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Showing 1 to 20 of 31 for “"allosteric modulator"”.

  1. Pharmacology of a novel biased allosteric modulator for NMDA receptors

    Kwapisz, LinaVirginia Tech2021

    … approach to regulate NMDAR receptors is thorough allosteric modulators that could allow cell type or circuit-specific modulation, due to widely distributed GluN2 expression, without global NMDAR overactivation59,65,122. In one study, we hypothesized that the compound CNS4 selectively modulates …

    vt Repository record

  2. Pharmacological and Pharmacokinetic Studies of a K<sub>Ca</sub>2.2 Positive Allosteric Modulator

    Rahman, Mohammad Asikur2024

    … channel rescued by a K<sub>Ca</sub>2.2 positive modulator. A positive allosteric modulator of K<sub>Ca</sub>2.2/K<sub>Ca</sub>2.3 channels (compound <strong>2q</strong>) has been developed, and a method for quantitating it in mouse plasma has been validated using FDA guidelines. The developed …

    chapman Repository record

  3. Role of Microglial α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator in Neuroinflammatory Pain Models in Mice

    Abbas, Muzaffar2019

    … hypothesized that microglial α7 nAChRs positive allosteric modulation in the hippocampus will decrease neuroinflammatory pain at behavioral, cellular, biochemical, and molecular level. The primary objective of current study was to examine the role of an α7 nAChR positive allosteric modulator …

    sdstate Repository record

  4. Testing the efficacy of LSN2463359, a metabotropic glutamate 5 receptor positive allosteric modulator, in animal models of schizophrenia

    Freamon, Dierdre M.2016

    … of the metabotropic glutamate 5 receptor modulator LSN2463359, previously shown to act as an indirect agonist of the NMDA receptor, in two different animal models of schizophrenia. Our study found that when LSN2463359 was administered to rats given SDZ 220-581 (an NMDA antagonist) levels …

    shu-thes Repository record

  5. Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine

    Alcaino-Ayala, COxford Brookes University2015

    Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. By binding to a site of the receptor distinct from the neurotransmitter binding site, allosteric modulators alter the response of the receptors to …

    oxford-brookes Repository record

  6. Structural and molecular determinants of the sensitivity of alpha4beta2 nicotinic acetylcholine receptors to the allosteric ligand desformylflustrabromine

    Alcaino-Ayala, Constanza AlejandraOxford Brookes University

    Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. By binding to a site of the receptor distinct from the neurotransmitter binding site allosteric modulators alter the response of the receptors to …

    oxford-brookes Repository record

  7. Small Molecule Allosteric Modulation of G Protein-Coupled Receptors and Applications in the Pharmacological Targeting of 5-HT2 Receptors

    Wold, Eric A.The University of Texas Medical Branch at Galveston2021

    … target GPCRs. Predictably, small molecule allosteric modulation has emerged in recent years as a new means to control GPCR function with numerous examples nearing FDA approval. This body of work begins with a substantive review of drug discovery efforts in the development of Class A GPCR …

    utmb Repository record

  8. Characterisation of novel alpha1-adrenoceptor ligands

    Chen, JunliUNSW, Sydney2014

    … pocket, but that C7-C11 interacted with a second allosteric site in a bitopic manner. 4-aminoquinoline, C9, C10, and C11 increased the dissociation rate of [3H] prazosin from the α1A-AR, suggesting allosteric modulation. C9 was further characterised and demonstrated to be a negative allosteric …

    unsw Repository record

  9. Excitotoxic Injury Mechanisms in Central White Matter

    Doyle, Seán P.2017

    … myelin stain (QNZ-46) which is a negative allosteric modulator of NR2C/D-containing NMDA receptors. QNZ-46 selectively accumulates in myelinated WM regions of the CNS following systemic administration, and is retained following wash-out. As a result, QNZ-46 provides persistent protection …

    plymouth Repository record

  10. The Structural Mechanism of Allosteric Modulation of The Nmda Receptor: A Balance of Tensions

    Sirrieh, Rita E.2015

    … disorders. Studies targeting the mechanism of allosteric modulation, such as this study, hope to contribute to the understanding of how NMDA receptors are modulated to allow for better drug development.</p> <p>NMDA receptors are obligate heterotetramers, typically composed of glycine-binding …

    uthsc Repository record

  11. Aromatic Amino Acid Metabolome In The Human Gut Microbiota

    Hsieh, David Chun-cheng2027

    … of phenylacetic acid, a precursor of negative allosteric modulator (NAM) for β2-adrenergic receptor (β2AR). This work highlights several interesting metabolites specific to C. <em>difficile</em>, with potential biological roles that warrant further exploration.</p>

    rockefeller Repository record

  12. NOVEL THERAPEUTIC APPROACHES EMERGING FROM HCN CHANNELS STRUCTURAL AND FUNCTIONAL STUDIES

    CASTELLI, ROBERTAUniversità degli Studi di Milano2026

    … We further explore the use of pore blockers and allosteric modulators to restore wild-type-like function in mutant HCN1 channels in vitro, highlighting the potential of precision medicine approaches tailored to mutation-specific phenotypes. Extending these studies ex vivo, we demonstrate that the …

    milano Repository record

  13. Allosteric Modulation of Metabotropic Glutamate Receptor 5 as a Treatment for Pain

    Montana, Michael2012

    … a selective and potent non-competitive negative allosteric modulator of mGlu5, and previously shown to be safe and effective in clinical trials of human anxiety. I found Fenobam to be analgesic in models of chemical nociception and inflammatory pain. Fenobam was also found to be without analgesic …

    wustl Repository record

  14. Studies on rationally designed, allosteric, coagulation inhibitors

    Boothello, Rio2019

    Heparin is a natural allosteric modulator, with numerous structural and conformational variations leading to many reports of bleeding complications and variations in anticoagulant effects. A flurry of research has been directed towards understanding this puzzle. This work entails the utilization of …

    vcu Repository record

  15. Characterizing novel protease activated receptor 2 compounds for potential use in examining depression-like behavior

    Coyle, ChelbiUniversity of Strathclyde2020

    … of the recently developed PAR2 negative allosteric modulator (NAM) AZ8838.;Methods: The selectivity of SLIGRL-NH2 and AC264613 was examined by transfecting tsA201 cells with either PAR2-YFP or MrgprC11-YFP, which were then exposed to the proposed activators and imaged using the …

    strathclyde Repository record

  16. Neonatal exposure to estradiol in female rats influences neuroactive steroid concentrations and behaviour in the adult rat

    BERRETTI, ROBERTAUniversità degli Studi di Cagliari2013

    … in the behavioural sensitivity to the positive allosteric modulator of the GABAA receptor, diazepam. These effects of estradiol suggest that it plays a major role in pharmacological regulation both of GABAergic transmission and of the abundance of endogenous modulators of such transmission …

    cagliari Repository record

  17. The Emergence of Network Hyperexcitability and Functional Impairment in a Mouse Model of Alzheimer’s Disease

    Turner, RichardUniversity of Cambridge2024

    … α1-selective nanobody, acting as a positive allosteric modulator, was shown to decrease activity in WT networks but paradoxically exacerbate burst-driven hyperexcitability in AppNL-G-F networks in a dose-dependent manner. Perturbed excitation-inhibition balance, and consequent network …

    cambridge Repository record

  18. Design, Synthesis, and Pharmacological Characterization of Serotonin (5-HT) 5-HT2C Receptor (5-HT2CR) Positive Allosteric Modulators

    Wild, Christopher TimothyThe University of Texas Medical Branch at Galveston

    … pharmacologically evaluated as 5-HT2CR positive allosteric modulators (PAMs). Several analogues potentiated intracellular calcium release by 5-HT in h5-HT2CR-CHO cells. Several compounds exhibited a favorable overall pharmacokinetic profile and modulated 5-HT2CRassociated behaviors (e.g., …

    utmb Repository record

  19. Characterization Of Initial Iron Binding Location And The Structure/iron Binding Site On S.cerevisiae Isu And On D.melanogaster Frataxin

    Rodrigues, Andria V.2014

    … the capacity of a potential iron provider and an allosteric modulator of both the cysteine desulfurase and scaffold protein ISU. My research has been focused on studying the interaction between frataxin and ISU, particularly the mechanism of iron binding/ iron acceptance by ISU from frataxin. …

    wayne-thes Repository record

  20. Effect Of CBD On D2 Dopamine Receptor And CB1 Cannabinoid Receptor Function And Localization

    Dull, ElizabethEastern Kentucky University

    … suggests that CBD may also be a CB1 negative allosteric modulator of (−)-trans-Δ9-tetrahydrocannabinol (Δ9-THC). Interestingly, the ECS is linked to the main circuit thought to modulate reward signaling when taking substances of abuse, the dopamine (DA) pathway. The DA pathway contains …

    eku Repository record

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