Responses gaba a receptor antagonists. Medical search. Frequent questions

Taken together these separate lines of evidence suggest that the effects of GABA in central neurons can be mediated by heteromeric complexes of GABA A and GABA C receptor subunits. (jneurosci.org)
The excitatory center and classical inhibitory surround of the RF together control the responses of neurons to a stimulus inside the RF, whereas the extraclassical surround controls the modulation of the neuron's responses by a competing stimulus outside the RF. (nature.com)
We also review current models for the mechanisms of GABA-mediated synchronization of neural activity, focusing on parvalbumin-positive GABA neurons, which are altered in schizophrenia and whose function has been strongly linked to the production of neural synchrony. (hindawi.com)
GABAergic responses of acutely dissociated rat retinal neurons, including both bipolar cells (BCs) and other, morphologically round cells (RCs), were assayed with the fluorescent (FL), voltage-sensitive probe oxonol DiBaC4(5). (nih.gov)
This variation has been useful experimentally to identify the structurally heterogeneous populations of receptors produced in neurons and has raised the possibility that selective drugs could be developed to target specific GABAR isoforms. (aspetjournals.org)
We used single neuron recordings and controlled whisker deflections to examine responses of thalamocortical neurons to sensory stimulation in rat survivors of 9 min of asphyxial cardiac arrest incurred on post-natal day 17. (cdc.gov)
We found that 48-72 hours after cardiac arrest, thalamocortical neurons demonstrate significantly elevated firing rates both during spontaneous activity and in response to whisker deflections. (cdc.gov)
Despite the overall increase in firing, by 6 weeks, thalamocortical neurons display degraded receptive fields, with decreased responses to adjacent whiskers. (cdc.gov)
Altogether, we suggest that borneol contributes in part toward mediating the inhibitory GABA and glycine transmission on the SG neurons of the Vc and may serve as an herbal therapeutic for orofacial pain ailments. (kjpp.net)
Ethanol binds to postsynaptic GABAA receptors (inhibitory neurons). (medscape.com)
Bumetanide (20 μM), a NKCC1 antagonist, partially suppressed muscimol-induced excitation in large neurons. (arizona.edu)
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)

Responses to GABA C agonists were also enhanced by the GABA A receptor modulator pentobarbitone (300 μM). (jneurosci.org)
Electrophysiology revealed that responses to GABA C receptor agonists were enhanced by the GABA A receptor modulator zolpidem (500 n m ), which acts on the α1 subunit when the γ2 subunit is also present. (jneurosci.org)
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. (lookformedical.com)
Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. (wakehealth.edu)
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)

Proximal cortical feedback inputs can relieve the tonic Mg block of NMDA receptors (NMDARs) at distal synapses and gate dendrodendritic inhibition onto mitral cells. (jneurosci.org)
Tetanic stimulation of axons in the granule cell layer (GCL) not only activates granule cells but also relieves the Mg blockade of NMDA receptors at distal dendrodendritic synapses ( Halabisky and Strowbridge, 2003 ). (jneurosci.org)
In the voltage-clamp mode, holding at -60 mV, the borneol-induced non-desensitizing inward currents were not affected by tetrodotoxin, a voltage-gated Na + channel blocker, 6-cyano-7-nitro-quinoxaline-2,3-dione, a non- N -methyl-D-aspartate (NMDA) glutamate receptor antagonist and DL-2-amino-5-phosphonopentanoic acid, an NMDA receptor antagonist. (kjpp.net)
LTP is triggered by activation of NMDA receptors (a specific glutamate receptor). (adxs.org)
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)
Potent, selective and competitive NMDA receptor antagonist which reversibly binds to the glutamate binding site. (hellobio.com)
Measurement of NMDA Receptor Antagonist, CPP, in Mouse Plasma and Brain Tissue Following Systematic Administration Using Ion-Pair LCMS/MS. (hellobio.com)
CPP, a selective N-methyl-D-aspartate (NMDA)-type receptor antagonist: characterization in vitro and in vivo. (hellobio.com)
CPP, a new potent and selective NMDA antagonist. (hellobio.com)
A peripheral injection of the GABA-NAM MRK-016 restored hedonic behavior and AMPA-to-NMDA ratios in wild-type mice. (illinois.edu)

Fast inhibition in the nervous system is commonly mediated by GABA A receptors comprised of 2α/2β/1γ subunits. (jneurosci.org)
Fast inhibition in the CNS is principally mediated by the neurotransmitter GABA acting on GABA A and GABA C ionotropic receptors ( Macdonald and Olsen, 1994 ). (jneurosci.org)
Electrolytic lesions of the LPBN display increased water intake in response to central and peripheral injection of ANG II, the blockade of serotonin and cholecystokinin receptors of the LPBN increased water and sodium intake, suggested that exist an area that control inhibition of sodium appetite. (fapesp.br)
Here, we report that GABA(A) and GABA(B) receptor-mediated inhibition have distinct and complementary roles in balancing and terminating persistent activity. (ox.ac.uk)
These results suggest that while GABA(A) receptor-mediated inhibition is necessary for balancing persistent activity, activation of GABA(B) receptors contributes to terminating Up states. (ox.ac.uk)
Fast inhibition in the nervous system is commonly mediated by GABA(A) receptors comprised of 2alpha/2beta/1gamma subunits. (ox.ac.uk)
In addition, the inhibition was prevented by the CB 1 receptor antagonist PF 514273 (0.2 μM) but not by the TRPV1 receptor antagonist SB 366791 (10 μM). (frontiersin.org)
Since the GABAergic system is implicated in inhibition, the authors were hopeful to use the GABA agonist, baclofen (BAC), to enhance extinction of a CTA, but first a preliminary evaluation of BAC's peripheral effects on animals' sensorium had to be completed due to a lack of published literature in this area. (biomedcentral.com)
CCh also decreased the paired-pulse inhibition of field potentials and the inhibitory conductances mediated by GABA A and GABA B receptors. (biomedcentral.com)

Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. (lookformedical.com)
Peimine (Pm), an anti-inflammatory compound from Fritillaria , is known to inhibit some voltage-dependent ion channels and muscarinic receptors, but its interaction with ligand-gated ion channels remains unexplored. (mdpi.com)

Previous studies evaluated the effects of GABA receptors of LPBN on water and sodium intake in satiated and depleted-sodium rats. (fapesp.br)
Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats. (lookformedical.com)
1. The present study examined the effects of the selective 5-HT6 receptor antagonist 4-amino-N-(2, 6 bis-methylamino-pyrimidin-4-yl)-benzene sulphonamide (Ro 04-6790) on locomotor activity and unconditioned behaviour in male Sprague Dawley rats (230-300 g). 2. (lookformedical.com)
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)
Our first experiment aimed to evaluate the extent to which the GABA B agonist, BAC, altered the ability of rats to differentiate between 0.3% and 0.6% saccharin (SAC) in a two bottle preference test. (biomedcentral.com)
Given the role of the GABA B system in mediating learning and memory and its specific involvement in CTA learning and consummatory behaviors, combined with the increasing frequency of BAC use in learning, memory and addiction research, we were drawn to investigate the effects of BAC on acquisition and extinction using the CTA paradigm in rats. (biomedcentral.com)
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)
To test reward-response, we used the morphine and the nicotine induced conditioned place-preference and place-aversion model in rats with non-painful inflammation. (scirp.org)

A cDNA encoding the human gamma-aminobutyric acidA (GABAA) receptor alpha 6 subunit has been cloned and sequenced. (drugbank.com)
Recombinant human alpha 6 beta gamma 2S GABAA receptors have been expressed in both stably transfected cells and Xenopus oocytes, and the pharmacology of the benzodiazepine binding site has been determined. (drugbank.com)

The selective activity of amiloride could also be helpful for isolating the contribution of receptors composed of α6 subtypes in heterogeneous native GABAR populations. (aspetjournals.org)
4. Pretreatment (30 min) with the non-selective muscarinic antagonists scopolamine (0.1, 0.3 or 1 mg kg(-1), i.p.) and atropine (0.3, 1 or 3 mg kg(-1), s.c.) but not methylatropine (1, 3 or 10 mg kg(-1), s.c) significantly inhibited stretching induced by Ro 04-6790 (30 mg kg(-1), i.p.). 5. (lookformedical.com)
Conclusions: α5-Selective GABA-NAMs exert rapid anti-anhedonic actions and restore the strength of synapses in reward regions by acting at the benzodiazepine site of α5-containing GABA A receptors. (illinois.edu)
2021) Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC). (guidetopharmacology.org)

However, borneol-induced inward currents were partially decreased in the presence of picrotoxin, a γ-aminobutyric acid (GABA) A receptor antagonist, or strychnine, a glycine receptor antagonist, and was almost suppressed in the presence of picrotoxin and strychnine. (kjpp.net)

Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. (drugbank.com)
Characterization of receptors in a native system is a crucial issue. (biomedcentral.com)
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)

At postnatal day 15 (P15), SNR infusion of GABA A receptor agonist muscimol have proconvulsant effects in males but not in females. (elsevierpure.com)

In males, administration of an androgen receptor antagonist flutamide between P0-P2 led to the disappearance of the proconvulsant muscimol effects at P15. (elsevierpure.com)
Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ and the vitamin D receptor. (nature.com)

2016) Zinc as Allosteric Ion Channel Modulator: Ionotropic Receptors as Metalloproteins. (guidetopharmacology.org)

In this review, we summarize that the representative dimers, such as B3C, provide neuroprotection against a variety of neurotoxins via multiple targets, including the inhibitions of N-methyl-d-aspartic acid receptor with pathological-activated potential, neuronal nitric oxide synthase, and beta-amyloid cascades synergistically. (inrae.fr)
We have studied if Pm affects nicotinic acetylcholine receptors (nAChRs), since they play broad functional roles, both in the nervous system and non-neuronal tissues. (mdpi.com)
The increase of neuronal firing was antagonized by pirenzepine (M 1 /M 4 mAChRs antagonist) but not by AF-DX 116 (M 2 /M 4 mAChRs antagonist). (biomedcentral.com)

However, D-tubocurarine, a nicotinic receptor antagonist, while not blocking the ACh effect, altered the cell's apparent operating point. (northwestern.edu)

This observation demonstrates definitively that efficacy of benzodiazepine compounds cannot be generalized across receptor subtypes and may also help explain some of the behavioral effects that have been reported for these compounds. (drugbank.com)
Experiments by Jacobson and colleagues [ 4 , 14 ] used genetically altered mice lacking specific subtypes of the GABA B receptor and reported a vital role for the GABA B system in conditioned emotional responses and conditioned taste aversion (CTA) acquisition/extinction. (biomedcentral.com)
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)

6. These data suggest that systemic injection of the 5-HT6 antagonist, Ro 04-6790, produces a stretching behaviour that appears to be mediated by an increase in cholinergic neurotransmission in the CNS and which could be a useful functional correlate for 5-HT6 receptor blockade. (lookformedical.com)
Heida, JG, Velíšková, J & Moshé, SL 2008, ' Blockade of androgen receptors is sufficient to alter the sexual differentiation of the substantia nigra pars reticulata seizure-controlling network ', Epileptic Disorders , vol. 10, no. 1, pp. 8-12. (elsevierpure.com)

In a model of Up-Down states expressed in slices of rat entorhinal cortex, the GABA(A) receptor antagonist, gabazine (50-500 nM), concentration-dependently decreased Up state duration, eventually leading to epileptiform bursts. (ox.ac.uk)

In the olfactory bulb (OB), locally generated inhibitory synaptic interactions play a central role in shaping mitral and tufted cell responses to sensory stimuli ( Hamilton and Kauer, 1985 , 1989 ). (jneurosci.org)
Whereas our understanding of its pathophysiology is limited, postmortem studies suggest that schizophrenia is associated with deficits of GABA-mediated synaptic transmission. (hindawi.com)
Interestingly, a number of findings from postmortem brain studies suggest that schizophrenia is associated with deficits of GABA-mediated synaptic transmission [ 6 ]. (hindawi.com)
Alterations in the transient and steady-state electromotility transfer curves were examined by application of acetylcholine (ACh) and γ-aminobutyric acid (GABA) to the synaptic pole. (northwestern.edu)
Negative allosteric modulators of GABA A (gamma-aminobutyric acid A) receptors (GABA-NAMs) have rapid antidepressant-like properties in rodents and exert few adverse effects, but molecular targets underlying their behavioral and synaptic effects remain undetermined. (illinois.edu)

One of the two major classes of cholinergic receptors. (lookformedical.com)
GABARs belong to the superfamily of ligand-gated ion channels that includes the glycine, nicotinic cholinergic (nAChR), and 5-hydroxytryptamine receptors. (aspetjournals.org)

The dopamine D2-like receptor antagonist, haloperidol (0.03, 0.1 or 0.3 mg kg(-1), s.c.) given at the same time as Ro 04-6790 (30 mg kg(-1), i.p.) had no effect on the stretching induced by the 5-HT6 antagonist. (lookformedical.com)
There is no evidence for dopamine D2-like receptor involvement in this behaviour. (lookformedical.com)
The effects of morphine on memory consolidation in mice involve both D1 and D2 dopamine receptors. (uniroma1.it)

TRPV1 and CB 1 receptors share the endogenous agonist anandamide (AEA), produced from N-arachidonoylphosphatidylethanolamine (20:4-NAPE). (frontiersin.org)
Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. (nature.com)
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)

The recombinant receptor has a diazepam-insensitive pharmacology, with negligible affinity for a number of classic benzodiazepines. (drugbank.com)

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)

In this context metabotropic ACh receptors, termed muscarinic ACh receptors (mAChRs) [ 7 ] play a crucial role. (biomedcentral.com)

Though borneol did not show any effect on the glycine-induced inward currents, borneol enhanced GABA-mediated responses. (kjpp.net)
Spontaneous and GABAR single-channel currents from α1β3ε receptors had single-channel conductances of ∼24 pS. (aspetjournals.org)

The activity of most of these modulators depends upon the subunit composition of the receptor. (aspetjournals.org)
Although several other modulators have specific effects at α6-containing receptors, amiloride is the first inhibitor to be reported with no additional dependence on the identity of the β or γ subunit. (aspetjournals.org)
GABA Modulators" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (wakehealth.edu)
This graph shows the total number of publications written about "GABA Modulators" by people in this website by year, and whether "GABA Modulators" was a major or minor topic of these publications. (wakehealth.edu)
Below are the most recent publications written about "GABA Modulators" by people in Profiles. (wakehealth.edu)
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 competitively inhibits the activity of benzodiazepine and non-benzodiazepine substances that interact with benzodiazepine receptors site on the GABA/benzodiazepine receptor complex. (nih.gov)

These studies showed that GABA receptors activation induced water and NaCl intake, responses that was reduced by previous injections of angiotensin antagonist losartan(the AT1 receptor antagonist). (fapesp.br)
Thus, activation of androgen receptors is important for the presence of proconvulsant SNR muscimol responses. (elsevierpure.com)
Yuan-Ping Pang and Paul R. Carlier has developed three series of homo/hetero dimeric acetylcholinesterase inhibitors derived from tacrine and/or huperzine A. The representative dimers bis(3)-Cognitin (B3C), bis(12)-hupyridone, and tacrine(10)-hupyridone might possess disease-modifying effects through the modulation of N-methyl-d-aspartic acid receptors, the activation of myocyte enhancer factor 2D gene transcription, and the promotion of neurotrophic factor secretion. (inrae.fr)
At nanomolar concentrations, A10E could inhibit Abeta oligomers-induced neurotoxicity via the activation of tyrosine kinase receptor B (TrkB)/Akt pathway in SH-SY5Y cells. (inrae.fr)
The switch between TRPV1 and CB 1 receptor activation by the AEA precursor 20:4-NAPE during inflammation may play an important role in nociceptive processing, hence the development of pathological pain. (frontiersin.org)
Accordingly, CB 1 receptor activation has been reported to suppress nociceptive behavior both in pathological pain states and in healthy organisms ( Pertwee, 2009 ). (frontiersin.org)
Activation of these receptors enhances the effects of GABA. (medscape.com)
Conclusions: GABA A receptor-mediated excitation, due in part to differential expression of NKCC1 and KCC2 and subsequent activation of L-type calcium channels, may contribute to seizure genesis in HH tissue. (arizona.edu)
However, the cellular effects induced by muscarinic acetylcholine receptors (mAChRs) activation are poorly understood in the neocortex. (biomedcentral.com)
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)

In GABA-sensitive BCs, muscimol responses were typically weak or absent. (nih.gov)

The gp120-induced mucus formation was clogged from the inhibitors of CXCR4 α7-nicotinic acetylcholine receptor (α7-nAChR) and γ-aminobutyric acid (GABA)AR but not the antagonists of CCR5 and epithelial growth element receptor (EGFR). (biongenex.com)
We and others have shown that airway mucus formation is definitely strongly affected by gamma aminobutyric acid (GABA)AR [14-16] and nicotinic acetylcholine receptors (nAChRs) (17) in the airway epithelial cells and reciprocally nAChR antagonists suppress allergen and cigarette Etomoxir smoke (CS)/nicotine-induced airway mucus formation both and [16]. (biongenex.com)

A number of compounds that bind to the benzodiazepine site potentiated the GABA response of alpha 6 beta 2 gamma 2 receptors. (drugbank.com)
We hypothesized that GABA-NAMs act at the benzodiazepine site of GABA A receptors containing α5 subunits to increase gamma oscillatory activity, strengthen synapses in reward circuits, and reverse anhedonia. (illinois.edu)
These actions were prevented by pretreatment with the benzodiazepine site antagonist flumazenil. (illinois.edu)

We measured its effects on recombinant GABARs to determine its mechanism of action at mammalian receptors and to examine the effect of subunit composition. (aspetjournals.org)
We examined the effect of amiloride on the activity of recombinant GABARs expressed transiently in L929 fibroblasts to determine its mechanism of action on mammalian GABARs and to determine whether the subunit composition of the receptor influenced its sensitivity to amiloride. (aspetjournals.org)

Bicuculline-resistant GABA responses occurred in approximately 80% of GABA-responsive RCs and BCs. (nih.gov)
Both bicuculline-sensitive (GABA(A)-like) and bicuculline-insensitive (GABAc-like) responses were resistant to picrotoxin. (nih.gov)
Although a small minority of GABA-sensitive cells hyperpolarized in response to R(+)baclofen, bicuculline-insensitive responses were not antagonized by 2-hydroxysaclofen, and were abolished in low [Cl-]o. (nih.gov)
Bicuculline methiodide, a GABA(A)-receptor antagonist, completely arrested GABA influences on the electromotility response. (northwestern.edu)
These responses were blocked by bicuculline methiodide (50 μM). (arizona.edu)

Zinc and copper modulate differentially the P2X receptor. (cdc.gov)

Consistent with this, in vivo recording showed that nociceptive-evoked responses of ON- and OFF-cells were suppressed by optogenetic inactivation of archaerhodopsin (ArchT)-expressing PB terminals in RVM, demonstrating that a net inhibitory input to OFF-cells and net excitatory input to ON-cells are engaged by acute noxious stimulation. (eneuro.org)

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)
and (3) that oxonol was a sensitive probe for retinal GABA responses. (nih.gov)
Retinal ganglion cells vary significantly in terms of their size, connections, and responses to visual stimulation but they all share the defining property of having a long axon that extends into the brain. (eyewire.org)

In contrast, GABA C receptors containing onlyρ subunits (ρ1-ρ3) have been predominantly detected in the retina. (jneurosci.org)
We therefore tested the hypothesis that GABA A and GABA C subunits formed a heteromeric receptor. (jneurosci.org)
One explanation could be that ρ subunits assemble with subunits from other receptor subfamilies, but this hypothesis is contentious. (jneurosci.org)
Receptors containing an α6 subunit were about 10-fold more sensitive to amiloride than those containing other α subunits. (aspetjournals.org)
In contrast, GABA(C) receptors containing only rho subunits (rho1-rho3) have been predominantly detected in the retina. (ox.ac.uk)
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)

Therefore, it probably represents a unique modulatory site on the GABAR, which could be useful for developing drugs targeting these receptors. (aspetjournals.org)
The γ-aminobutyric acid A (GABA A ) receptor (GABAR) is a target for many clinically and experimentally important drugs. (aspetjournals.org)
Most GABAR isoforms require binding of GABA to initiate entry into open states. (aspetjournals.org)

Flumazenil is a benzodiazepine antagonist. (nih.gov)

Alterations of GABA signaling that impair gamma oscillations and, as a result, cognitive function suggest paths for novel therapeutic interventions. (hindawi.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)

GABA-sensitive cells were also TACA-sensitive (trans-4-Aminocrotonic acid), and these ligands appeared interchangeable in ability to evoke responses. (nih.gov)
γ-Aminobutyric acid A (GABA A ) receptors (GABARs) are responsible for most fast inhibitory neurotransmission in the mammalian brain. (aspetjournals.org)
Action of 3-((+/-)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPP): a new and highly potent antagonist of N-methyl-D-aspartate receptors in the hippocampus. (hellobio.com)

Estrone is only a weak agonist of estrogen receptor but it serves as a precursor for biosynthesis of 17β-estradiol, 16α-hydroxyestrone and catechol estrogens. (helsinki.fi)
While 16α-hydroxyestrone has relatively weak affinity for estrogen receptor, it has prolonged effect due to covalent binding to the receptor. (helsinki.fi)

With this communication we present evidence that HIV gp120 induces mucus formation in NHBE cells through the HIV co-receptor CXCR4 using the α7-nAChR-GABAARα2 pathway but not the epithelial growth element receptor (EGFR) pathway. (biongenex.com)

TTFB displays negligible activity at representatives of the GABA A , glycine, 5-HT 3 and nicotinic ACh receptors, and thus it constitutes a potential pharmacological tool for ZAC. (guidetopharmacology.org)

Depression of central neuron responses, affinity for [3H]D-AP5 binding sites on brain membranes and anticonvulsant activity. (hellobio.com)
These results encourage human studies using GABA-NAMs to treat depression by providing readily translatable measures of target engagement. (illinois.edu)

Downregulation of the 5HT1A serotonin receptor in sleep-promoting cells mediates the effect of sleep need on seizures, and we identify an FDA-approved 5HT1A agonist to mitigate seizures. (bvsalud.org)

These receptor molecules are concentrated at sites of synapses with amacrine and bipolar cells. (eyewire.org)
Magnitude response decreased about 30% for long cells and 14% for short ones. (northwestern.edu)
We discovered that NHBE cells indicated the HIV-coreceptor CXCR4 but not CCR5 and produced mucus in response to CXCR4-tropic gp120. (biongenex.com)

Transient receptor potential ion channel, vanilloid subfamily, type 1 (TRPV1) cation channel, and cannabinoid receptor 1 (CB 1 ) are essential in the modulation of nociceptive signaling in the spinal cord dorsal horn that underlies different pathological pain states. (frontiersin.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)

It can also reverse the binding of benzodiazepines to benzodiazepine receptors. (nih.gov)

Anatomy8

Organisms6

Diseases2

Chemicals and Drugs211

Analytical, Diagnostic and Therapeutic Techniques and Equipment10

Psychiatry and Psychology2

Phenomena and Processes15

Disciplines and Occupations1

Health Care1

Neurons12

Agonists6

NMDA10

Inhibition9

MUSCARINIC RECEPTORS2

Rats8

GABAA2

Selective4

Glycine receptor1

Characterization3

Agonist muscimol1

Androgen receptor2

Ionotropic receptors1

Neuronal3

Nicotinic receptor1

Subtypes3

Blockade2

Gabazine1

Synaptic5

Cholinergic2

Dopamine3

Endogenous3

Pharmacology1

Postsynaptic1

Metabotropic1

Currents2

Modulators6

Inhibits1

Activation10

Muscimol responses1

Acetylcholine2

Benzodiazepine site3

Subunit composition2

Bicuculline5

Differentially1

Excitatory1

Retinal3

Subunits6

GABAR3

Flumazenil1

Gamma2

Acid3

Estrogen receptor2

Pathway1

Pharmacological1

Depression2

Serotonin1

Cells3

Cation1

Modulate1

Benzodiazepines1