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Gabaa antagonist

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https://www.readbyqxmd.com/read/29432796/opioid-and-%C3%AE-2-adrenergic-mechanisms-are-activated-by-gaba-agonists-in-the-lateral-parabrachial-nucleus-to-induce-sodium-intake
#1
Lisandra B De Oliveira, Carina A F Andrade, Laurival A De Luca, Débora S A Colombari, José V Menani
The activation of GABA, opioid or α 2 adrenergic mechanisms in the lateral parabrachial nucleus (LPBN) facilitates hypertonic NaCl intake in rats. In the present study, we combined opioid or α 2 adrenergic antagonists with GABA agonists into the LPBN in order to investigate if NaCl intake caused by GABAergic activation in normohydrated rats depends on opioid or α 2 -adrenergic mechanisms in this area. Male Holtzman rats with stainless steel cannulas implanted bilaterally in the LPBN were used. Bilateral injections of muscimol or baclofen (GABA A and GABA B agonists, respectively, 0...
February 9, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29432603/in-vitro-screening-for-seizure-liability-using-microelectrode-array-technology
#2
Jenifer A Bradley, Harry H Luithardt, Monica R Metea, Christopher J Strock
Drug induced seizure liabilities produce significant compound attrition during drug discovery. Currently available in vitro cytotoxicity assays cannot predict all toxicity mechanisms due to the failure of these assays to predict sublethal target specific electrophysiological liabilities. Identification of seizurogenic and other electrophysiological effects at early stages of the drug development process is important to ensure that safe candidate compounds can be developed while chemical design is taking place, long before these liabilities are discovered in costly preclinical in vivo studies...
February 8, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29410359/modulation-of-the-zebrafish-optokinetic-reflex-by-pharmacologic-agents-targeting-gabaa-receptors
#3
Enhua Shao, Seth D Scheetz, Wenting Xie, Edward A Burton
Optokinetic reflex (OKR) responses provide a convenient means to evaluate visual, integrative and oculomotor function in larval zebrafish. We measured multiple aspects of the OKR response in zebrafish exposed systemically to compounds altering signaling at GABAA receptors in order to derive quantitative concentration-response relationships. The GABAA antagonist picrotoxin caused concentration-dependent decreases in reflex gain, saccade velocity, saccade amplitude, interocular concordance and interocular gain...
February 2, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29408089/anti-allodynic-effects-of-n-demethylsinomenine-an-active-metabolite-of-sinomenine-in-a-mouse-model-of-postoperative-pain
#4
Yuntao Ou, Man Su, Yong Ling, Qianqian Wei, Fei Pan, Jiejia Li, Jun-Xu Li, Qing Zhu
Sinomenine, a major bioactive ingredient isolated from traditional Chinese medicine Sinomenium acutum, has been reported to have analgesic effects in various pain animal models. N-demethylsinomenine, the N-demethylated product of sinomenine, has been identified to be the major metabolite of sinomenine and is also a natural component extracted from Sinomenium acutum. This study examined the anti-allodynic effects of N-demethylsinomenine in a mouse model of postoperative pain. A significant and sustained mechanical allodynia that lasted for 4 days was induced by making a surgical incision on the right hind paw in mice...
February 3, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29407219/gabaa-receptor-positive-and-negative-allosteric-modulators
#5
REVIEW
Richard W Olsen
gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the gene products involved were discovered during the mid-twentieth century. Historically, myriad existing nervous system drugs act as positive and negative allosteric modulators of these proteins, making GABA a major component of modern neuropharmacology, and suggesting that many potential drugs will be found that share these targets. Although some of these drugs act on proteins involved in synthesis, degradation, and membrane transport of GABA, the GABA receptors Type A (GABAAR) and Type B (GABABR) are the targets of the great majority of GABAergic drugs...
January 30, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29388357/airway-obstruction-produces-widespread-sympathoexcitation-role-of-hypoxia-carotid-chemoreceptors-and-nts-neurotransmission
#6
Caroline B Ferreira, Sergio L Cravo, Sean D Stocker
Obstructive sleep apnea (OSA) is the most common respiratory disturbance of sleep and is closely associated to cardiovascular diseases. In humans, apnea increases respiratory effort and elevates muscle sympathetic nerve activity (SNA), but the primary stimulus for the SNA activation has not been identified. We recently developed a model of apnea in rodents using acute airway obstruction. In this study, we employed this model to test whether the elevation in SNA was mediated by hypoxia, carotid chemoreceptors, or neurotransmission in the nucleus tractus solitarius (NTS)...
February 2018: Physiological Reports
https://www.readbyqxmd.com/read/29374303/negative-allosteric-modulation-of-alpha-5-containing-gabaa-receptors-engenders-antidepressant-like-effects-and-selectively-prevents-age-associated-hyperactivity-in-tau-depositing-mice
#7
Nina Z Xu, Margot Ernst, Marco Treven, Rok Cerne, Mark Wakulchik, Xia Li, Timothy M Jones, Scott D Gleason, Denise Morrow, Jeffrey M Schkeryantz, Md Toufiqur Rahman, Guanguan Li, Michael M Poe, James M Cook, Jeffrey M Witkin
RATIONALE: Associated with frank neuropathology, patients with Alzheimer's disease suffer from a host of neuropsychiatric symptoms that include depression, apathy, agitation, and aggression. Negative allosteric modulators (NAMs) of α5-containing GABAA receptors have been suggested to be a novel target for antidepressant action. We hypothesized that pharmacological modulation of this target would engender increased motivation in stressful environments. METHODS: We utilized electrophysiological recordings from Xenopus oocytes and behavioral measures in mice to address this hypothesis...
January 26, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29370841/expression-of-functional-inhibitory-neurotransmitter-transporters-glyt1-gat-1-and-gat-3-by-astrocytes-of-inferior-colliculus-and-hippocampus
#8
Elsa Ghirardini, Simon L Wadle, Vanessa Augustin, Jasmin Becker, Sina Brill, Julia Hammerich, Gerald Seifert, Jonathan Stephan
Neuronal inhibition is mediated by glycine and/or GABA. Inferior colliculus (IC) neurons receive glycinergic and GABAergic inputs, whereas inhibition in hippocampus (HC) predominantly relies on GABA. Astrocytes heterogeneously express neurotransmitter transporters and are expected to adapt to the local requirements regarding neurotransmitter homeostasis. Here we analyzed the expression of inhibitory neurotransmitter transporters in IC and HC astrocytes using whole-cell patch-clamp and single-cell reverse transcription-PCR...
January 25, 2018: Molecular Brain
https://www.readbyqxmd.com/read/29369902/contribution-of-the-%C3%AE-5-gabaa-receptor-to-the-discriminative-stimulus-effects-of-propofol-in-rat
#9
Benfu Wang, Kun Lv, Huifeng Liu, Yin Su, Hong Wang, Sicong Wang, Suhao Bao, Wen-Hua Zhou, Qing-Quan Lian
Propofol as an agonist of GABAA receptor has a rewarding and discriminative stimulus effect. However, which subtype of the GABAA receptor is involved in the discriminative stimulus effects of propofol is still not clear. We observed the effects of an agonist or an antagonist of the subtype-selective GABAA receptor on discriminative stimulus effects of propofol. Male Sprague-Dawley rats were trained to discriminate 10 mg/kg (intraperitoneal) propofol from intralipid under a fixed-ratio 10 schedule of food reinforcement...
January 24, 2018: Neuroreport
https://www.readbyqxmd.com/read/29368126/pharmacotherapy-for-refractory-and-super-refractory-status-epilepticus-in-adults
#10
Martin Holtkamp
Patients with prolonged seizures that do not respond to intravenous benzodiazepines and a second-line anticonvulsant suffer from refractory status epilepticus and those with seizures that do not respond to continuous intravenous anesthetic anticonvulsants suffer from super-refractory status epilepticus. Both conditions are associated with significant morbidity and mortality. A strict pharmacological treatment regimen is urgently required, but the level of evidence for the available drugs is very low. Refractory complex focal status epilepticus generally does not require anesthetics, but all intravenous non-anesthetizing anticonvulsants may be used...
January 24, 2018: Drugs
https://www.readbyqxmd.com/read/29325900/orexin-b-modulates-synaptic-transmission-of-rod-bipolar-cells-in-rat-retina
#11
Gong Zhang, Xiao-Hua Wu, Guo-Zhong Xu, Shi-Jun Weng, Xiong-Li Yang, Yong-Mei Zhong
Orexin-A, -B play a crucial role in arousal and feeding by activating two G-protein-coupled receptors: orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R). Orexins, along with orexin receptors, are expressed in retinal neurons, and they have been shown to differentially modulate excitatory AMPA receptors of amacrine and ganglion cells in the inner retina. In this work we report that orexin-B modulates the activity of rod bipolar cells (RBCs) located in the outer retina of rat. Intravitreal injection of orexin-B increased the amplitude of the scotopic electroretinographic b-wave, a reflection of RBC activity, recorded in vivo...
January 8, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29316656/azemiopsin-a-selective-peptide-antagonist-of-muscle-nicotinic-acetylcholine-receptor-preclinical-evaluation-as-a-local-muscle-relaxant
#12
Irina V Shelukhina, Maxim N Zhmak, Alexander V Lobanov, Igor A Ivanov, Alexandra I Garifulina, Irina N Kravchenko, Ekaterina A Rasskazova, Margarita A Salmova, Elena A Tukhovskaya, Vladimir A Rykov, Gulsara A Slashcheva, Natalya S Egorova, Inessa S Muzyka, Victor I Tsetlin, Yuri N Utkin
Azemiopsin (Az), a linear peptide from the Azemiops feae viper venom, contains no disulfide bonds, is a high-affinity and selective inhibitor of nicotinic acetylcholine receptor (nAChR) of muscle type and may be considered as potentially applicable nondepolarizing muscle relaxant. In this study, we investigated its preclinical profile in regard to in vitro and in vivo efficacy, acute and chronic toxicity, pharmacokinetics, allergenic capacity, immunotoxicity and mutagenic potency. The peptide effectively inhibited (IC50 ~ 19 nM) calcium response of muscle nAChR evoked by 30 μM (EC100) acetylcholine but was less potent (IC50 ~ 3 μM) at α7 nAChR activated by 10 μM (EC50) acetylcholine and had a low affinity to α4β2 and α3-containing nAChR, as well as to GABAA or 5HT₃ receptors...
January 7, 2018: Toxins
https://www.readbyqxmd.com/read/29309796/prenatal-exposure-to-valproic-acid-alters-the-development-of-excitability-in-the-postnatal-rat-hippocampus
#13
Yukiko Fueta, Yuko Sekino, Sachiko Yoshida, Yasunari Kanda, Susumu Ueno
Prenatal valproic acid (VPA) exposure is a well-known animal model of autism spectrum disorder (ASD) that produces alterations in embryonic and adult neurogenesis as well as adolescent/adulthood neurobehavioral phenotypes. However, the effects of prenatal VPA exposure on neural network excitability, especially during the synaptogenic period around eye opening, are not fully understood. In this study, we orally administered VPA (300 mg/kg) to pregnant Wistar rats on gestation day 15 and subsequently performed field potential recording in the CA1 area of hippocampal slices obtained from control (saline-exposed) and VPA-exposed rat pups between postnatal day (PND) 13 and PND18...
January 5, 2018: Neurotoxicology
https://www.readbyqxmd.com/read/29289597/hippocampal-gabaa-antagonism-reverses-the-novel-object-recognition-deficit-in-sub-chronic-phencyclidine-treated-rats
#14
Nichole M Neugebauer, Masanori Miyauchi, Tatsuya Sato, Jun Tadano, Hanife Akal, Hossein Ardehali, Herbert Y Meltzer
BACKGROUND: Abnormalities in prefrontal cortical and hippocampal GABAergic function are postulated to be major causes of the cognitive impairment associated with schizophrenia (CIAS). There are conflicting views on whether diminished or enhanced GABAergic activity contributes to the deficit in short-term novel object recognition (NOR) in the sub-chronic phencyclidine (scPCP) rodent model of CIAS. This study assessed the role of GABAA signaling in the medial prefrontal cortex (mPFC) and ventral hippocampus (vHPC) in NOR in saline (scSAL)- and scPCP-treated rats...
December 28, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29283314/delayed-inhibition-of-tonic-inhibition-enhances-functional-recovery-following-experimental-ischemic-stroke
#15
James E Orfila, Himmat Grewal, Robert M Dietz, Frank Strnad, Takeru Shimizu, Myriam Moreno, Christian Schroeder, Joan Yonchek, Krista M Rodgers, Andra Dingman, Timothy J Bernard, Nidia Quillinan, Wendy B Macklin, Richard J Traystman, Paco S Herson
The current study focuses on the ability to improve cognitive function after stroke with interventions administered at delayed/chronic time points. In light of recent studies demonstrating delayed GABA antagonists improve motor function, we utilized electrophysiology, biochemistry and neurobehavioral methods to investigate the role of α5 GABAA receptors on hippocampal plasticity and functional recovery following ischemic stroke. Male C57Bl/6 mice were exposed to 45 min transient middle cerebral artery occlusion and analysis of synaptic and functional deficits performed 7 or 30 days after recovery...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/29259544/dichotomous-effects-of-mu-opioid-receptor-activation-on-striatal-low-threshold-spike-interneurons
#16
Rasha Elghaba, Enrico Bracci
Striatal low-threshold spike interneurons (LTSIs) are tonically active neurons that express GABA and nitric oxide synthase and are involved in information processing as well as neurovascular coupling. While mu opioid receptors (MORs) and their ligand encephalin are prominent in the striatum, their action on LTSIs has not been investigated. We addressed this issue carrying out whole-cell recordings in transgenic mice in which the NPY-expressing neurons are marked with green fluorescent protein (GFP). The MOR agonist (D-Ala(2), N-MePhe(4), Gly-ol)-enkephalin (DAMGO) produced dual effects on subpopulations of LTSIs...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29259493/gamma-aminobutyric-acida-receptor-agonist-muscimol-increases-kiss-1-gene-expression-in-hypothalamic-cell-models
#17
Haruhiko Kanasaki, Tuvshintugs Tumurbaatar, Aki Oride, Tomomi Hara, Hiroe Okada, Satoru Kyo
Purpose: Accumulating evidence indicates that hypothalamic kisspeptin plays a pivotal role in the regulation of the hypothalamic-pituitary-gonadal (HPG) axis. In this study, the direct action of the gamma-aminobutyric acid (GABA)A receptor agonist on kisspeptin-expressing neuronal cells was examined. Methods: A hypothalamic cell model of rat hypothalamic cell line R8 (rHypoE8) cells and primary cultures of neuronal cells from fetal rat brains were stimulated with a potent and selective GABAA receptor agonist, muscimol, to determine the expression of the KiSS-1 gene...
October 2017: Reproductive Medicine and Biology
https://www.readbyqxmd.com/read/29232839/agarwood-essential-oil-displays-sedative-hypnotic-effects-through-the-gabaergic-system
#18
Shuai Wang, Canhong Wang, Deqian Peng, Xinmin Liu, Chongming Wu, Peng Guo, Jianhe Wei
Although agarwood has been used as a tranquilizer in Asian countries for hundreds of years, the underlying pharmacological basis is still unclear. This study investigated the sedative-hypnotic effect of agarwood essential oil (AEO) using locomotor activity and pentobarbital-induced sleeping assays in mice. Single (1-day) and multiple (7- and 14-days) administrations of 60 mg/kg AEO generated significant sedative effect on inhibiting locomotor activity and hypnotic effect on pentobarbital-induced sleeping in mice...
December 9, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29225040/differential-neuromodulatory-role-of-endocannabinoids-in-the-rodent-trigeminal-sensory-ganglion-and-cerebral-cortex-relevant-to-pain-processing
#19
Francesca Eroli, Inge C M Loonen, Arn M J M van den Maagdenberg, Else A Tolner, Andrea Nistri
Endocannabinoids are suggested to control pain, even though their clinical use is not fully validated and the underlying mechanisms are incompletely understood. To clarify the targets of endocannabinoid actions, we studied how activation of the endocannabinoid CB1 receptor (CB1R) affects neuronal responses in two in vitro preparations of rodents, namely the trigeminal sensory ganglion (TG) in culture and a coronal slice of the cerebral cortex. On TG small-medium size neurons, we tested whether submicromolar concentrations of the endogenous CB1R agonist anandamide (AEA) modulated inhibitory GABAA receptors and excitatory ATP-gated P2X3 receptors...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29225001/dorsal-hippocampal-cannabinergic-and-gabaergic-systems-modulate-memory-consolidation-in-passive-avoidance-task
#20
Mohammad Nasehi, Parisa Gerami, Fatemeh Khakpai, Mohammad-Reza Zarrindast
In the present research, we examined the possible interaction between the hippocampal CB2 and GABAA receptors on modulation of memory consolidation. In this research, step-down passive avoidance task was used to evaluate memory consolidation in adult male NMRI mice. The results showed that post-training intra-CA1 administration of muscimol (0.05 and 0.1μg/mouse) impaired memory consolidation as evidenced by a decrease in step-down latency on the test day, which was suggestive of drug-produced amnesia. However co-administration of different doses of muscimol (0...
December 7, 2017: Brain Research Bulletin
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