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15 results about "TRPV4" patented technology
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Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the TRPV4 gene. The TRPV4 gene encodes TRPV4, initially named "vanilloid-receptor related osmotically activated channel" (VR-OAC) and "OSM9-like transient receptor potential channel, member 4 (OTRPC4)", a member of the vanilloid subfamily in the transient receptor potential (TRP) superfamily of ion channels. The encoded protein is a Ca²⁺-permeable, nonselective cation channel that has been found involved in multiple physiologic functions, dysfunctions and also disease. It functions in the regulation of systemic osmotic pressure by the brain, in vascular function, in liver, intestinal, renal and bladder function, in skin barrier function and response of the skin to ultraviolet-B radiation, in growth and structural integrity of the skeleton, in function of joints, in airway- and lung function, in retinal and inner ear function, and in pain. The channel is activated by osmotic, mechanical and chemical cues. It also responds to thermal changes (warmth). Channel activation can be sensitized by inflammation and injury.
Solid forms of TRPV4 antagonists
The present disclosure provides a solid form of 5-fluoro-1-(((5S, 7S, 8R)-8-fluoro-3-(5-(2-hydroxypropyl-2-yl) pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro [4.5] decane-7-yl) methyl)-1H-benzo [d] imidazole-6-formonitrile: which is useful as a TRPV4 antagonist.
Owner:ACTIO BIOSCIENCES INC
Pyrimidin-4(3H)-one derivatives as TRPV4 antagonists
This invention relates to pyrimidin-4(3H)-one derivatives of formula (I),that act as modulators of the TRPV4 receptor. The present invention also relates to processes for the preparation of novel pyrimidin-4(3H)-one derivatives of formula (I) and to their use in the treatment of a wide range of diseases, syndromes, and disorders, in particular, for the treatment of inflammation, pain, and urological diseases or disorders.
Owner:RAQUALIA PHARMA INC
Use of dasabuvir in the preparation of trpv4 inhibitors and ulcerative colitis drugs
This application discloses the application of dasabuvir as a TRPV4 inhibitor in improving diseases caused by increased TRPV4 expression or enhanced activity, particularly ulcerative colitis. Specifically, it relates to the biomedical field. Dasabuvir is a novel TRPV4 inhibitor that can improve symptoms in a DSS-induced mouse ulcerative colitis model and is suitable for use in TRPV4 inhibitor drugs and ulcerative colitis drugs. In HEK-293 cells overexpressing TRPV4, dasabuvir can dose-dependently inhibit the increase in intracellular calcium ion concentration induced by the TRPV4-specific agonist GSK1016790A within a concentration range of 0.03-30 μM, with an IC50 concentration of [missing information]. 50 At a concentration of 0.27 μM, Dasabuvir is a highly active TRPV4 inhibitor. In a DSS-induced ulcerative colitis model, Dasabuvir can improve weight loss, reduce the disease activity index, alleviate colonic shortening, reduce histopathological changes, and inhibit the expression of inflammatory factors, thus improving ulcerative colitis.
Owner:CHINA PHARM UNIV
Application of TRPV4 inhibitor in preparation of medicine for preventing or treating diseases caused by trimethyltin chloride poisoning
The invention belongs to the field of biological medicine, and relates to application of a TRPV4 inhibitor in preparation of a medicine for preventing or treating diseases caused by trimethyltin chloride poisoning. The TRPV4 ion channel inhibitor can remarkably prolong the incubation period of epilepsy caused by trimethyltin chloride poisoning, relieve the severity of epileptic seizure, improve nerve injury and increase the survival rate. Therefore, a new drug target is provided for diagnosis of trimethyltin chloride poisoning and drug research and development, and a new strategy is provided for clinical treatment of trimethyltin chloride poisoning.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES
Pharmaceutical composition comprising TRPV4 inhibitor for preventing or treating cerebral cavernous malformation (CCM)
The present invention relates to a pharmaceutical composition for preventing or treating cerebral cavernous malformation (CCM), comprising a transient receptor potential vanilloid 4 (TRPV4) inhibitor.
Owner:UNIVERSITE GRENOBLE ALPES +3
TRPV4, application of TRPV4 inhibitor, head and neck cancer medicine and in-vitro non-therapeutic inhibition method
The invention relates to application of TRPV4 and an inhibitor thereof, a head and neck cancer medicine and an in-vitro non-therapeutic inhibition method. According to the application of the TRPV4 as a head and neck cancer treatment target, the TRPV4 protein is remarkably and highly expressed in head and neck cancer tissues, and proliferation and migration of head and neck cancer cells can be inhibited and apoptosis can be promoted by knocking down the expression of the TRPV4 protein. The invention provides a novel therapeutic target for the head and neck cancer, and the target can be effectively used for judging and / or treating the head and neck cancer, so that a novel diagnostic and / or therapeutic agent is provided for the field and has a clinical application prospect.
Owner:SHENZHEN LONGGANG DISTRICT OTOLARYNGOLOGY HOSPITAL (SHENZHEN OTOLARYNGOLOGY RES INST SHENZHEN LONGGANG DISTRICT ORAL MEDICINE RES INST)
Compound for specifically enhancing spatial coupling degree of TRPV4-KCa2.3 complex and use thereof
The present disclosure provides a compound for specifically enhancing the spatial coupling degree of a TRPV4-KCa2.3 complex and use thereof, and belongs to the field of chemical medicine. The compound with a structure shown in a general formula (I) in the present disclosure is mainly used for re-coupling two uncoupled proteins and restoring the proteins to a normal state under uncoupling of TRPV4 and KCa2.3 in hypertensive patients. Under normal conditions of the TRPV4 and the KCa2.3, a signal of calcium ions is received by the TRPV4. As the calcium ions flow in, potassium ions in a KCa2.3 channel in the downstream are stimulated to flow out. Due to depolarization, vasodilation is caused, and therefore, the blood pressure of the hypertensive patients is returned to a normal level.
Owner:JIANGNAN UNIV
Fusion protein capable of regulating and controlling neuron activity, system for remotely controlling neuron activity and application
The invention provides a fusion protein capable of regulating and controlling neuron activity, a system for remotely controlling neuron activity and application, and belongs to the technical field of nerve regulation and control. The invention discloses a fusion protein with neuron regulation activity. The fusion protein is obtained by fusion expression of a delta TRPV4 protein and a magnetic receptor protein MagR. The MagR protein and a mechanically sensitive ion channel TRPV4 are subjected to fusion expression, the MagR enables a delta TRPV4 channel to be opened under the action of a magnetic field to trigger a cell calcium influx biological effect, intracellular calcium signal transduction is further regulated, the neuronal function is controlled, and then accurate and controllable regulation of brain region neuron subpopulation excitability is achieved.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES
Treatment of retinal ganglion cell loss
PendingUS20260048098A1Organic active ingredientsSenses disorderGrammostola spatulataMedicinal chemistry
The present invention is directed to methods of treating or preventing glaucoma comprising administering an effective amount of one or more compounds selected from the group consisting of transient receptor potential vanilloid 4 (TRPV4) antagonists, Grammostola spatulata MTx4 peptide and D-Grammostola spatulata MTx4 peptide to a subject in need thereof.The present invention is further directed to methods of treating or preventing retinal ganglion cell loss comprising administering an effective amount of one or more compounds selected from the group consisting of transient receptor potential vanilloid 4 (TRPV4) antagonists, Grammostola spatulata MTx4 peptide and D-Grammostola spatulata MTx4 peptide to a subject in need thereof.
Owner:PS THERAPY INC
Compositions and methods for the modulation of piezo1 and TRPV4
Described herein are methods and compositions for treating or reducing the likelihood of a subject developing a pancreatic disease or disorder or keloids. In one embodiment, the method comprises administering a therapeutically effective amount of one or more of a Piezol antagonist, a PLA2 antagonist, a TRPV4 antagonist, or combinations thereof.
Owner:DUKE UNIV
PYRIMIDIN-4(3H)-ON-DERIVATE ALS TRPV4-ANTAGONISTEN
Owner:RAQUALIA PHARMA INC
Application of chemical fiber formula of fortune euonymus herb in treatment of hepatic fibrosis
The invention discloses an application of a fortune euonymus herb chemical fiber formula in treatment of hepatic fibrosis, and relates to the field of biological medicines. According to the present invention, the anti-hepatic fibrosis effect is provided by inhibiting hepatic stellate cell activation and reducing extracellular matrix deposition, and the hepatic fibrosis is the chronic liver injury pathological stage caused by viral hepatitis, alcoholic liver disease, non-alcoholic fatty liver disease or drug-induced liver injury; in an in-vitro experiment, the euonymus fortunei chemical fiber formula also plays a role in resisting hepatic fibrosis by inhibiting a transient receptor potential vanillic acid subtype 4 signal channel. The method has the following comprehensive advantages that (1) HSC activation and ECM deposition are inhibited through multi-component and multi-target cooperation; (2) key signal channels such as TGF-beta1 / Smad, TRPV4 and the like can be regulated and controlled at the same time; (3) liver function indexes are obviously improved, and tissue structure damage is relieved; and (4) the medicine is natural in source, high in safety and suitable for long-term application.
Owner:CHONGQING TRADITIONAL CHINESE MEDICINE HOSPITAL +1
Application of narirutin targeting to TRPV4 channel in preparation of medicine or preparation for treating alopecia
The invention discloses an application of Narirutin (NR) of a targeted TRPV4 (transient receptor potential vanilloid 4) channel in preparation of a medicine or a preparation for treating alopecia. The narirutin is an active component separated from citrus, and experiments prove that the narirutin can promote activation of hair follicle melanocyte and melanin synthesis and effectively relieve androgen-induced alopecia, so that the phenotype of a mouse with androgenetic alopecia is improved, and hair growth is promoted. The narirutin is high in safety and convenient to use, so that the narirutin has wide application prospects in the fields of pharmaceutical preparations, cosmetics, care products, health care products, beauty products and the like for preventing, nursing and treating less hair and alopecia and promoting hair health and growth.
Owner:HANGZHOU THIRD PEOPLES HOSPITAL (HANGZHOU HUIMIN HOSPITAL HANGZHOU THIRD AFFILIATED HOSPITAL OF ZHEJIANG UNIV OF TRADITIONAL CHINESE MEDICINE)
Compositions and methods for hair follicle regeneration
Among the various aspects of the present disclosure is the provision of compositions and methods for treating hair regeneration disorders or conditions such as hair loss or thinning. An aspect of the present disclosure provides for a method of treating hair loss, promoting hair growth, or treating hair loss, such as alopecia or telogen effluvium, comprising administering a TRPV4 activating agent to a subject.
Owner:WASHINGTON UNIV IN SAINT LOUIS