi)

9. Björklund, A., Skagerberg, G.: Evidence for a major spinal cord projection from the diencephalic A11 dopamine cell group in the rat. (lu.se)

CB2 RECEPTORS IN ALZEHIMER'S DISEASE Ester Aso and Isidro ferrer, frontiers in neuroscience, 2016 Front. (slideshare.net)

BFx and intact rats were then given oral ALM, the benzodiazepine agonist zolpidem (ZOL) or vehicle (VEH) at lights-out. (sri.com)
In adult rats, we determined the effects of bilateral zolpidem (an agonist of the BZD 1 receptor site) microinfusions in the anterior or in the posterior SNR (SNR(anterior) or SNR(posterior), respectively) on flurothyl-induced clonic and tonic-clonic seizures. (elsevierpure.com)
In 15 day old (PN 15) rats, the SNR microinfusions of zolpidem had anticonvulsant effects on clonic and tonic- clonic seizures. (elsevierpure.com)

Some of the receptors are cation channels, which can directly depolarize the nociceptor upon activation, while other receptors activate second messenger systems to change neuronal excitability by changing expression of, or modifying the function of, other cation channels. (frontiersin.org)
Activation of the CB1 receptor can produce two peaks of ceramide. (slideshare.net)
CB2 RECEPTORS and microglia Yutaka Nakagawa, pharmaceuticals, 2014  Microglial activation occurs in response to diverse CNS insults, and as a result, a transition is seen in microglial phenotype from anti-inflammatory to the reactive (proinflammatory) phenotype. (slideshare.net)

The cortical silent period (CSP) represents a TMS neurophysiological index of GABA B receptor mediated inhibitory neurotransmission whereas short interval cortical inhibition (SICI) represents a TMS neurophysiological index of GABA A receptor mediated inhibitory neurotransmisssion. (biomedcentral.com)

An interaction with the GABA type A (GABA(A)) receptor has long been recognized as one of the main neurochemical mechanisms underlying many of the pharmacological actions of ethanol. (unica.it)
However, they also noted that, "exogenous taurine has in many instances turned out to have profound neuroprotective effects, many of which can be ascribed to interaction with GABA-A receptors. (life-enhancement.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)

Functional properties of ryanodine receptors from rat dorsal root ganglia. (wisc.edu)

To investigate whether tenascin-C and tenascin-R may play important functional roles in the lesioned central nervous system, we have analysed their expression in the olivocerebellar system of the adult rat after 3-acetylpyridine-induced degeneration of nerve cells in the inferior olivary nucleus. (researchgate.net)
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)
Touchscreen-Based Cognitive Training Alters Functional Connectivity Patterns in Aged But Not Young Male Rats. (ufl.edu)

The amplitude of IPSCs was depressed by the synthetic mixed CB1/CB2 cannabinoid receptor agonist WIN55212-2 (10(-6) and 10(-5) m). (cannabisuk.com)

In the presence of clozapine, a left shift was shown for specific 3 H]-CGP54626A binding in competition with different concentrations of GABA. (biomedcentral.com)

Anatomy15

Organisms7

Diseases1

Chemicals and Drugs204

Analytical, Diagnostic and Therapeutic Techniques and Equipment9

Psychiatry and Psychology2

Phenomena and Processes16

Disciplines and Occupations1

Health Care1

Antagonist11

Neurons23

Glutamate8

Gamma-amin5

Selective7

Benzodiazepine receptor agonist1

GABAA8

Presynaptic9

Muscimol3

Wistar1

Potentiates1

GABAergic1

Modulators1

Inhibits1

Baclofen7

Sprague-Dawley2

Inverse agonists1

Slices4

Endogenous5

Full agonist2

Cerebral Cortex2

Glycine7

Potentiation2

Modulate2

Brain5

Regulates2

Antagonists1

NMDA2

Subunit4

Chloride1

Type A receptor1

Serotonin2

Male and female3

Behavior4

Modulation2

Mechanism2

Efficacy1

Stimulation2

Recombinant2

Significantly3

Potential therapeutic target1

Hypothesis1

Hippocampus1

Affinity1

Dopamine1

Neuroscience1

Zolpidem3

Activation3

Cortical1

Interaction2

Pyramidal1

Dorsal1

Functional3

IPSCs1

Concentrations1