This effect was blocked by coinjection of 1 μg (hr)IL-1β receptor antagonist or 0.1 ng of 3-((+)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate, selective antagonists of IL-1β and NMDA receptors, respectively. (jneurosci.org)
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)
Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies. (bvsalud.org)
γ-Aminobutyric acid A (GABA A ) receptors (GABARs) are responsible for most fast inhibitory neurotransmission in the mammalian brain. (aspetjournals.org)
Animal studies support that L-theanine rapidly crosses the blood brain barrier, increases brain levels of serotonin, GABA and dopamine, binds to glutamate and NMDA receptors, and may increase levels of brain-derived neurotrophic factor (BDNF). (iherb.com)
Trazodone - found in Sleep-T Synergy and Sleep-T Synergy Forte this antidepressant medication increases serotonin in the brain by preventing its reuptake and subsequent breakdown in brain cells and acts as an antagonist at 5-HT-2A/2C serotonin receptors. (victoryselect.com)
Neuroactive glutamate is classified as an excitatory amino acid (EAA) because glutamate binding onto postsynaptic receptors typically stimulates, or depolarizes, the postsynaptic cells. (org.es)
2006 ). The majority of CB1 receptors is localized on striatal glutamatergic and gamma-aminobutyric acid (GABA)-ergic interneurons and projection neurons. (springer.com)
Inhibitors1
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)
Receptor antagonist6
Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo . (mcw.edu)
The facilitatory effect of GRP on sIPSCs was blocked by the GRP receptor antagonist, RC3095. (biomedcentral.com)
Spontaneous EPSCs were recorded in the presence of GABA A receptor antagonist, picrotoxin (100 μM) and spontaneous IPSCs were recorded in the presence of a NMDA receptor antagonist, AP5 (100 μM) and a non-NMDA receptor antagonist, CNQX (20 μM). (biomedcentral.com)
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)
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)
Agonists3
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)
In in vitro fertilization (IVF) cycles controlled ovarian hyperstimulation (COH) is established by gonadotropins in combination with gonadotropin-releasing hormone (GnRH) agonists or antagonists, to prevent premature luteinizing hormone (LH) surge. (elsevierpure.com)
We applied Affymetrix gene expression profiling in CC of oocytes at different maturation stages using either GnRH agonists or GnRH antagonists. (elsevierpure.com)
These neurons are believed to release GABA, not glutamate, as their neurotransmitter (Yazulla, 1986), suggesting the weak glutamate labeling reflects the pool of metabolic glutamate used in the synthesis of GABA. (org.es)
This has been supported by the results from double-labeling studies using antibodies to both GABA and glutamate: glutamate-positive amacrine cells also label with the GABA antibodies (Jojich and Pourcho, 1996, Yang, 1996). (org.es)
Gamma hydroxybutyrate (GHB) is similar to the neurotransmitter gamma-aminobutyric acid (GABA), but it can cross the blood-brain barrier and can be taken by mouth. (msdmanuals.com)
Dopamine1
Among other differentially expressed genes we observed a marked number of new genes connected to cell adhesion and neurotransmitters such as dopamine, glycine and γ-Aminobutyric acid (GABA). (elsevierpure.com)
Neurons1
Nonlethal concentrations of EO increased agonist binding and decreased antagonist binding in cortical neurons. (hindawi.com)
Endogenous3
Low concentrations significantly inhibited GABA uptake, especially in astrocytes, suggesting an accumulation of endogenous GABA in the synaptic cleft. (hindawi.com)
Kynurenic acid (KYNA) is an endogenous tryptophan (Trp) metabolite known to possess neuroprotective property. (mdpi.com)
3 The existence of the d -receptor was subsequently proposed to explain the profile of activity in vitro of the enkephalins (the first endogenous opioid peptides), and on the basis of the relative potency of the non-selective opioid antagonist naloxone to reverse endogenous opioid peptide inhibition of the nerve-evoked contractions of the mouse vas deferens. (opioids.wiki)
Serotonin1
At low doses, trazodone appears to act as a serotonin antagonist and at higher doses as an agonist. (victoryselect.com)
Amino2
Some neuroactive compounds are amino acids, which also have metabolic functions in the presynaptic cell. (org.es)
Two splice variants of the MOR-1 gene have been cloned, differing only in the presence or absence of 8 amino acids in the C-terminal tail. (opioids.wiki)
Modulators1
Development of Inhaled GABA A Receptor Modulators to Improve Airway Function in Bronchoconstrictive Disorders. (mcw.edu)
MicroM1
GABA(A)-mediated postsynaptic currents were subject to paired-pulse depression that was inhibited by the GABA(B) antagonist CGP 55845A (5 microM). (nih.gov)
Systemic injection1
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)
Chloride2
Lotilaner is an antagonist of γ-aminobutyric acid (GABA)-gated chloride channels [ 13 ]. (biomedcentral.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)
Obeticholic acid1
INT-747, so called obeticholic acid (OCA) or 6-alpha-ethyl chenodeoxycholic acid (6-ECDCA), is a 6-alpha-alkyl-substituted analog of CDCA selectively inducing FXR transactivation at 1 μM 15 . (nature.com)
Modulation1
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)
Selective2
Metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3-selective GABAkine KRM-II-81. (mcw.edu)
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)
Compounds1
These compounds require metabolic activation to their oxon analogs (compounds in which the =S is replaced by =O) for anticholinesterase activity. (cdc.gov)
Anesthetics1
Ketamine and Phencyclidine (PCP) Ketamine and phencyclidine are N-methyl-D-aspartate receptor antagonists and dissociative anesthetics that can cause intoxication, sometimes with confusion or a catatonic state. (msdmanuals.com)
Currents1
When recording GABA A receptor-mediated currents, K-gluconate was replaced by Cs-MeSO 3 and a holding potential of 10 mV. (biomedcentral.com)
Synthetic1
1. Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin. (nih.gov)
Hippocampus1
Using immunocytochemistry and ELISA, we investigated the production of interleukin (IL)-1β in the rat hippocampus after focal application of kainic acid inducing electroencephalographic (EEG) seizures and CA3 neuronal cell loss. (jneurosci.org)
Anticonvulsant3
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)
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)
Comparative anticonvulsant activity of the GABAkine KRM-II-81 and a deuterated analog. (mcw.edu)
Inhibitor1
Development and validation of an LC-MS/MS method for the determination of ARN14988, an acid ceramidase inhibitor, and its application to a pharmacokinetic study in a mouse model. (mcw.edu)
Competitive3
The present study shows the capsazepine acts as a competitive antagonist of capsaicin. (nih.gov)
This could mean that penicillin is a competitive GABA specific antagonist, which would further explain its epileptogenic properties. (epiphanyasd.com)
Amiloride acted primarily as a competitive antagonist, reducing the sensitivity of the receptor to GABA without affecting the maximal current amplitude. (aspetjournals.org)
Effects3
GHB and its analogs have been used for their sedative and amnesic effects to facilitate sexual assaults. (msdmanuals.com)
In this review they concluded the effects relate to GABA and here we are talking about negative effects. (epiphanyasd.com)
Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system. (lookformedical.com)
Neuronal1
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)
Drugs2
The γ-aminobutyric acid A (GABA A ) receptor (GABAR) is a target for many clinically and experimentally important drugs. (aspetjournals.org)