32 results about "TRPV1" patented technology

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.

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.

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 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.

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 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.

The invention discloses an application of a circium japonicum extract in preparation of cosmetics with an instant skin soothing effect, and the circium japonicum extract can quickly and remarkably reduce the calcium ion influx level in cells, inhibit the activity of TRPV1 and reduce the content of TRPV1, so that the instant soothing effect is achieved, and discomfort symptoms such as skin sensitivity, redness and stabbing pain are relieved. In addition, the invention further provides that an extracting agent in the preparation process of the circium japonicum extract has an influence effect on the instant relieving effect of the circium japonicum extract, and the instant relieving effect of the circium japonicum extract is optimized by selecting the extracting agent.

The application relates to the cosmetic technical field, and particularly discloses a water-oil balance composition suitable for sensitive skin and application thereof. The components in a suitable mass ratio range are matched with each other, so that the temperature-sensitive receptors of the skin can be synergistically regulated, natural moisturizing production is promoted, and ultraviolet protection is improved. The water-oil balance composition can selectively inhibit TRPV1-mediated 5alpha-reductase activity and ultraviolet-induced oxidative stress under high temperature in summer, accurately regulate sebum secretion without damaging the barrier, and promote the generation of natural moisturizing factors by activating filaggrin degradation in a low-temperature environment in winter, dynamically adjust the hydration degree of the stratum corneum, break through the technical limitations of traditional products, such as seasonal use and single and one-sided functions of active ingredients, realize cross-seasonal balanced care of a single formula, and are mild and non-irritating, and are suitable for sensitive skin.

Provided herein are methods of stabilizing blood pressure in severe sepsis / septic shock and other types of distributive shock using TRPV1 agonists. Also provided are pharmaceutical formulations for increasing blood pressure in septic shock the formulation including at least one TRPV1 agonist in a dosage form for parenteral administration, wherein the TRPV1 agonist is selected from capsaicin, daphnane TRPV1 agonists, vanillotoxin, N-oleoyl dopamine, N-arachidonyl dopamine, BrP-LPA, and derivatives and analogues thereof. Also provided are TRPV1 agonists co-lyophilized with adrenergic agonists and / or angiotensins in a dosage form for reconstitution and parenteral administration.

The invention discloses a new application of schizonepeta fordii vesicles, which is realized through in-vitro cells, and proves that the schizonepeta fordii vesicles can obviously reduce the expression of TNF-alpha and NF-kappa B inflammatory factors of macrophages, reduce the expression of TRPV1 of keratinocytes, increase the expression of LOR and FLG of the keratinocytes and reduce the expression of SREBP-1 and ACC of sebaceous gland cells. The schizonepeta tenuifolia vesicle has the advantages that the schizonepeta tenuifolia vesicle has obvious soothing, repairing, oil control and tightening effects and can be applied to a skin care product with at least one of soothing, repairing, oil control and tightening effects, and accordingly the schizonepeta tenuifolia vesicle can be applied to skin care products with at least one of soothing, repairing, oil control and tightening effects by the aid of the schizonepeta tenuifolia vesicle.

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

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 an alkyl group formed by removing a hydroxyl group from a saturated or unsaturated monohydric alcohol, and the saturated or unsaturated monohydric alcohol includes one of ethanol, octanol, hexadecanol, stearyl alcohol, 2-hexyl-1-decanol, decyltetradecin, oleyl alcohol, cis,cis-9,12-octadecadienol and bisabolol. 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, is easily soluble in natural oil, alkane and other ester solvents, and has a significant inhibitory effect on EDNRA and TRPV1 and obviously enhanced bioactivity. The asiatic acid derivative of the present application has high availability, and the asiatic acid derivative has no safety risk.

The invention discloses application of TRPV1, NUDT9 and MT-ND5 as targets in preparation and screening of drugs for treating brain glioma, and belongs to the technical field of biology. According to the application disclosed by the invention, experiments prove that the expression of NUDT9 and MT-ND5 in brain glioma cells is knocked down, the proliferation of the brain glioma cells is reduced, TRPV1 in the brain glioma cells is knocked down, the proliferation of the brain glioma cells is promoted, the expression of NUDT9 and MT-ND5 in the brain glioma cells is reduced by beta-elemene, and the beta-elemene has the effect of inhibiting tumor growth; the application prospect of the TRPV1, the NUDT9 and the MT-ND5 serving as the target spot in screening the medicine for treating the brain glioma is shown. According to the application disclosed by the invention, the condition that the beta-elemene and the TMZ are combined to enhance DNA damage accumulation through a synergistic effect, continuously activate a cell apoptosis pathway and increase the sensitivity of glioma cells to the TMZ is determined for the first time, so that the curative effect is improved, and the toxicity is reduced.

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

The invention relates to the technical field of biological medicines, and particularly provides a magnetocaloric nanoparticle for targeted activation of a cell membrane TRPV1 as well as a preparation method and application of the magnetocaloric nanoparticle. According to the preparation method, after the surface of FeNPs is modified with PEGylated long-circulating lipid DSPE-PEG2000 molecules, a special extracellular TRPV1 monoclonal antibody is added, and the FeNPs-TRPV1 particles are obtained through an ammonia carboxylic acid reaction. The FeNPs-TRPV1 particles provided by the invention have a magnetic-thermal conversion effect, FeNPs are accurately sent to the periphery of TRPV1 on the surface of a cell membrane through an extracellular TRPV1 monoclonal antibody, an extracellular TRPV1 channel is activated through heating of an alternating magnetic field, calcium ions are caused to flow inwards, nociceptive neural signals of myocardial ischemia reperfusion injury are regulated and controlled, and the myocardial ischemia reperfusion injury is effectively relieved.

The application provides a recombinant collagen IV and a preparation method and application thereof, and belongs to the technical field of bioengineering; based on part of active amino acid sequences in a natural human collagen IV alpha 5 chain as a basic monomer, a recombinant collagen IV sequence with repair and soothing effects is designed, and a recombinant expression vector is provided based on this, and a recombinant engineering bacterium is constructed; it is verified through experiments that the recombinant collagen IV can improve TGM1 expression, reduce TRPV1 expression, has cell adhesion activity and cell migration activity, the product has high HPLC purity, does not cause an immune response when applied to a human body, and has the value of being applied to the fields of cosmetics, medicines, health products, medical devices and biological materials.

The present application relates to the field of medicinal chemistry and pharmacotherapy, in particular to a phenylpiperazine compound or a pharmaceutically acceptable salt thereof, a preparation method and use thereof in the preparation of analgesic drugs or drugs for treating pain, wherein the phenylpiperazine compound or the pharmaceutically acceptable salt thereof has the following structure: the phenylpiperazine compound has obvious inhibitory activity on TRPV1, can obviously inhibit the pain response, and has no side effect of body temperature rise.

The present invention provides a new pharmaceutical composition and a method for treating and / or preventing social impairments such as autism spectrum disorder, fragile X syndrome, and / or autism spectrum disorder-like symptoms. Specifically, provided is a pharmaceutical composition for the treatment and / or prevention of social impairment, including a compound represented by Formula (I): wherein R1 is substituted or unsubstituted alkyl, R2 is a hydrogen atom or the like, A is N or the like, dashed lines indicate presence or absence of binding, R3 is substituted or unsubstituted alkyl or the like, m is 0 or 1, R4 and R5 are each independently a hydrogen atom or the like, or a pharmaceutically acceptable complex thereof.

The invention belongs to the technical field of biological medicine, and particularly relates to polypeptide targeting TRPV1 and application of the polypeptide. The amino acid sequence of the polypeptide is as shown in SEQ ID NO. 1 in a sequence table. The polypeptide further comprises a mutant obtained by performing amino acid scanning mutation on the basis of the sequence shown as SEQ ID NO.1 in the sequence table. The amino acid sequence of the mutant is shown as any one of SEQ ID NO.2-16 in a sequence table. The polypeptide is used for preparing a preparation for blocking or inhibiting TRPV1 activity. According to the TRPV1-targeting polypeptide and the application thereof provided by the invention, the SEQ ID NO.1 is successfully identified and the action mechanism of the TRPV1-targeting polypeptide is clarified through a strategy of combining artificial intelligence screening and structure prediction. Experimental results show that the SEQ ID NO.1 and the mutant thereof show excellent analgesic activity and good safety in vitro and in vivo, and have significant clinical application potential.

Provided herein are methods of producing a population of pluripotent stem cell-derived sensory neurons (PSC-SNs) expressing a target gene associated with pain. In addition, provided herein are compositions and methods comprising populations of pluripotent stems cells for treating pain, osteoarthritis, and osteoarthritis related conditions.

This invention relates to the field of pharmaceutical technology, disclosing the application of *Melastoma candida* polysaccharide in the preparation of drugs for the prevention or treatment of chronic urticaria. This invention is the first to discover that *Melastoma candida* polysaccharide can regulate immune homeostasis, inhibit inflammatory responses, improve skin lesions, and restore intestinal flora balance through multiple pathways. It also inhibits the overactivation of the NGF / TRPV1 / p38 signaling pathway, reduces neurogenic inflammation and mast cell-mediated responses, thereby alleviating the pathological process of chronic urticaria. This broadens the application scope of *Melastoma candida* polysaccharide and provides a new approach for the treatment of allergic skin-related diseases.

The application belongs to the field of pharmaceutical chemistry, and specifically discloses a TRPV1 agonist and a preparation method thereof. The structural feature of the TRPV1 agonist is that a OH or F substituent is introduced at the 3-position of a benzene ring of capsaicin, and the TRPV1 agonist is prepared by reacting vanillylamine hydrochloride and an acyl chloride compound with OH or F at the 3-position of the benzene ring. The reaction is carried out in a two-phase system composed of an aqueous solution of an inorganic base and an organic solvent at room temperature. The melting point of the TRPV1 agonist compound provided by the application is obviously improved, which is of great significance for developing capsaicin micro-powder type medicaments. The preparation method of the capsaicin derivative provided by the application uses a two-phase system composed of an aqueous solution of an inorganic base and an organic solvent for reaction, avoids the use of an organic base, and improves the selectivity of the acylation reaction.

The present disclosure relates to chemical compositions and methods for treating pain, including osteoarthritis pain. The composition comprises a group of TRPV1 ion channel modulator derivatives, including capsaicin derivatives, which can be covalently linked to a polymer. The disclosed TRPV1 ion channel modulator derivatives are covalently linked to a polymer, and alternatively or additionally, the ion channel modulator derivatives are mixed with a polymer. Also disclosed are methods of treating pain using the disclosed compounds via injection into or near a pain site. The disclosed compositions and methods are advantageous in that they exhibit sustained release of TRPV1 ion channel modulators, mitigate initial acute pain associated with TRPV1 modulators, and can be used at high concentrations, thereby effectively treating pain, including osteoarthritis knee joint pain.

The invention belongs to the technical field of biological medicine, and particularly relates to the field of gene therapy and pain therapy. The invention provides an sgRNA and AAV-CRISPRi virus system for targeted inhibition of TRPV1 gene, the AAV-CRISPRi virus system is a CRISPRi system based on AAV delivery, and the core functional structure sequence of the AAV-CRISPRi virus system is a 5 '-ITR inverted repeat sequence, an EF1 alpha core promoter, a ZIM3 transcription inhibition structural domain, a linker, a sadCas9-NLS nuclear localization signal-SV40 poly (A) termination signal-U6 promoter, and an sgRNA-3'-ITR inverted repeat sequence, according to the core functional structure, the miniaturization of a CRISPRi system is realized, and the infection success rate and the target gene inhibition efficiency are improved while the plasmid construction and AAV packaging costs are reduced. The AAV-CRISPRi virus system for targeted inhibition of the TRPV1 gene is used for preparing drugs for chronic pain, and has the characteristics of high efficiency, strong specificity and few side effects.

The present invention provides a composition having an action to enhance adrenomedullin gene expression. One or more embodiments of the present invention relate to a composition for enhancing adrenomedullin gene expression containing a TRPV1 agonist and a TRPA1 agonist as active ingredients. The TRPV1 agonist can be, for example, at least one selected from capsaicin, 6-shogaol, 6-gingerol and piperine. The TRPA1 agonist can be, for example, at least one selected from allyl isothiocyanate, cinnamaldehyde, diallyl disulfide, ASP7663 and oxylipin.