GABA A receptor agon 
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  • ||||||||||  ketamine / Generic mfg.
    THE USE OF PHENOBARBITAL IN ECMO ([VIRTUAL]) -  Mar 23, 2022 - Abstract #SCCM2022SCCM_1937;    
    Based on our results, we concluded that limited drug sequestration occurred within the circuit and no dosing adjustment may be needed. The standard dose may be similar to non-ECMO patients and should be guided by therapeutic drug monitoring.
  • ||||||||||  Journal:  GABA receptors in the olfactory epithelium of the gilthead seabream (Sparus aurata). (Pubmed Central) -  Mar 11, 2022   
    Furthermore, exposure of the OE to muscimol (a specific GABAA receptor agonist) increases or decreases the apparent olfactory sensitivity to some odorants. Thus, although the exact function of GABAA receptors in the OE is not yet clear, this may complicate the interpretation of studies wherein water-borne gabazine is used to reverse the effects of high CO2 levels on olfactory-driven behaviour in fish.
  • ||||||||||  The Mechanism of Novel Benzodiazepine PI320-Mediated Airway Relaxation in Mouse Lung Slice (Room 2009/2011 (West Building, Level 2), Moscone Center) -  Feb 19, 2022 - Abstract #ATS2022ATS_809;    
    Although PI320 is a GABAAR ligand, this relaxation does not appear to be totally GABAAR-dependent or totally the result of inhibited ASM calcium influx. We further demonstrated that PI320 inhibits airway constriction induced by exogenous IP3 and inhibits MCh-mediated calcium oscillations in ASM cells.
  • ||||||||||  Multifunctional fiber-based neurotechnology enables cortical neuromodulation in non-human primates (Virtual Only) -  Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_9539;    
    An infusion of saline at 50 nl/min did not reduce the firing rate. In summary, we translated and validated multifunctional fiber-based devices in NHPs.; Grant Support: NIMH R37MH087027; Picower Institute for Learning and Memory (ENB, EKM, AJM); NSF DMR-1419807 (PA); McGovern Institute for Brain Research (PA); NSF EEC-1028725 (PA); National Institutes of Health Award P01-GM118629 (ENB, EKM); NSF GRFP 1745302 (ICG); National Institutes of Health Award 5T32EB019940-05 (ICG); Simons Center for the Social Brain Postdoctoral Fellowship (AJM); ONR MURI N00014-16-1-2832
  • ||||||||||  Layer-specific deactivation of prefrontal cortex as a causal test of predictive coding (Virtual Only) -  Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_7738;    
    In support of the model, preliminary data show deactivation of deep-layer PFC resulted in heightened V4 gamma and spiking activity. This work will provide a causal test to a prevalent model of laminar cortical processing and yield specific insights into conditions related to sensory filtering, such as autism spectrum disorder and schizophrenia.; Grant Support: NIMH R37MH087027; The MIT Picower Institute Innovation Fund; ONR MURI N00014-16-1-2832; Simons Center for the Social Brain Postdoctoral Fellowship
  • ||||||||||  memantine / Generic mfg.
    Fluoroethylnormemantine (FENM) used in combination with other therapeutic drugs offers new opportunities in Alzheimer's disease (Virtual Only) -  Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_2139;    
    Results confirmed that FENM presents a different neuroprotective profile than its parent molecule memantine and which extend to the way FENM is active when used in combination with combination with other pharmacological agents. Particularly, outstanding results for combination potentially useful in the treatment of AD will be exposed and discussed.; Grant Support: SATT AXLR /UM 210384
  • ||||||||||  Increased excitability of pyramidal neurons in the secondary motor cortex mediates cocaine relapse (Virtual Only) -  Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_1264;    
    Our results demonstrate that cocaine IVSA induces differential short-term and prolonged excitability changes in the motor cortex and mPFC. Importantly, the increased excitability in the M2, particularly in L2, as a prolonged effect after cocaine IVSA, could be a novel target in preventing drug-relapse during withdrawal.; Grant Support: NIH Grant: R01AA028938; NIH Grant: R01AA025784; NIH Grant: R21NS108128
  • ||||||||||  amantadine / Generic mfg.
    Preclinical, Journal:  GABAergic and glutamatergic effects on nigrostriatal and mesolimbic dopamine release in the rat. (Pubmed Central) -  Sep 26, 2021   
    In these studies, [123I]iodobenzamide binding to the D2/3R was mesured in nucleus accumbens (NAC), caudateputamen (CP), substantia nigra/ventral tegmental area (SN/VTA), frontal (FC), motor (MC) and parietal cortex (PC) as well as anterior (aHIPP) and posterior hippocampus (pHIPP) with small animal SPECT in baseline and after injection of either the GABAAR agonist muscimol (1 mg/kg), the GABAAR antagonist bicuculline (1 mg/kg), the NMDAR agonist d-cycloserine (20 mg/kg) or the NMDAR antagonist amantadine (40 mg/kg)...Taken together, similar actions on regional dopamine levels were exterted by the GABAAR agonist and the NMDAR antagonist on the one side and by the GABAAR antagonist and the NMDAR agonist on the other, with agonistic action, however, affecting more brain regions. Thereby, network analysis suggests different roles of GABAARs and NMDARs in the mediation of nigrostriatal, nigrothalamocortical and mesolimbocortical dopamine function.
  • ||||||||||  Dayvigo (lemborexant) / Eisai, Belsomra (suvorexant) / Merck (MSD)
    Journal:  Current and emerging therapies for insomnia. (Pubmed Central) -  Sep 22, 2021   
    However, several other agents are in later stages of development. This article will review the available pharmacotherapeutic options for treating insomnia.
  • ||||||||||  bumetanide / Generic mfg.
    [VIRTUAL] Sex differences in chloride homeostasis of c-fiber primary afferents in the spinal cord dorsal horn. () -  Sep 10, 2021 - Abstract #CANACN2021CAN_ACN_242;    
    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.
  • ||||||||||  morphine sulphate / Generic mfg.
    Journal:  GABA-cannabinoid interplays in the dorsal hippocampus and basolateral amygdala mediate morphine-induced amnesia. (Pubmed Central) -  Aug 19, 2021   
    It should be noted that the intra-CA1 microinjection of muscimol, intra-BLA microinjection of WIN55,212-2 or AM251 alone could not affect memory consolidation. Accordingly, it can be concluded that there may be a synergistic interaction between the CA1 GABAergic system and the BLA endocannabinoid neurotransmission with respect to the modulation of morphine-induced memory impairment.
  • ||||||||||  Journal:  Cell transplantation of retinal ganglion cells derived from hESCs. (Pubmed Central) -  Aug 4, 2021   
    Accordingly, it can be concluded that there may be a synergistic interaction between the CA1 GABAergic system and the BLA endocannabinoid neurotransmission with respect to the modulation of morphine-induced memory impairment. Our protocol provides a novel, short, and cost-effective approach for RGC differentiation from hESCs, and may broaden the scope for cell replacement therapy in RGC-related optic neuropathies such as glaucoma.
  • ||||||||||  Journal:  Activation state of the supramammillary nucleus regulates body composition and peripheral fuel metabolism. (Pubmed Central) -  Jun 23, 2021   
    Consistent with these results, circadian-timed activation of neuronal activity at the SuMN area with daily local infusion of glutamate receptor agonists, AMPA or NMDA at the natural daily peak of SuMN neuronal activity improved insulin resistance and obesity in high fat diet-induced insulin resistant animals. These studies are the first of their kind to identify the SuMN area as a novel brain locus that regulates peripheral fuel metabolism.
  • ||||||||||  ByFavo (remimazolam) / PAION, Cosmo Pharma, Mundipharma, Pharmascience, Acacia Pharma
    Journal:  Remimazolam: a short-acting benzodiazepine for procedural sedation. (Pubmed Central) -  Jun 8, 2021   
    Remimazolam is highly selective in its action, only having activity at the GABAA receptor. It has been shown to be highly effective in providing sedation for bronchoscopy and colonoscopy without having a prolonged duration of action, therefore having a short effect until patients are fully awake and ready for discharge.
  • ||||||||||  Journal:  Amygdala inhibition impairs fear conditioning but increases the stimulus-driven activity in the inferior colliculus. (Pubmed Central) -  May 1, 2021   
    We repeated the injection protocol with another group of rats but without pairing the tone to an aversive stimulus and observed that the inhibition of the basolateral amygdala enhances the stimulus-driven activity in the inferior colliculus regardless of the conditioning task. Our findings suggest that the basolateral amygdala exerts a tonic modulation over the encoding of sensory information at the early stages of the sensory pathway.
  • ||||||||||  ganaxolone oral (CCD-1042) / Marinus
    Review, Journal:  Experimental GABA A Receptor Agonists and Allosteric Modulators for the Treatment of Focal Epilepsy. (Pubmed Central) -  Mar 18, 2021   
    Several compounds with more selective action on GABA A receptors, perhaps only in certain brain regions, have the potential to become effective drugs against specific subtypes of focal-onset epilepsy. However, their development needs time, and in the near future we can expect only one or two new GABA A agonists to obtain marketing authorization for focal epilepsy, an advance that would be of use for just a fraction of patients with drug-resistant epilepsy.
  • ||||||||||  [VIRTUAL] PKA signaling: a friend or foe to pediatric medulloblastoma () -  Mar 11, 2021 - Abstract #AACR2021AACR_1454;    
    To our knowledge, this study for the first time focuses on GABAA receptor agonist mediated PKA/Gli1 signaling inhibition. Most importantly, moxidectin is an FDA approved drug and is already in clinical use for the treatment of river blindness in humans with an established safety record, therefore any positive findings from our studies will prompt further clinical investigation into repositioning moxidectin for the treatment of MB patients.
  • ||||||||||  Clinical, Journal:  Zolpidem related persistent genital arousal disorder: An interesting case. (Pubmed Central) -  Sep 20, 2020   
    Nevertheless, in our patient, receiving zolpidem for insomnia seemed to be timely connected to the onset of PGAD symptomatology. The aim of the present paper is to highlight the need for more research into the possible factors that may contribute to PGAD.
  • ||||||||||  sirolimus / Generic mfg., University of Cincinnati
    Preclinical, Journal:  Hypothesis-driven investigations of diverse pharmacological targets in two mouse models of autism. (Pubmed Central) -  Apr 19, 2020   
    Combining pharmacological and behavioral therapies could reduce symptoms and improve the quality of life for people with autism. Here we report reductions in repetitive behavior by a GABA-A receptor agonist, gaboxadol, and improvements in social and cognitive behaviors by a TrkB receptor agonist, in mouse models of autism.
  • ||||||||||  Clinical, Journal:  Convection-Enhanced Delivery of Muscimol in Patients with Drug-Resistant Epilepsy. (Pubmed Central) -  Mar 26, 2020   
    This study did not confirm that intracerebral muscimol infusion effectively suppressed seizures. A surrogate tracer is recommended to track infusion distribution to the epileptic focus and surrounding structures in future studies using CED to suppress the seizure focus.
  • ||||||||||  Anxiolytic, antinociceptive and anticonvulsant effect of α2/3-subtype selective GABAA receptor agonist KRM-ii-81 (Exhibit Hall D, Pennsylvania Convention Center) -  Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_4107;    
    KRM-II-81 had much greater BBB penetration, as indicated by the high concentration of compound found within brain samples two hours after oral administration, whereas HZ-I-66 was below the quantifiable limit (< 12 nM). The results of these studies indicate that KRM-II-81 or its analogs have great potential to advance to clinical trials as non-sedating anxiolytic, anticonvulsant and antinociceptive agents, which do not develop tolerance to the anticonvulsant or antinociceptive effects.
  • ||||||||||  Decadron (dexamethasone) / Merck (MSD)
    Immunological stress during development might delay pubertal onset through altering Srd5a1 gene regulation in GnRH-neurons () -  Dec 16, 2019 - Abstract #Fertility2020FERTILITY_171;    
    Our findings suggest that immunological stress during pre-pubertal development could inhibit Srd5a1 upregulation by DHEA, potentially explaining delayed puberty in Bangladeshi girls. These preliminary data support observations of a developmental window at adrenarche when immunological stress could affect neurosteroid metabolism and fine-tune the GABAergic system.
  • ||||||||||  Journal:  The Effect of Serotonin on Penicillin-induced Epileptiform Activity. (Pubmed Central) -  Sep 6, 2019   
    CBT-I may promote dose reduction by optimizing the protocol and duration of treatment. The electrophysiological data from the present study suggest that serotonin 5-HT receptors have an important role in controlling penicillin-induced epileptiform activity in the rat.
  • ||||||||||  Journal:  AT1a influences GABAa mediated inhibition through the regulation of KCC2 expression. (Pubmed Central) -  Aug 30, 2019   
    The impaired GABAA mediated inhibition in AT1a knockdown neurons was recovered by bath application of phospholipase C (PLC) and protein kinase C (PKC) activators. The following study indicates that AT1a receptor activation mediates the excitability of MnPO neurons, in part, through the regulation of KCC2.
  • ||||||||||  S20: Pathophysiological insights from animal models of restless legs syndrome (217-219) -  Aug 20, 2019 - Abstract #WSS2019WSS_588;    
    They come from 3 countries and one speaker is a successful women scientist. Learning Objectives Upon Completion of this CME activity, participants should be able to: Recall the latest update on the pathophysiology of the RLS from the studies of iron deficient rats Recognize the biological function of BTBD9 and MEIS1 and how mutations of these genes can cause RLS Indentify how animal models can be constructed and used to gain pathophysiological insights of RLS Recognize how these new pathophysiological insights can inspire new targeted therapy of RLS Target Audience Clinicians, basic research scientists, technologists interested in RLS