14 results about "Receptor subtype" patented technology

The invention relates to the technical field of medicines, in particular to application of a neuropeptide Y1 receptor antagonist in preparation of a hereditary polycystic kidney disease treatment medicine. The neuropeptide Y1 receptor antagonist is selected from a compound BIBO3304 which plays a role in blocking combination of neuropeptide Y (NPY) and a Y1 receptor subtype thereof. On the basis that early-stage histopathology, high-throughput sequencing, cytobiology and molecular biology are combined with in-vitro cell culture and in-vivo animal experiments, the potential treatment effect of the neuropeptide Y1 receptor antagonist in preparation of hereditary polycystic kidney disease treatment drugs is provided, and a new basis is provided for hereditary polycystic kidney disease treatment.

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 invention relates to the technical field of medicinal chemistry, in particular to a 2-methyl-2-azabicyclo [3.2. 1] octane derivative which has a structure as shown in a general formula I or a general formula II or pharmaceutically acceptable salt, solvate, hydrate, isomer or prodrug of the 2-methyl-2-azabicyclo [3.2. 1] octane derivative, and a preparation method and application of the 2-methyl-2-azabicyclo [3.2. 1] octane derivative. As an acetylcholine receptor agonist, the compound shows high activity and high selectivity to M3 receptor subtypes. In-vitro experiments show that under the concentration of 40 mu M, the receptor excitation rate of the compound (such as 9a, 10a and the like) exceeds 95%, and is obviously superior to that of a positive control drug Aceclidine (48.65%). Due to the characteristic, the compound can generate a powerful pupil contraction pinhole effect by efficiently exciting an eye iris M3 receptor so as to improve near vision, and meanwhile, stimulation to ciliary muscles and related side effects are expected to be reduced due to high selectivity of the compound.

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.

1,1'-Biphenyl-4-yl-(het)arylimino-λ6-sulfanone compounds are 5-HT2A receptor activators, and these compounds and their pharmaceutical compositions are useful for the treatment of neurological or psychiatric disorders.

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.

The present invention relates to halogenated somatostatin analogs with selectivity for multiple somatostatin receptor subtypes and pharmaceutical compositions comprising the same. Moreover, the present invention relates to said halogenated somatostatin analogs and pharmaceutical compositions for use in therapy and / or diagnosis, for example in the treatment and / or diagnosis of diseases (e.g., cancer such as a neuroendocrine cancer) that are characterized by a high expression (e.g., overexpression) of one or more somatostatin receptor subtypes (e.g., somatostatin receptor 2 (SST2) and / or somatostatin receptor 5 (SST5)).

The present invention relates to novel compounds of Formula (I'), wherein P, Q, A, B, m, n, R1, R2, R9, R10, R11 and R12 are defined as in Formula (I'). These compounds may be useful asmuscarinic M4 receptor subtype ("M4-mAChR") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with muscarinic M4 receptor dysfunction and diseases in which the M4 receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases such as for example, cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders modulated by M4 muscarinic receptors.

A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof. The compounds have activity against multiple histamine receptor subtypes, including for example histamine H1 and H4.

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).