Aquaporin 4 inhib 
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  • ||||||||||  Journal:  Glymphatic inhibition exacerbates tau propagation in an Alzheimer's disease model. (Pubmed Central) -  Apr 4, 2024   
    These results indicate that by modulating AQP4 function and, consequently, glymphatic clearance, it is possible to modify the propagation and pathological impact of tau in the brain, particularly during the initial stages of the disease. These findings highlight the critical role of the glymphatic system in preserving healthy brain homeostasis and offer valuable insights into the therapeutic implications of targeting this system for managing neurodegenerative diseases characterized by protein aggregation and spread.
  • ||||||||||  AER-271 / Aeromics
    Journal:  Glymphatic fluid transport is suppressed by the aquaporin-4 inhibitor AER-271. (Pubmed Central) -  Mar 20, 2024   
    Importantly, AER-271 did not affect AQP4 localization to the astrocytic endfeet, nor have any effect in AQP4 deficient mice. Since acute pharmacological inhibition of AQP4 directly decreased glymphatic flow in wild-type but not in AQP4 deficient mice, we foresee AER-271 as a new tool for manipulation of the glymphatic system in rodent brain.
  • ||||||||||  Journal:  Norepinephrine-Activated p38 MAPK Pathway Mediates Stress-Induced Cytotoxic Edema of Basolateral Amygdala Astrocytes. (Pubmed Central) -  Feb 23, 2024   
    Briefly, NE-induced activation of the p38 MAPK pathway mediated cytotoxic edema in BLA astrocytes from RS rats. Thus, our data provide novel evidence that NE-induced p38 MAPK pathway activation may be one of the mechanisms leading to cytotoxic edema in BLA under stress conditions, which also could enable the development of an effective therapeutic strategy against cytotoxic edema in BLA under stress and provide new ideas for the treatment of neuropsychiatric diseases.
  • ||||||||||  Mytesi (crofelemer) / Jaguar Health, Knight Therap
    Journal:  Toward New AQP4 Inhibitors: ORI-TRN-002. (Pubmed Central) -  Jan 27, 2024   
    Thus, our data provide novel evidence that NE-induced p38 MAPK pathway activation may be one of the mechanisms leading to cytotoxic edema in BLA under stress conditions, which also could enable the development of an effective therapeutic strategy against cytotoxic edema in BLA under stress and provide new ideas for the treatment of neuropsychiatric diseases. Evaluating ORI-TRN-002 on AQP4-expressing Xenopus laevis oocytes using a high-resolution volume recording system revealed an IC of 2.9
  • ||||||||||  Journal:  Mechanisms of aquaporin-4 vesicular trafficking in mammalian cells. (Pubmed Central) -  Dec 16, 2023   
    AQP4 trafficking mechanisms were validated in primary human astrocytes, which express high levels of endogenous AQP4. The results highlight the role of early and recycling endosomes and cytoskeletal dynamics in AQP4 translocation in response to hypotonic and hypoxic stress and suggest continuous cycling of AQP4 between intracellular vesicles and the cell surface under physiological conditions.
  • ||||||||||  Journal:  miR-211-5p targeting MMP9 regulates the expressions of AQP4 in traumatic brain injury. (Pubmed Central) -  Jul 14, 2023   
    Findings suggest that AQP4 deficiency could be associated with autistic disorder and may be a potential pharmaceutical target for treating autism in the future. miR-211-5p inhibits the MMP9/AQP4 axis in human astrocyte cells, which represents a promising approach for the TBI treatment.
  • ||||||||||  Water channel Aquaporin 4 is required for T cell activation. (P1018) (Exhibit Hall; Poster Board No. P1018) -  Apr 11, 2023 - Abstract #IMMUNOLOGY2023IMMUNOLOGY_1351;    
    We found that loss of AQP4 resulted in significantly impaired TCR capping and dysfunctional post-TCR stimulation actin remodeling kinetics. Our findings reveal novel mechanisms underlying the importance of AQP4 in optimal T lymphocyte activation and identify AQP4 as a potential therapeutic target for preventing TCR-mediated T cell activation in solid organ transplantation and other diseases.
  • ||||||||||  temozolomide / Generic mfg.
    Biomarker, Journal, MRI:  Transmembrane water-efflux rate measured by magnetic resonance imaging as a biomarker of the expression of aquaporin-4 in gliomas. (Pubmed Central) -  Mar 28, 2023   
    Water-efflux rates correlated with stages of glioma proliferation as well as with changes in the heterogeneity of intra-tumoural and inter-tumoural AQP4 in rodent and human gliomas following treatment with temozolomide and with the AQP4 inhibitor TGN020. Regions with low water-efflux rates contained higher fractions of stem-like slow-cycling cells and therapy-resistant cells, suggesting that maps of water-efflux rates could be used to identify gliomas that are resistant to therapies.
  • ||||||||||  Journal:  Matrix metalloproteinase-9 inhibition prevents aquaporin-4 depolarization-mediated glymphatic dysfunction in Parkinson's disease. (Pubmed Central) -  Mar 21, 2023   
    Regions with low water-efflux rates contained higher fractions of stem-like slow-cycling cells and therapy-resistant cells, suggesting that maps of water-efflux rates could be used to identify gliomas that are resistant to therapies. AQP4 depolarization contributes to glymphatic dysfunction and aggravates PD pathologies, and MMP-9-mediated ?-DG cleavage regulates glymphatic function through AQP4 polarization in PD, which may provide novel insights into the pathogenesis of PD.
  • ||||||||||  Water channel Aquaporin 4 is required for T cell activation (Grand Georgian) -  Mar 10, 2023 - Abstract #ITS2023ITS_17;    
    We found that the absence or inhibition of AQP4 resulted in significantly impaired TCR capping as well as dysfunctional post-TCR stimulation actin remodeling kinetics. Our findings reveal novel mechanisms underlying AQP4 importance in optimal T lymphocyte activation and identify AQP4 as a potential therapeutic target for preventing TCR-mediated T cell activation in solid organ transplantation and other diseases.
  • ||||||||||  trifluoperazine / Generic mfg.
    Drugging aquaporins (Sagamore Ballroom 2 (Indiana Convention Center)) -  Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_316;    
    Given the difficulties in developing pore-blocking aquaporin-4 inhibitors or activators and controversies in the field over the status of many proposed molecules, targeting dynamic aquaporin-4 subcellular relocalization provides a new approach to modulating aquaporin-4 function. This approach opens up new treatment avenues for CNS oedema, neurovascular and neurodegenerative diseases.Targetting aquaporin-4 subcellular relocalization with the licenced drug trifluoperazine reduces central nervous system oedema and promotes functional recovery.
  • ||||||||||  minocycline / Generic mfg.
    Preclinical, Journal:  A novel aquaporin-4-associated optic neuritis rat model with severe pathological and functional manifestations. (Pubmed Central) -  Nov 4, 2022   
    We established an AQP4-IgG-induced ON rat model with severe functional impairments that reproduce the histological characteristics of patients with NMO. Using this model, we revealed that minocycline treatment ameliorates functional and pathological outcomes, highlighting the usefulness of our model for evaluating potential therapeutic drugs for ON in NMO.
  • ||||||||||  sirolimus / Generic mfg.
    Preclinical, Journal:  Autophagy promotes membrane trafficking of NR2B to alleviate depression by inhibiting AQP4 expression in mice. (Pubmed Central) -  Aug 31, 2022   
    Rapamycin treatment enhanced the expression of NR2B (surface), and repressed the expression of AQP4, NR2B (intracellular) and P-NR2B in the primary hippocampal neurons by activating autophagy...In conclusion, our data demonstrated that autophagy ameliorated depression by repressing AQP4 expression in mice, and AQP4 knockdown promoted membrane trafficking of NR2B and inhibited phosphorylation of NR2B via CaMK II/CK2 pathway. Thus, our work suggests that AQP4 may be a promising molecular target for the development of antidepressant drugs.
  • ||||||||||  Aquaporin 4 is a Mediator of Essential Dendritic Cell Functions (Hynes Room 309) -  May 20, 2022 - Abstract #ATC2022ATC_1486;    
    Moreover, ADCuh could reflect the AQP4 polarization. Our data indicate that AQP4 plays a critical role in the processing of antigens by dendritic cells that impacts their ability to prime T cells, and can be therapeutically targeted in a transplant setting.
  • ||||||||||  Aquaporin 4 Is A Mediator Of Essential Dendritic Cell Function (Exhibit Hall; P116) -  Apr 8, 2022 - Abstract #IMMUNOLOGY2022IMMUNOLOGY_1574;    
    Consistent with this, the absence or inhibition of AQP4 resulted in decreased DQ-OVA signal, indicating that AQP4 is required for the antigen loading into the lysosome. Our data indicate that AQP4 plays a critical role in the processing of antigens by dendritic cells that impacts their ability to prime T cells, and can be therapeutically targeted in a transplant setting.
  • ||||||||||  Journal:  Emerging roles for dynamic aquaporin-4 subcellular relocalization in CNS water homeostasis. (Pubmed Central) -  Apr 2, 2022   
    We have demonstrated that reducing dynamic relocalization of AQP4 to the BSCB/BBB reduces CNS oedema, and accelerates functional recovery in rodent models. Given the difficulties in developing pore-blocking AQP4 inhibitors, targeting AQP4 subcellular localization opens up new treatment avenues for CNS oedema, neurovascular and neurodegenerative diseases, and provides a framework to address fundamental questions about water homeostasis in health and disease.
  • ||||||||||  dizocilpine (MK801) / Merck (MSD)
    Review, Journal:  Aquaporin 4 in Traumatic Brain Injury: From Molecular Pathways to Therapeutic Target. (Pubmed Central) -  Apr 1, 2022   
    In addition, inhibition of AQP4 with FK-506, MK-801 (indirectly by targeting N-methyl-D-aspartate receptor), inactivation of adenosine A2A receptor, levetiracetam, adjudin, progesterone, estrogen, V1aR inhibitor, hypertonic saline, erythropoietin, poloxamer 188, brilliant blue G, HIF-1alpha inhibitor, normobaric oxygen therapy, astaxanthin, epigallocatechin-3-gallate, sesamin, thaliporphine, magnesium, prebiotic fiber, resveratrol and omega-3, as well as AQP4 gene silencing lead to reduced edema upon TBI. This review summarizes current knowledge and evidence on the relationship between AQP4 and TBI, and the potential mechanisms involved.
  • ||||||||||  minocycline / Generic mfg.
    Journal:  Minocycline improves the functional recovery after traumatic brain injury via inhibition of aquaporin-4. (Pubmed Central) -  Mar 29, 2022   
    In primary cultured astrocytes, small-interfering RNA (siRNA) AQP4 treatment prevented glutamate-induced astrocyte swelling. To sum up, our study suggests that minocycline improves the functional recovery of TBI through reducing AQP4 level to optimize BBB integrity and astrocyte function, and highlights that the AQP4 may be an important therapeutic target during minocycline treating for TBI.
  • ||||||||||  Soliris (eculizumab) / AstraZeneca
    Journal:  Targeting the complement system in neuromyelitis optica spectrum disorder. (Pubmed Central) -  Feb 1, 2022   
    Clinical studies supported the approval of eculizumab, an inhibitor of C5 cleavage, in AQP4-IgG seropositive NMOSD...Various drug candidates targeting distinct complement effector mechanisms may offer improved safety and efficacy. However, notwithstanding the demonstrated efficacy of complement inhibition in AQP4-IgG seropositive NMOSD, the ultimate niche for complement inhibition is not clear given multiple drug options with alternative mechanisms of action.