8 results about "Receptor subtype" patented technology

The present application relates to endogenous NMDA receptor subtypes in brain tissue and their assembly and structure. The present application provides a method for evaluating the function of endogenous NMDA receptors in brain tissue (cortex and hippocampus), comprising obtaining data on the structure and / or quantity of endogenous NMDA receptors (NMDAR) in the brain tissue, wherein the NMDA receptor comprises a GluN1-N2A-N2B triheteromer; and comparing the structure and / or quantity of the GluN1-N2A-N2B triheteromer with a reference structure and / or quantity reference value, thereby giving an evaluation result of the function of endogenous NMDA receptors in brain tissue. The present application also provides a device for performing the evaluation and a method for drug screening based on changes in the structure and / or quantity of specific NMDA receptors.

The present application relates to a compound represented by the general formula (I) (where all symbols represent the same meanings as those described in the specification) or a pharmaceutically acceptable salt thereof, which is useful as an EP4 agonist, and in particular, which has EP4 agonist activity, is selective to other PGE receptor subtypes, and has a low risk of toxicity to the circulatory system, and thus is useful as an active ingredient for preventing and / or treating diseases associated with the EP4 receptor.

The present application relates to compounds of Formula (I), wherein P, Q, A, B, m, n, R1, R2 and R3 are defined as in Formula (I) which are negative allosteric modulators of the metabotropic glutamate receptor subtype 7 (mGlu7) and which are useful for the treatment or prevention of neurological, ear and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGlu7 subtype of metabotropic receptors is involved. The application is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological, ear and psychiatric disorders and diseases in which mGlu7 is involved.

An N-formamidopyrazoline derivative is a compound having General Formula (I) or an enantiomer, a diastereomer, an epimer and a racemate thereof, or a pharmaceutically acceptable salt thereof. The compound is an antagonist of a ligand-gated non-selective cation channel receptor subtype P2X3, and can be used for treating or preventing various diseases mediated by the receptor P2X3.

This invention pertains to the field of inflammatory bowel disease and relates to a quaternary ammonium salt-based locally acting sphingosine 1-phosphate receptor subtype 1 agonist. The compounds, their stereoisomers, and pharmaceutically acceptable salts of this application are locally acting S1PR1 agonists. These compounds exhibit good agonistic activity against sphingosine 1-phosphate receptor subtype 1, are almost not absorbed orally, and have low oral bioavailability. However, they still possess good in vivo anti-ulcerative colitis activity, improving intestinal inflammatory damage in mice with ulcerative colitis, increasing mouse weight, and increasing colon length. Therefore, these compounds, while maintaining in vivo anti-ulcerative colitis activity, can reduce the risk of infection caused by systemic immunosuppression. The structural formula of the sphingosine 1-phosphate receptor subtype 1 agonist is shown in Formula I.

This application relates to a 7α-substituted piperazine morphine derivative, its preparation method, and its uses. Specifically, it relates to 7α-(N-substituted piperazine)-tetrahydrothebaine derivatives as shown in general formula (I) or pharmaceutically acceptable salts thereof, and their preparation methods. Furthermore, it relates to the use of such derivatives in the preparation of analgesic, anti-irritable bowel syndrome, antipruritic, anti-addictive, and antidepressant drugs. The derivatives described in this invention exhibit significantly enhanced κ-receptor agonist activity and κ-receptor subtype selectivity.

The present invention belongs to the field of inflammatory bowel diseases, and relates to a locally acting quaternary ammonium salt-type sphingosine-1-phosphate receptor subtype 1 agonist. The compounds of the present application, and stereoisomers thereof and pharmaceutically acceptable salts thereof are locally acting S1PR1 agonists. The compounds exhibit a good agonistic activity against sphingosine-1-phosphate receptor subtype 1, are hardly absorbed upon oral administration, and have a low oral bioavailability, but still have a good in-vivo activity against ulcerative colitis. The compounds are capable of ameliorating intestinal inflammatory injuries in mice with ulcerative colitis, increasing mouse body weight, and increasing mouse colon length. Therefore, the compounds can reduce the risk of infection caused by systemic immunosuppression while maintaining an in-vivo anti-ulcerative colitis activity. The sphingosine-1-phosphate receptor subtype 1 agonist has a structural formula represented by formula (I).

Described herein are methods of treating, ameliorating and / or preventing a stress-related disorder in a subject in need thereof. The method, in certain embodiments, includes administering to the subject a therapeutically effective amount of a selective β-adrenergic receptor antagonist compound. In certain embodiments, the compound has a larger dissociation constant (pKD) for the β1-adrenergic receptor subtype (β1-AR) than for the β2-adrenergic receptor subtype (β2-AR) and / or β3-adrenergic receptor subtype (β3-AR).