35 results about "TRPV1 receptor" patented technology

A personal care composition and method of using a personal care composition having menthol and/or hydrogen peroxide and a TRPA1 and/or TRPV1 receptor antagonists.

The present application is directed to compounds that are TRPV1 antagonists and have formula (I)

wherein variables Ar₁, L₁, R₁, R₂, R₃, R₄, R₅, Y₁, Y₂, and Y₃, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.

The invention relates to compounds of formulae I(a)-I(d):

and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof.

Compounds of formula (I)

wherein A, R₁, R₂, and R₃ are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.

The invention relates to applications of dragon's blood and a flavonoid chemical component thereof in serving as an antagonist of a capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) and in preparing a medicament for treating diseases related to TRPV1 receptors, wherein the flavonoid chemical component is cochinchinenin A or a mixture of at least two of cochinchinenin A, cochinchinenin B and loureirin B. The invention also relates to a medicinal composition comprising the dragon's blood and and the flavonoid chemical component thereof. Independent component of the dragon's blood or the cochinchinenin A, or a combination of every two of the cochinchinenin A, the cochinchinenin B and the loureirin B, or a combination comprising the cochinchinenin A, the cochinchinenin B and the loureirin B has strong capsaicin receptor TRPV1 activation inhibition effect and excellent pharmacological action based on the inhibition effect, so that the dragon's blood or the flavonoid chemical component thereof serving as an active component can be used for preparing medicaments for treating or preventing TRPV1 related diseases, such as nociceptive pains, neurogenic pains, cancer pains, headache, urinary bladder functional disorder, inflammation and the like.

The invention discloses a novel 4-(2-(pyrrolidine/piperidine-1-yl)benzyl)-piperazine urea type TRPV1 antagonist and a preparation method and application thereof. The invention relates to a compound ina general formula (I) and a pharmaceutically acceptable salt thereof, in the formula, n is equal to 1 or 2, R is H, F, Cl, Br, I, CF3, CH3 or OH, and Ar is phenyl or aromatic heterocyclic group. Thecompounds have a strong analgesic effect, the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC, almost no body temperature rise side effect exists, and theinvention further relates to the preparation method of the compounds and pharmaceutical preparations containing the compounds.

The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.

The invention relates to a 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole transient receptor potential vanilloid 1 (TRPV1) antagonist or a pharmaceutically-acceptable salt thereof. The structure generalformula is shown in the specifications, in the formula, R is H, or F, or Cl, or Br, or I, or CF3, or methyl, or isopropyl, or tertiary butyl, or cyclopropyl, or propenyl, or acetenyl, or hydroxyl, orphenoxyl, or acetyl or phenyl; n is 1, or 2 or 3; L is triazole, or tetrazole, or carbamido or thioureido; Ar is phenyl, or pyridyl, or isoquinolyl, or quinolyl or pyrimidyl. Through tests, it is found that 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole compounds have good TRPV1 inhibitory activity, and the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC;compared with the BCTC, the side effect of body temperature increasing is almost avoided. Therefore, the 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole compounds as shown in the general formula and medicinal salts thereof are safe and effective and have a high analgesic effect.

The invention provides a lactobacillus plantarum capable of relieving irritable bowel syndrome, which is characterized in that the lactobacillus plantarum is an AR495 strain and has been preserved in China General Microbiological Culture Collection Center (CGMCC) on March 22, 2017, and the preservation number is CGMCC No.14004. The lactobacillus plantarum is a lactobacillus plantarum strain. The lactobacillus plantarum AR495 can reduce the content of tryptase in intestinal tracts, alleviate the activation of mast cells, inhibit the activation of PAR2-TRPV1 receptors and recover a neuropathic pain threshold value, so that the IBS symptom is effectively improved, and the AR495 also can regulate the homeostasis of intestinal flora and improve the condition of dysbacteriosis.

Described is a transdermal ethosome composition for the treatment of pain. The transdermal ethosome composition comprises: an alcohol; a phospholipid; water; and a magnesium salt, a TRPV1 receptor agonist, or both a magnesium salt and a TRPV1 receptor agonist. The present compositions can be used to treat pain that is muscular, nociceptive or neuropathic in origin.

The invention discloses (S)-4/5-phenyl-2-(pyrrolidin-2-yl)thiazole novel TRPV1 antagonists as well as a preparation method and application thereof, and particularly relates to compounds represented bya general formula (I) or a general formula (II) and a pharmaceutically acceptable salt thereof. The compound have a strong analgesic effect, the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC, almost no body temperature rise side effect exists, and the invention further relates to a preparation method of the compounds and pharmaceutical preparationscontaining the compounds.

A method for screening compounds and compositions that reduce cetyl pyridinium chloride activation of TRPA1 receptor or TRPV1 receptor.

The invention provides a natural efficient anti-hair-loss hair restorer. A formula of the natural efficient anti-hair-loss hair restorer comprises cannabidiol crude oil, Morocco nut oil, frankincenseoil, tea tree oil, castor oil, bergamot oil and cannabis oil. Raw materials are weighed according to the formula, the raw materials are put into a mixing kettle to be stirred for 10-15 minutes at thetemperature of 35-39 DEG C to enable the raw materials to be in a homogenate state, still standing is conducted for two hours to obtain the natural efficient anti-hair-loss hair restorer, and bottlingis conducted by using a rubber head dropper tool. The natural efficient anti-hair-loss hair restorer is prepared by taking the cannabidiol crude oil as the main raw material, cannabidiol acts on receptors such as the CB1 receptor, the TRPV1 receptor and the 5-HT1A receptor in a human body, thus the activity of 5-alpha reductase is inhibited advantageously, androgen can be generated after the 5-alpha reductase is controlled to react with and testosterone in the human body, and thus the aim of treating alopecia is fulfilled by reducing the androgen level.

The invention relates to the field of medicine, specifically relates to the new application of ginsenoside Rf, and in particular relates to the application of the ginsenoside Rf serving as a TRPV1 antagonist. The antagonist ginsenoside Rf is capable of remarkably inhibiting TRPV1 protein expression at the cellular level, and at the animal level, is capable of remarkably prolonging the paw withdrawal latency of a rat induced by capsaicin (CAP) and reducing the degree of sensitivity of the rat to pain. As a result, the ginsenoside Rf can be used as the TRPV1 antagonist to ease pain with TRPV1 as the target spot, and also can be used for preparing analgesics for treating diseases related to a TRPV1 receptor.

TRPV1 antagonists and associated methods are provided. A TRPV1 channel antagonist can have the structure: Formula (I) wherein R₁ can be —CH₃, —(CH₂)_X(CH)_YCH₃ where x+y=1-20, an aromatic, a (CH₂)_n aromatic where n can be less than or equal to 6, a lipid, or a linker, and wherein R₂ can be either Formula (II) or Formula (III) Additionally, R₃ can be —O—R₄ or —NH—R₄ and R₄ can be —H, —CH₃, an ester, a cyclic ester, or an amide.

Disclosed is a method for preventing or treating atopic dermatitis using TRPV1 receptor antagonist. More specifically, it may be possible to prevent and/or treat the atopic dermatitis without any side effects such as an increase in body temperature, epidermal atrophy, and the like by percutaneously administrating a composition for external use on the skin containing the TRPV1 receptor antagonist.

The invention provides a virus overexpression vector and a cell containing the virus overexpression vector. The invention also provides a method for evaluating the pain-causing risk of a reagent or a product. The method comprises the following steps: (a) constructing the virus overexpression vector pCDH-CMV-Puro-hTRPV1 (SEQ ID NO:1); (b) infecting SH-SY5Y cells by using the virus overexpression vector pCDH-CMV-Puro-hTRPV1 (SEQ ID NO:1), and constructing a human TRPV1 receptor overexpression cell strain; (c) treating the human TRPV1 receptor overexpression cells through dihydrocapsaicin to establish a pain detection method; and (d) evaluating the pain-causing risk of the reagent or product to be detected by adopting the established pain detection method.

The invention discloses blood fat reducing effect of evodiamine. Evodiamine is capable of reducing blood fat through increasing human THP-1 macrophage cholesterol outflow, and cholesterol outflow regulation is realized through inhibition on ABCA1 protein degradation and activation of TRPV1 acceptor. The beneficial effects are that: new target points are provided for prevention and treatment of atherosclerosis, and a convenient approach is provided for further development of novel blood fat reducing medicines or health care products.

Provided herein are pharmaceutical compositions that comprise myrcene, optionally in admixture with cannabinoids and other terpenes, typically substantially free of THC and THCA, for targeting TRPV1 receptors. Also provided are methods of using the pharmaceutical compositions to desensitize TRPV1 receptors in order to treat pain, cardiovascular diseases such as cardiac hypertrophy, overactive bladder, and chronic cough.

The present disclosure is directed to methods of cleansing, decontaminating and/or treating an affected area (such as the mouth, skin, hair, fur, nose, one or both eyes or combinations thereof) of a subject that has been exposed to a chemical irritant such as a cyanocarbon, a capsaicin, an oleoresin Capsicum or a vanilloid which binds to a TRPV1 receptor by applying to the affected area (e.g., mouth, skin, hair fur, nose, one or both eyes or combinations thereof), a cleansing, decontaminating and/or effective amount of a composition that comprises at least one salt, at least one zwitterionic surfactant, at least one quaternary ammonium compound, at least one reducing agent and water to decontaminate the affected area.

Provided herein are compounds and pharmaceutical compositions useful for treating diseases or disorders mediated by the TRPV1 receptor. The present invention also provides methods for treating ocular diseases or disorders by administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a pharmaceutical composition described herein.

The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R¹ and R² are hydrogen etc., R³ is lower alkyl, R⁴ is lower alkyl or aryloxy, or R³ and R⁴ taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.