102 results about "TRPV1" patented technology

Compositions are provided that contain a TRPV1 agonist, such as capsaicin, and a solvent system. Topical application of the composition results in rapid delivery of agonist to the dermis and epidermis. Method of using the compositions for reducing nociceptive nerve fiber function in subjects, and for treatment of capsaicin-responsive conditions are also provided.

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 present invention relates to the use of cannabinoid-containing plant extracts in the prevention or treatment of diseases or conditions that are alleviated by blockade of one or more types of TRP channel. Preferably the subset of TRP channel that is blockaded is the TRPA channel. More preferably the TRPA channel is the TRPA1 channel. Preferably the diseases or conditions to be prevented or treated include: neuropathic pain, inflammation or vasoconstriction. Alternatively the TRP channel that is blockaded is the TRPM channel. More preferably the TRPM channel is the TRPM8 channel. Preferably the diseases or conditions to be prevented or treated are cancer. More preferably the cancers to be treated include: cancer of the prostate, cancer of the breast, cancer of the colon, cancer of the lung or cancer of the skin. Alternatively the TRP channel that is blockaded is the TRPV channel. More preferably the TRPV channel is the TRPV1 channel. Preferably the diseases or conditions to be prevented or treated include neuropathic pain, inflammation or vasoconstriction.

The methods and compositions of the present invention are directed to the treatment or amelioration of muscle cramps using a composition that includes one or more TRPV1 channel activators, and / or one or more TRPA1 channel activators, and / or one or more ASIC channel activators.

Described here are drug delivery devices including an occlusive backing layer and a drug depot containing a TRPV1 agonist and a non-hydrophilic solvent. The drug depot may take various forms, such as an adhesive polymeric matrix, liquid reservoir, or microreservoir droplets. Methods of making and using the drug delivery devices are also described.

The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

Methods of inhibiting ischemia-related and ischemia-reperfusion-related injury are provided. Remote administration of a C-fiber activator or TRPV1 agonist or remote electrical stimulation and activation of TRPV1 reduces ischemia-related tissue damage in subjects at risk for ischemia-related tissue damage. In aspects of the invention, remote application of a TRPV1 agonist inhibits ischemia-related cardiac tissue damage. Methods of inhibiting cardiac tissue damage by topically administering the TRPV1 agonist, capsaicin are provided.

The invention relates to compounds shown as a general formula (1) and salts of the compounds. The compounds are TRPV1 (transient receptor potential cation channel, subfamily V, member 1) antagonists, and have better analgesic action. The invention also relates to a preparation method for the compounds, medicinal preparations containing the compounds, and application of the compounds and medicinal compositions thereof in treatment of pain.

The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

Disclosed herein are methods for increasing analgesic potency of TRPV1 antagonists, said methods comprise of repeated administration of the TRPV1 antagonists in a subject. Methods for treating or preventing pain by repeated administration of a TRPV1 antagonist are also discussed.

The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

A magnetic nanoparticles including a TRPV1 agonist, as well as methods of preparation and use, are described herein. A magnetically responsive pharmaceutical can include a core region having a magnetic nanoparticle (MNPs) and a TRPV1 protein agonist. Further, an exterior coating comprising a polymer can be formed around the core region. The magnetically responsive pharmaceutical can be administered to a recipient and directed to a target region using an external magnetic field.

A compound represented by formula (I′):(wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

This disclosure relates to multifunctional formulations, methods of manufacture and methods of use of natural topical and oral compositions to treat various dermatitis and pruritus conditions in mammals. In particular, this disclosure relates to a multifunctional topical pharmaceutical composition effective to treat dermatitis and associated pruritus comprising at least one natural plant extract TRPV1 antagonist, at least one natural plant extract is a TRPA1 antagonist, and a carrier. Also, in particular, this disclosure also relates to a multifunctional method to treat histamine induced and non-histamine dermatitis and associated pruritus in mammals from one or more of non-atopic and atopic dermatitis (AD), contact dermatitis, allergenic contact dermatitis (ACD), psoriasis, eczema, infestations, urticarial, nociceptive, neuropathic, neurogenic, psychogenic pruritus comprising treating with a composition comprising at least one natural plant extract TRPV1 antagonist, at least one natural plant extract is a TRPA1 antagonist, and a carrier.

The invention discloses a lactobacillus casei strain Qian (CCTCC No. M2013514) working leavening agent product and an intestinal tract regulating health use thereof. The lactobacillus casei strain Qian working leavening agent product and a downstream product thereof are relatively strong in acid resistance, are 62.51+ / -7.35% in survival rate after being treated for 3 hours in artificial gastric juice with pH of 3.0, and are capable of slowly growing in 1.0% cholate, wherein the growth efficiency is 7.86+ / -0.45% that in non-cholate cultivation; the hydrophobic property of lactobacillus casei strain Qian cells is up to 51.30+ / -4.28%, and the lactobacillus casei strain Qian working leavening agent product normally grows in human intestinal tract. The lactobacillus casei strain Qian working leavening agent product can be used for slowing down mouse weight reducing trend caused by constipation, shortening dark stool defecating time, increasing a small intestine advance rate, reducing the gene expression level of mouse TRPV1. NOS, reducing the defecation quantity, and reducing defecation granule number and excrement moisture content reducing trend, achieves similar effects of constipation drugs and shows a certain constipation prevention effect.

An object of the present invention is to find a novel pharmacological action of a urea compound having a structure represented by the general formula [I]. The urea compound having a structure represented by the general formula [I] or a salt thereof has an excellent therapeutic effect on a TRPV1-mediated disease. In the formula, A represents a lower alkylene group or a lower alkenylene group; R1 represents a hydrogen atom, an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and R2 and R3 are the same or different and represent a hydrogen atom or a lower alkyl group which may be substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group, or an aryl group.

Described herein are drug delivery devices comprising a occluded liner and a drug depot comprising a TRPVl agonist and a non-hydrophilic solvent. The depot can take different forms, such as a viscous polymer matrix, a liquid reservoir, or microreservoir droplets. Methods of making and using the drug delivery device are also described.

The invention relates to the technical field of medicines and cosmetics, and discloses a polysaccharide composition for inhibiting a TRPV1 pathway as well as a preparation method and application of the polysaccharide composition. The polysaccharide composition comprises saussurea involucrata polysaccharide, tremella polysaccharide, dendrobium polysaccharide and salvia miltiorrhiza polysaccharide,wherein the concentration of the saussurea involucrata polysaccharide is not higher than 0.4 mg / mL, the concentration of the dendrobium polysaccharide is not higher than 0.35 mg / mL, the concentrationof the tremella polysaccharide is not higher than 0.2 mg / mL, and the concentration of the salvia miltiorrhiza polysaccharide is not higher than 0.2 mg / mL. The polysaccharide composition disclosed by the invention can effectively inhibit the expression of the TRPV1 pathway so as to pre-protect and repair a skin nerve barrier, and can be used in preparation of related cosmetics and medicines for preventing and treating skin allergy.

The invention belongs to the technical field of pharmacy, particularly discloses a benzylpiperazine urea TRPV1 antagonistic and MOR agonistic double-target drug as well as a preparation method and application thereof, and particularly relates to a compound in a general formula (I) and pharmaceutically acceptable salts thereof, and the drug can be used for preventing and / or treating diseases related to TRPV1 and / or MOR activity, such as pain, inflammation, immune dysfunction, neurological and psychiatric disorders, respiratory diseases, urinary and reproductive disorders. the invention also relates to a preparation method of the compounds and a pharmaceutical preparation containing the compounds.

A compound represented by formula (I′):(wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

In organic sulfur compounds, dialkyl amino dithiocarbamate alkyl ester plays a very important role. Researches show that dialkyl amino dithiocarbamate alkyl ester and the derivatives thereof have widebiological characteristics and pharmacological activity. For example, many studies show that the dialkyl amino dithiocarbamate alkyl ester has various activities, including anti-proliferative, anti-glaucoma, antibacterial, antifungal, breast cancer treatment and cholinesterase inhibition activities, and can be used as a myocardial imaging agent. It is known that dialkyl amino dithiocarbamate alkyl ester and the derivatives thereof can be taken as inhibitors of HIV-1 NCp7, antiviral agents, and non-flavonoid TRPV1 antagonists. Dialkyl amino dithiocarbamate alkyl ester has a wide application range, and is massively produced in the world. The invention provides a method for efficiently synthesizing dialkyl amino dithiocarbamate alkyl ester. Under the catalysis of CuI, a chiral quaternary ammonium salt and a dialkyl amino dithioformate are used for C-S cross coupling for the first time, and dialkyl amino dithiocarbamate alkyl ester is prepared. The target product is further converted andcoupled with brominated aromatic hydrocarbons to obtain high-purity enantiomer chiral thioethers. The synthesis process has the advantages of mild reaction conditions, wide universality, no toxicity or danger, high yield, wide substrate range and the like.