87 results about "TRPV1" patented technology

Tobacco products comprising smokeless tobacco products and active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel are disclosed. Nicotine replacement therapies comprising active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel. The active ingredient may reduce or eliminate sensory irritation arising due to use of the product. Analgesic compositions comprising active ingredients. Methods of reducing taste and sensory irritation by employing an active ingredient.

The invention relates to a composition with moisturizing, soothing and repairing effects and application thereof. The composition with the moisturizing, soothing and repairing effects comprises a pomelo fruit extract, a capparis spinosa fruit extract and hydroxyphenyl propionamide benzoic acid. Three active components, namely the pomelo fruit extract, the capparis spinosa fruit extract and the hydroxyphenyl propionamide benzoic acid, are creatively combined for use, wherein the pomelo fruit extract can inhibit release of inflammatory factors, reduce ultraviolet-induced DNA damage and inflammatory response, neutralize free radicals and reduce oxidative stress damage; wherein the capparis spinosa fruit extract can quickly moisturize, enhance cell viability and promote enhancement of a skin barrier; wherein hydroxyphenyl propionamide benzoic acid can block symptoms such as skin redness and swelling, pruritus and pain caused by the fact that histamine activates a TRPV1 pathway. The three components are matched with one another, have a synergistic effect in the aspects of moisturizing, relieving the skin and repairing the skin barrier, and have an excellent effect when being applied to cosmetics with related effects.

The invention discloses an antioxidant repairing composite composition containing a picea norvegensis leaf extract and a preparation method thereof, and relates to the field of skincare products, the picea norvegensis leaf extract, leontopodium alpinum and citrus fruit extract are used as main materials, and the picea norvegensis leaf extract and leontopodium alpinum can play a role in the whole pathway of Nrf2 and NF-kappa B, so that the antioxidant repairing composite composition has the advantages that the antioxidant repairing composite composition is free of toxic and side effects; and the citrus fruit extract can inhibit the activation of TRPV1 and relieve the discomfort of the sensitive skin, so that the composition not only can improve the skin barrier of the sensitive skin, but also can inhibit the activity of the TRPV1, and the TRPV1 can be activated only by breaking the barrier and damaging the barrier under the two actions, so that the skin barrier can be well repaired. And the vicious circle of barrier injury can be aggravated by the excessive activation of the TRPV1, so that the stabilization and repair of the skin are realized, and the emulsion provided by the invention has a relatively good DPPH clearance rate and relatively good oxidation resistance.

The invention provides a compound for regulating and controlling a TRPV1 ion channel. The structural formula of the compound is as shown in formula I. The invention also provides application of the compound in preparation of a medicine for regulating and controlling the TRPV1 ion channel. The invention provides a pharmaceutical composition with an anti-inflammatory effect, the pharmaceutical composition comprises the compound, and pharmaceutically acceptable auxiliary materials or auxiliary components are added to prepare a pharmaceutically common preparation. Compared with azobenzene, the compound has the advantages that the illumination wavelength is increased, the illumination wavelength is 660 nm, a TRPV1 targeted photosensitizer is used, a channel is activated by using a low-energy near-infrared light'precise key ', depth, safety and reversibility are considered, and the anti-inflammatory effect of the compound is obvious.

A method of producing a population of mature human pluripotent stem cell-derived sensory neurons (hPSC-SNs) expressing a target gene associated with at least one of nociceptive pain, chronic pain, pruriception and a nociceptive- or pruriceptive- mediated condition, the method comprising introducing into a population of human pluripotent stem cells (hPSCs) a composition comprising at least one site-directed nuclease targeting a site within the target gene, and at least one nucleic acid comprising a nucleotide sequence encoding at least one screenable, selectable marker that is flanked by (i) a nucleotide sequence homologous with a region located upstream of the target site within the target gene and (ii) a nucleotide sequence homologous with a region located downstream of the target site within the target gene, wherein the target site is located downstream of the open reading frame of the target gene, and wherein the site-directed nuclease cleaves the target site of the target gene and the nucleic acid encoding the screenable, selectable marker is inserted at the target site; covering said population of hPSCs under an extracellular matrix comprising at least one neuronal differentiation driver to produce a sensory committed neural crest population; contacting said sensory committed neural crest population with at least one neuronal differentiation driver and at least one neurotrophic factor to produce a population of early sensory neurons (SNs); and contacting said population of early SNs with at least one neurotrophic factor to produce a population of mature hPSC-SNs expressing at least one of SN marker or one pan neuronal marker; isolating the cells expressing the at least one screenable, selectable marker, wherein said population of mature hPSC-SNs expressed said one target gene associated with nociceptive pain, chronic pain, pruriception a nociceptive- or pruriceptive- mediated condition, and wherein said population of mature hPSC-SNs responds to a nociceptive and pruriceptive stimulus.

The present application discloses a compound of formula (I), compositions comprising said compound, and a method of using said compound as a cannabinoid receptor ligand in the treatment or prevention of diseases associated with a cannabinoid receptor, such as, CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR119, TRPV1, TPRV2, PPARγ or a μ-opioid receptor.

Compounds represented by Formula I: (I) wherein A, B, W, V, Z, Ra, Rb, n and m are as defined in the instant specification, or by Formula la, lb, III, IV or V, as defined in the instant specification, and uses thereof in modulating an activity of a voltage-dependent potassium channel and / or a TRPV1 channel and in treating a medical condition associated with an activity of these channels, such as medical conditions associated with neuronal hyper-excitability, are provided.

This application provides a barrier-repairing composition and its use. The composition comprises panthenol, niacinamide, folic acid, and cobalamin in a mass ratio of 3-7:1-5:0.0005-0.1:0.00005-0.01. This application also provides uses of the composition and products containing the same. The composition utilizes panthenol, niacinamide, folic acid, and cobalamin in combination, where the components complement and enhance each other, achieving a synergistic effect in upregulating BMAL2 gene expression. This enhances the DNA damage repair capacity of skin fibroblasts and potentially promotes barrier repair. Furthermore, the composition provided herein can significantly reduce the expression of capsaicin receptor 1 (TRPV1) and increase the expression of involucrin, PIEZO1, and TNXB, reducing skin discomfort and enhancing skin barrier function. Furthermore, the composition provided herein can reduce the expression of inflammatory factors, demonstrating its anti-inflammatory effect.

The application discloses a composition with soothing anti-inflammatory anti-wrinkle firming efficacy and a preparation method thereof, and the composition comprises a TRPV1 inhibitor, an extract of Glycyrrhiza inflata Bat., palmitoyl tripeptide-1 and palmitoyl tetrapeptide-7. The four raw materials are compounded to have a synergistic effect, reduce the release of pro-inflammatory mediators and inhibit the high reactivity of nerve fibers to achieve soothing anti-inflammatory and anti-irritation; promote the generation of self collagen and sodium hyaluronate, reduce the oxidative stress response to achieve the anti-wrinkle firming efficacy and delay skin aging. The composition has comprehensive effects in soothing, anti-inflammatory, anti-irritation, anti-oxidation, anti-wrinkle and firming, reduces the generation of inflammation and delays skin aging, relieves the burning and stinging sensation of the skin at the same time, and meets the requirements of safety and high efficiency pursued by sensitive skin groups.

The present application relates to the technical field of asiatic acid, and particularly relates to an asiatic acid derivative and a preparation method.The asiatic acid derivative provided by the present application has R which is a straight chain or a branched chain with 1-24 carbon atoms, or a saturated or unsaturated monohydric alcohol alkyl formed by removing a hydroxyl group.The R group of the asiatic acid derivative of the present application has higher water solubility and oil solubility, especially oil solubility, so that the asiatic acid derivative has obviously enhanced liposolubility compared with asiatic acid, is easily dissolved in natural oil, alkane and other ester solvents, and has obviously enhanced biological activity, so that the asiatic acid derivative of the present application has high availability, improves the inhibition effect of the asiatic acid derivative on EDNRA and TRPV1, and further improves the anti-tumor effect, and the asiatic acid derivative has no safety risk.

The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure and an application of the TRPV1 / URAT1 dual inhibitor. The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure, and the structural formula of the TRPV1 / URAT1 dual inhibitor is as follows: # imgabs0 #. The compound is unique and novel in structure, a preparation method of the compound is researched and provided, the compound has high inhibitory activity as a TRPV1 / URAT1 dual inhibitor, IC50 to TRPV1 is smaller than or equal to 100 nM, IC50 to URAT1 is smaller than or equal to 1 mu M, and inhibitory activity IC50 to an hERG channel is larger than 30 mu M; the traditional Chinese medicine composition has an excellent treatment effect on hyperuricemia, gout, inflammatory pain and the like, also has a better analgesic effect, and can be used as an analgesic medicine, a medicine for treating gout or hyperuricemia and the like.

The present invention relates to antibodies that bind to TRPV1. The present invention also relates to certain epitopes of the protein TRPV1. The present invention also relates to immunoconjugates and compositions comprising such antibodies. The present invention also provides methods of producing such antibodies. The present invention further provides the use of such antibodies for therapeutic purposes, for example in the treatment of pain.

Disclosed herein is a novel pharmaceutical composition for treating pain, wherein the pharmaceutical composition targets a transient receptor potential vanilloid 1 (TRPV1) receptor and acts as an antagonist.

The application belongs to the technical field of genetic engineering, and relates to a gene editing method for enhancing low-temperature tolerance of fish by targeting a trpv1 gene and application. The application precisely edits a fish trpv1 gene by using CRISPR-Cas9 technology, blocks negative signal transduction induced by low temperature, and releases the inhibition on related metabolic pathways. The application provides a brand-new molecular target for improvement of low-temperature tolerance of fish and cold-resistant breeding of aquatic products, and has important application value.

This application relates to the field of molecular biology, and in particular to a screening method for TRPV1 agonists and its application. The provided screening method includes: obtaining transcriptome gene sequences from the coral *Dipsastraea rotumana* for functional annotation analysis, followed by classification to obtain transcriptome data; performing sequence alignment and phylogenetic tree construction on the transcriptome data to identify polypeptide sequences highly homologous to existing TRPV1 agonists; performing three-dimensional modeling of the polypeptide sequences to obtain the polypeptide 3D structure; and sequentially performing molecular docking and molecular dynamics analysis on the polypeptide 3D structure and the TRPV1-3D structure to screen for TRPV1 agonists. This method is highly efficient and low-cost, with high efficiency and accuracy; it facilitates the application of TRPV1 agonists in the preparation of products for treating neuroinflammation, providing new ideas and solutions for the treatment of neurodegenerative diseases.

The application discloses a sciaenops ocellatus TRPV1 inhibiting peptide, a preparation method and application, belongs to the polypeptide field, and the amino acid sequence of the sciaenops ocellatus TRPV1 inhibiting peptide is RLF.The sciaenops ocellatus TRPV1 inhibiting peptide, the preparation method and the application take the skin of sciaenops ocellatus as starting raw material, and the amino acid sequence of the sciaenops ocellatus TRPV1 inhibiting peptide is successfully obtained through a specific process.Experiment verification shows that the prepared sciaenops ocellatus TRPV1 inhibiting peptide shows excellent inhibiting effect on TRPV1.The inhibiting peptide can be used for preparing a TRPV1 antagonist, the antagonist can play an anti-inflammatory regulation role through multiple channels, and can effectively down-regulate skin microvascular hyperreactivity.

This invention belongs to the field of biomedical technology, specifically relating to a peptide targeting TRPV1 and its applications. A peptide targeting TRPV1 has the amino acid sequence shown in SEQ ID NO.1. The peptide also includes a mutant obtained by amino acid scanning mutation based on the sequence shown in SEQ ID NO.1. The amino acid sequence of the mutant is shown in any one of SEQ ID NO.2-16. This peptide is used to prepare formulations that block or inhibit TRPV1 activity. This invention provides a peptide targeting TRPV1 and its applications. Through a strategy combining artificial intelligence screening and structural prediction, SEQ ID NO.1 was successfully identified and its mechanism of action was elucidated. Experimental results show that SEQ ID NO.1 and its mutants exhibit excellent analgesic activity and good safety both in vitro and in vivo, demonstrating significant clinical application potential.

This invention provides the application of a cyclic dipeptide in inhibiting the TRPV1 protein, wherein the cyclic dipeptide is a cyclic (D-leucine-L-proline) dipeptide. This invention also relates to the application of the cyclic dipeptide in the preparation of topical skin agents or pharmaceuticals with TRPV1 protein inhibitory activity, wherein the topical skin agent is selected from: creams, lotions, gels, toners, serums, masks, eye creams, aerosol cleansing foams, sprays, shower gels, or facial cleansers.

The invention discloses prevention and treatment of diseases by stimulating TRPV1 + sensory nerves. Specifically, the invention discloses application of a substance for stimulating TRPV1 + sensory nerves in preparation of products for prevention, treatment or adjuvant treatment of inflammatory diseases, autonomic nerve dysfunction diseases or adrenal insufficiency diseases, and application of the substance for stimulating TRPV1 + sensory nerves in preparation of products for inhibiting proinflammatory cytokines and products for promoting anti-inflammatory cytokines. The TRPV1 ion channel agonist disclosed by the invention can obviously and effectively inhibit the expression of numerous proinflammatory cytokines and obviously improve the expression of anti-inflammatory cytokines IL10, so that not only is the physiological status of an inflammatory mouse obviously improved, but also the survival rate of the inflammatory mouse is obviously improved; meanwhile, the spleen function can be adjusted, expression of spleen pro-inflammatory genes is remarkably inhibited, generation of catecholamine is increased, and secretion of cortisol hormones is promoted. The invention has wide clinical application value in prevention and treatment of related diseases.

To provide a novel TRPV1 activator.SOLUTION: Provided is a TRPV1 activator containing Brazilian green propolis and culifolin as active ingredients.SELECTED DRAWING: None

The present application belongs to the field of biological medicine, and relates to an in-situ spraying particle-gel composite as well as a preparation method and application thereof. The present application prepares a drug-loaded particle-gel composite material, which can be rapidly gelled in-situ in the form of spraying. In a wound infection model of diabetic rats, the composite material exhibits good photothermal activation TRPV1 channel-mediated local analgesia, as well as anti-inflammatory, antibacterial, antioxidant, hemostatic and wound healing-promoting multifunctional therapeutic effects. Through in-vitro and in-vivo material characterization, as well as histopathological examination of animal experiments, it is confirmed that the composite gel material has good biological safety and degradability, and is a local anesthetic biomaterial preparation which is expected to be clinically transformed for chronic wound analgesia and healing-promoting therapeutic effects.

The invention discloses a rapid detection kit for zebra fish cell capsaicin receptor activation. The rapid detection kit comprises an RNA purification column and an RNA collection tube or an RNA capture plate, washing buffer solutions A and B, a DNase I digestive juice, a 5x reverse transcription premix solution, a 2x SYBR Green qPCR premix solution, and specific primer dry powder or premix solution. The invention also discloses an application of the kit. The invention also discloses a method for screening a compound or a substance for regulating and controlling the activation of the capsaicin receptor of the zebra fish cell by using the kit. The novel primer sequence provided by the invention can accurately reflect the activation state of the TRPV1 pathway; a large number of samples can be processed in parallel through plate type design and reagent premixing, and the screening efficiency is improved by dozens of times; meanwhile, a receptor gene and a downstream early response gene are detected, so that an activation event can be confirmed, indirect evidence of pathway activity can be provided, and the result is more convincing.

The invention discloses application of isotoosendanin in preparation of a medicine for relieving neuropathic pain and application of TRPV1 and Nav1.7 as medicine targets of the isotoosendanin, and relates to the technical field of biological medicine. The medicine prepared from the isotoosendanin can inhibit the expression of dorsal root ganglion (DRG) neurons TRPV1 and Nav1.7 protein; the medicine prepared from the isotoosendanin can inhibit the reduction of mechanical pain threshold and crymodynia threshold; the neuropathic pain comprises pain after selective injury of sciatic nerve branches; the TRPV1 and Nav1.7 are used as drug targets to be applied to preparation of the neuropathic pain relieving drug taking the isotoosendanin as an effective component. The isotoosendanin plays a role in relieving neuropathic pain, and the isotoosendanin can be used for inhibiting the expression of TRPV1 and Nav1.7; the isotoosendanin can be used for treating neuropathic pain by inhibiting expression of TRPV1 and Nav1.7 channel proteins, and a new thought is provided for preparing the neuropathic pain medicine.

This TRPA1 activity inhibitor is characterized by containing glycyrrhizic acid or a salt thereof as an active ingredient. This TRPV1 activity inhibitor is characterized by containing glycyrrhizic acid or a salt thereof as an active ingredient. By using glycyrrhizic acid or a salt thereof as an active ingredient, a TRPA1 activity inhibitor and a TRPV1 activity inhibitor with excellent action and effect can be provided.

The invention discloses streptomyces coronatoxin DB-2408, a metabolite of the streptomyces coronatoxin DB-2408 and application of the streptomyces coronatoxin DB-2408 to preparation of a medicine for treating non-small cell lung cancer, and belongs to the technical field of biological medicine. The invention provides a streptomyces coronatoxin DB-2408. The streptomyces coronatoxin DB-2408 can produce schizoxanthomycin through metabolism. Experiments prove that the compound can highly selectively inhibit a TRPV1 channel, calcium influx is reduced by 28%, and experimental results prove that the compound is low in toxicity under effective concentration and has the survival rate gt of cells with low expression of TRPV1; the compound has the activity of inhibiting the non-small cell cancer, provides a novel broad-spectrum treatment strategy for the NSCLC, and has a wide and good market application prospect.

The invention discloses a new application of isopentadecanoic acid, and discloses an application of isopentadecanoic acid in preparation of skin care cosmetics, isopentadecanoic acid has the effects of up-regulating expression of hBD-2 and silk protein in human immortalized keratinocytes, reducing expression synthesis of ROS and TRPV1 in the human immortalized keratinocytes, inhibiting release of NO by mouse macrophages, and inhibiting expression of the human immortalized keratinocytes. And the secretion of sebaceous gland cell grease is reduced.

The application discloses a capsaicin stimulation inhibitor for cosmetics and a preparation method and application thereof. The preparation method of the capsaicin stimulation inhibitor for cosmetics comprises the following steps: A, soaking medicinal materials with 15-20 times weight of extraction solvent for 2-16 hours to obtain a soaking solution; the extraction solvent is an alkali aqueous solution with a concentration of 0.2-0.8 mol / L, and the medicinal materials are at least one of calendula, spade heron and radix scrophulariae; B, extracting the soaking solution at 95-105 DEG C for 1-3 hours. The capsaicin stimulation inhibitor for cosmetics prepared by the preparation method can significantly inhibit the secretion of IL-1 alpha of keratinocytes and the expression of TRPV-1 protein caused by capsaicin stimulation, and the combinations have certain synergies, so that the capsaicin stimulation inhibitor for cosmetics can be applied to the inhibition of TRPV1 expression induced by capsaicin, the inhibition of IL-1 alpha secretion induced by capsaicin and the preparation of skin external preparation.

The present invention provides novel pharmaceutical compositions and methods for the treatment and / or prevention of social disorders such as autism spectrum disorder, fragile X syndrome, and / or autism spectrum disorder-like symptoms. Specifically provided are: a compound represented by formula (I) (in the formula, R1 represents a substituted or unsubstituted alkyl group; r2 is a hydrogen atom or the like; a is N or the like; the dashed line represents the presence or absence of a bond; r3 represents a substituted or unsubstituted alkyl group or the like; m is 0 or 1; and R4 and R5 are each independently a hydrogen atom or the like) or a pharmaceutically acceptable complex thereof for the treatment and / or prevention of social disorders. # imgabs0 #

The application discloses a soothing and anti-allergic composition and a preparation method and application thereof. The soothing and anti-allergic composition comprises the following components in parts by weight: sea salt 0.001-5.0 parts; hydrolyzed seaweed extract 0.001-3.0 parts; Illicium micranthum leaf extract 0.001-5.0 parts; and polysaccharide 0.001-1.0 part. The soothing and anti-allergic composition is composed of sea salt containing rich mineral elements, hydrolyzed seaweed extract capable of promoting blood circulation, Illicium micranthum leaf extract capable of inhibiting TRPV1 expression and polysaccharide capable of improving skin activity. The sea salt, the polysaccharide, the Illicium micranthum leaf extract and the hydrolyzed seaweed extract have a synergistic effect, and can achieve unexpected effects of instant soothing and continuous alleviation of allergic symptoms.

Provided is stimulation of TRPV1+ and / or TRPA1+ sensory nerves for the prevention and treatment of diseases. Particularly provided is use of a substance for stimulating TRPV1+ and / or TRPA1+ sensory nerves in the prevention or treatment of inflammatory diseases, dysautonomia, or adrenal insufficiency, and in inhibiting the generation of pro-inflammatory cytokines and promoting the generation of anti-inflammatory cytokines. A TRPV1 and / or TRPA1 ion channel agonist can significantly effectively inhibit the expression of numerous pro-inflammatory cytokines and significantly improve the expression of the anti-inflammatory cytokine IL10, significantly improving both the physiological state and the survival rate of mice with inflammation. Moreover, the agonist can adjust spleen function, significantly inhibit the expression of pro-inflammatory genes in the spleen, increase the generation of catecholamine, and promote the secretion of cortisol-like hormones. The agonist has wide clinical application value for the prevention and treatment of related diseases.