GABA A receptor agon 
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  • ||||||||||  dizocilpine (MK801) / Merck (MSD)
    Review, Journal:  Vestibular compensation: Neural mechanisms and clinical implications for the treatment of vertigo. (Pubmed Central) -  Apr 1, 2024   
    The declining frequency of spontaneous nystagmus after UL is an index of the initial process, and short-term administration of diazepam, a GABAA receptor agonist, has been shown to accelerate the initial process in rats...The declining number of MK801-induced Fos-positive neurons in contra-MVe after UL is an index of the late process, and long-term administration of betahistine, a histamine H3 receptor antagonist, has been shown to accelerate the late process in rats...To facilitate dynamic vestibular compensation, early ambulation and subsequent vestibular rehabilitation exercise are recommended for the treatment of chronic vertigo in patients with uncompensated unilateral vestibular dysfunction. Although vestibular compensation after bilateral vestibular loss is not expected, vestibular rehabilitation with a sensory-substitution strategy can improve imbalance in patients with bilateral vestibular lesions.
  • ||||||||||  ByFavo (remimazolam) / PAION, Cosmo Pharma, Mundipharma, Pharmascience, Eagle Pharma
    Journal:  Remimazolam Improves the Markers of Post-Resuscitation Cerebral Injury in a Swine Model of Cardiac Arrest. (Pubmed Central) -  Mar 22, 2024   
    Although vestibular compensation after bilateral vestibular loss is not expected, vestibular rehabilitation with a sensory-substitution strategy can improve imbalance in patients with bilateral vestibular lesions. In a swine model of cardiac arrest and resuscitation, the remimazolam administered after resuscitation significantly improved the markers of post-resuscitation cerebral injury and therefore protected the brain against global ischemic stimulation.
  • ||||||||||  gaboxadol (OV101) / Ovid Therapeutics, Angelini Group, Healx
    Preclinical, Journal:  Enhancing GABAergic tonic inhibition reduces seizure-like activity in the neonatal mouse hippocampus and neocortex. (Pubmed Central) -  Feb 16, 2024   
    There has been no significant improvement in treating neonatal seizures for nearly 50 years, especially for patients in whom pharmacoresistance develops. Our results show that enhancing tonic inhibition in neonatal mice, a developmental age when GABA mainly depolarizes, decreases neuronal firing and epileptiform activity in vitro Our results suggest that augmenting tonic inhibition could be an alternative treatment for neonatal seizures, especially in pharmacy-resistant ones.
  • ||||||||||  Journal:  Application of ensemble learning for predicting GABA receptor agonists. (Pubmed Central) -  Feb 8, 2024   
    Our results show that enhancing tonic inhibition in neonatal mice, a developmental age when GABA mainly depolarizes, decreases neuronal firing and epileptiform activity in vitro Our results suggest that augmenting tonic inhibition could be an alternative treatment for neonatal seizures, especially in pharmacy-resistant ones. Overall, our ensemble learning-based model (PubMac-GB) achieved comparable performance and would be helpful in effectively identifying agonists of GABAA receptors.
  • ||||||||||  ivabradine / Generic mfg.
    Preclinical, Journal:  The role of HCN channels on the effects of T-type calcium channels and GABA receptors in the absence epilepsy model of WAG/Rij rats. (Pubmed Central) -  Feb 8, 2024   
    In this study we used ivabradine (IVA), a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker, to identify its effect on spike-wave discharges (SWDs); and aimed to determine the role of IVA on the effects of T-type calcium channel blocker NNC 55-0396, GABAA receptor agonist muscimol and antagonist bicuculline in male WAG/Rij rats...Subacute administration of IVA reduced the antiepileptic activity of NNC, while the proepileptic activity of muscimol and the antiepileptic activity of bicuculline were abolished. It might be suggested that subacute IVA administration reduces absence seizures by changing the HCN channel expressions in WAG/Rij rats, and this affects the T-type calcium channels and GABA receptors.
  • ||||||||||  Gabaergic activation by extract of zizyphus seed prolongs sleep and enhances sleep quality in animal models. (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_13461;    
    After oral administration of Zizy extract for 7 days in rats, the expression of GABAA receptors ?1-, and ?2-subunits and GAD65/67 were regulated in the rat brain. These results suggest that Zizy extract increases sleep duration through GABA receptor activation and gives a chance to become a functional food for improving sleep disorders.
  • ||||||||||  Autoregulation of striatal dopamine release by co-released GABA dampens phasic-to-tonic dopamine signaling (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_11273;    
    Importantly, however, the differential effect of PTX on optically-evoked phasic-to-tonic DA signaling was lost in mice devoid of GAT1 in DA neurons and lack GABA co-release. Together, these data provide evidence for direct autoinhibition of axonal DA release by co-released GABA that is likely faster than G-protein coupled D2 autoreceptors, thereby introducing a novel autoregulatory mechanism by which co-released GABA acts as a first responder to dampen phasic-to-tonic DA signaling.
  • ||||||||||  Prelimbic cortex controls the speed, but not the accuracy, of simple visually guided decisions (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_4138;    
    Drift diffusion models showed evidence for increased thresholds and non-decision times under intra-PLC DAMGO. Together, these studies suggest that inactivating PLC reduces the amount of sensory evidence and sensorimotor preparation necessary to make a decision, while stimulating the cortical opioid system has the opposite effects.
  • ||||||||||  Towards clinical advancement of non-invasive circuit modulation via ultrasound-mediated molecular control. (WCC 147B) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_1494;    
    1) synthesis of components of our UC-carriers using microfluidics, enabling tuning of carrier size (Z-Average ~ 70-250 nm) and dosing (nanogram to microgram quantity). These results demonstrate a viable translational platform approach towards treating a variety of brain disorders through precise molecular control of circuit activity.
  • ||||||||||  bumetanide / Generic mfg.
    Sex differences in contribution of Na/K/Cl co-transporter and GABA receptors in chloride homeostasis of c-fiber primary afferents in the spinal cord dorsal horn. (Montreal Bonaventure Hotel (CAN meeting headquarters)) -  Jun 10, 2023 - Abstract #CANACN2023CAN_ACN_525;    
    The GABAAR agonist and antagonist muscimol and bicuculline, as well as the NKCC1 antagonist bumetanide, were used to modulate [Cl-]i in afferent terminals in the dorsal horn...We revealed that in slices of WT mice, paired-pulse ratio of local field potential is bigger in males, which bicuculline could abolish it. Presynaptic inhibition appears to be under distinct control by GABAergic inhibition and NKCC1 function between sexes, which should be taken into consideration in future studies.
  • ||||||||||  lamotrigine liquid oral suspension / OWP Pharma
    Journal:  Pharmacological evaluation of lateral habenula and rostromedial tegmental nucleus in the expression of ethanol-induced place preference. (Pubmed Central) -  May 16, 2023   
    We found that activation of LHb glutamatergic system by intra-LHb administration of l-trans-2,4-pyrrolidine dicarboxylate (PDC) (glutamate transporter inhibitor) significantly decreased CPP score; on the contrary, lamotrigine (inhibits glutamate release) significantly increased CPP score and showed a rewarding effect in CPP...Furthermore, while intra-RMTg administration of muscimol increased, the bicuculline treatment significantly decreased the TH-ir in VTA and NAc. Together, our behavioral and immunohistochemical results signify the role of LHb and RMTg in the expression of ethanol-conditioned reward behavior.
  • ||||||||||  Tecentriq (atezolizumab) / Roche
    Negative impact of the GABA pathway on aPD(L)1 immunotherapy (Section 40; Poster Board #25) -  Mar 14, 2023 - Abstract #AACR2023AACR_5876;    
    We found that several key genes of the GABA pathway are upregulated in non-responders to atezolizumab and we derived a 5-gene signature associated with poor outcomes in 2L urothelial cancer patients receiving atezolizumab...A similar negative impact was seen in patients receiving standard of care anti-PD(L)1 immunotherapy in 2L NSCLC using EHR derived deidentified Flatiron Health - Komodo Health claims linked data. These findings highlight the need for further evaluation of concomitant GABA modulators to understand potential risk associated with palliative care in the setting of cancer immunotherapy
  • ||||||||||  Journal:  Alteration of LHb function prevents the proper exploration of a novel environment. (Pubmed Central) -  Mar 6, 2023   
    In addition, during the first, but not the two consecutive sessions, both treatments prevented a thorough exploration of the OF. Altogether, these results confirm the crucial role played by the LHb in anxiety-related behaviours and further suggest its implication in the exploration of new anxiogenic environments.
  • ||||||||||  Synthesis of potentially neurotoxic and structurally novel heterocycles (Hall F-H (Indiana Convention Center)) -  Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_4846;    
    Analysis using 1H 1-D NMR and IR spectroscopy determined that beta-carboline was yielded. The synthesized beta-carboline and derivatives prepared from this beta-carboline will be analyzed to determine its impact on the GABAA receptor.
  • ||||||||||  Journal:  Claustrum modulates behavioral sensitivity and EEG activity of propofol anesthesia. (Pubmed Central) -  Nov 16, 2022   
    Claustrum neurones and their GABAa receptors are implicated in the modulation of propofol anesthesia in both behavioral and EEG assessments. Our findings create scope to reveal the brain targets of anesthetic action further and add to the existing evidence on the consciousness-modulating role of the claustrum.
  • ||||||||||  Neuroactive steroids in relation to a single electroconvulsive therapy seizure and subsequent clinical outcome (Poster area [IN-PERSON]) -  Oct 13, 2022 - Abstract #ECNP2022ECNP_1209;    
    Hormone concentrations or postictal change at the first seizure did not predict any outcome measures at the end of the ECT series. Our observation of postictal PROG increase after one ECT seizure in the male subgroup has to our knowledge not been reported previously, but should be considered preliminary, although worthwhile exploring further.
  • ||||||||||  gaboxadol (OV101) / Ovid Therapeutics, Angelini Group, Healx
    Gaba signaling coordinates escape circuit activity in zebrafish (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_12835;    
    Consistent with this, gaboxadol (GABAA receptor agonist) reduced LLC responses, whereas bicuculline (GABAA receptor antagonist) application resulted in a selective increase in LLCs...Video analysis showed that bicuculline-exposed fish failed to acutely suppress LLCs after initiating an SLC, significantly more frequently than in controls. These results demonstrate that GABAergic signaling downstream of Mauthner cell firing promotes execution of an optimal escape by blocking LLCs from interfering with ongoing SLCs.
  • ||||||||||  phenobarbital / Generic mfg., dalfampridine / Generic mfg.
    Enhancing delta-subunit containing GABAAreceptors reduces seizure-like activity in neonates and adults (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_12209;    
    Grant Support: NIH/NINDS R01NS115800, The Iowa Neuroscience InstitutePhenobarbital modulates inhibition by enhancing GABAA receptors and is the main anticonvulsant used to treat neonatal seizures...Field electrodes recorded seizure-like activity induced by either a potassium channel blocker (4-Aminopyridine, 4-AP) or Low-MgCl2 containing artificial cerebrospinal fluid...Our results indicate that enhancing extrasynaptic GABAA delta-containing receptors reduces seizure-like activity in neonates and adults. We conclude that THIP, and other delta-subunit-specific agonists, could serve as novel treatments for neonatal seizures.
  • ||||||||||  gaboxadol (OV101) / Ovid Therapeutics, Angelini Group, Healx
    Development of subtype-selective photoswitchable agonists for GABAA receptors (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_12204;    
    Because δ-GABAARs can be selectively activated by THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol; gaboxadol), we created a series of azobenzene-containing THIP analogues as the candidates of their photoswitchable agonist...A “red-shifted” photoswitchable agonist, DMAAI, has been tested on cultured hippocampal neurons and enabled 460-nm light to rapidly and reversibly silence action potential firing at 10 μM. Together, our results suggest a novel class of photoswitchable GABAAR agonists for precisely manipulating neuronal inhibition in diverse applications.
  • ||||||||||  bumetanide / Generic mfg.
    Sex differences in Cl- homeostasis in c-fiber primary afferent terminals in the spinal dorsal horn. (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_11342;    
    The GABAAR agonist and antagonist muscimol and bicuculline, respectively, as well as the NKCC1 antagonist bumetanide, were used to modulate [Cl-]i in afferent terminals in the dorsal horn... Presynaptic inhibition appears to be under distinct control by GABAergic inhibition between sexes, which should be taken into consideration in future studies.
  • ||||||||||  Spontaneous GABAA receptor activity in sensory axons contributes to exaggerated sensory transmission to motoneurons and spasms after spinal cord injury (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_8513;    
    Interestingly, GABAA receptor blockers that act as inverse agonists at the GABAA receptor, including L655708 and bicuculline, reduced tonic PAD after SCI (in TTX), whereas those that are neutral antagonists, like gabazine, did not, suggesting that the tonic PAD and associated GABAA receptor activity after SCI results partly from constitutive GABAA receptor activity. Overall, these results imply that, unlike in clinical practice, blocking GABA receptors, rather than activating them, might be useful in reducing spasms and restoring function after SCI.
  • ||||||||||  gaboxadol (OV101) / Ovid Therapeutics, Angelini Group, Healx
    Insulin effect on epileptiform activity in prefrontal cortex. (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_6810;    
    Our results suggest that insulin reduces the neuronal excitability by an increase of GABAergic tonic currents. These actions could help to explain the alterations of cognitive processes associated with changes in insulin signaling.
  • ||||||||||  Modulation of the prefrontal cortex alters auditory processing and impairs perception in a challenging listening environment (SDCC Halls B-H) -  Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_1870;    
    When the same procedure was performed in the presence of a challenging listening environment, performance on the AM detection paradigm further eroded, such that rats were no longer able to accurately identify a significantly modulated acoustic stimulus. Collectively, the present work provides evidence of a causal role of the prefrontal cortex in the processing of simple acoustic stimuli as well as its critical importance in supporting accurate auditory perception in challenging listening environments.
  • ||||||||||  bumetanide / Generic mfg.
    Sex differences in chloride homeostasis of c-fiber primary afferents in the spinal cord dorsal horn. () -  Jun 16, 2022 - Abstract #CANACN2022CAN_ACN_189;    
    The GABAAR agonist and antagonist muscimol and bicuculline, as well as the NKCC1 antagonist bumetanide, were used to modulate [Cl-]i in afferent terminals in the dorsal horn... Presynaptic inhibition appears to be under distinct control by GABAergic inhibition between sexes, which should be taken into consideration in future studies.
  • ||||||||||  Germanin (suramin) / Optimum Therap, Tectin (tetrodotoxin) / WEX Pharma
    Journal:  Age-related differences of γ-aminobutyric acid (GABA)ergic transmission in human colonic smooth muscle. (Pubmed Central) -  Apr 27, 2022   
    Nω-nitro-l-arginine methyl ester (L-NAME), nitric oxide (NO) synthase inhibitor abolished the inhibitory responses in old preparations, but a residual responses persisted in young preparations, which in turn was abolished by suramin, purinergic receptor antagonist...Activation of GABAA receptor, through acetylcholine release, induces contraction, which increases in amplitude with age. GABAB receptor activation leads to neural release of NO and purines, being a loss of purinergic-component in aged group.