22 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 invention relates to a novel type of compounds which modulate the activity of Abscisic Acid (ABA) receptors in plants. More particularly, such novel compounds are acting as ABA antagonists, which specifically and potently block activation of clade III ABA receptors including but not only PYL1, while another subfamily of compounds has agonistic mode of action promoting activation of the receptor and the ABA signaling pathway. These compounds are, therefore, applicable in different fields of modulating target plant seed germination, modulating target plant growth, modulating tolerance to drought and abiotic stress, modulating fruit ripening, or modulating immunity of a target plant. More particularly, said compounds can be used to stimulate the germination of plant seeds, either under conditions favorable for the growth of crop plants, or unfavorable for the survival of weeds. The compounds can also be used to enhance plant growth under growing conditions where water is not a limiting factor on plant growth. The selectivity of the compounds for clade III ABA receptors will prevent unwanted effects from blocking other ABA receptor subtypes (for example in clade II and clade I groups) present in the plants of interest. The present invention also provides corresponding agrochemical compositions comprising such novel compounds.

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.

TIFF2025538048000094.tif34115 The present invention relates to novel compounds of formula (I), wherein P, Q, A, B, m, n, R 1 , R 2 and R 3 are defined as in Formula (I); which are negative allosteric modulators of metabotropic glutamate receptor subtype 7 (mGlu7) and are useful for treating or preventing neurological, otic, and psychiatric disorders associated with glutamate dysfunction, and disorders involving the mGlu7 subtype of metabotropic receptor. The present invention is also directed to pharmaceutical compositions comprising such compounds, processes for preparing such compounds and such compositions, and the use of such compounds for the prevention or treatment of neurological, otic, and psychiatric disorders involving mGlu7.

The present disclosure relates to compositions and methods for treating a maladapted stress response involving the corticotropin-releasing factor receptor subtype 2 (CRFR2), such as myalgic encephalomyelitis / chronic fatigue syndrome or an impairment of the musculoskeletal or the nervous system, resulting in measurable symptom improvement.

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.

Novel compounds which selectively target the nicotinic acetylcholine receptor (nAChR) α9, α10, and α7 subunits are provided. Substituted dialkylpiperazinium compounds, both with and without chiral switches, were identified as potent agonists exhibiting selectivity for human nAChRs containing α9 and α9α10 subunits over nAChRs containing α7 subunits. Chiral analogs demonstrated a preference for selectivity towards one receptor subtype over the other. The compounds can be used as α9- and α7-specific therapeutics for pain management. The compounds also exhibit inhibition of ATP-induced interleukin-1β release in THP-1 cells, indicating anti-inflammatory properties.

The application belongs to the field of neurobiology and pain treatment, and particularly relates to application of a GluK1 receptor agonist in preparation of a drug for treating chronic pain. The GluK1 receptor agonist is ATPA or a pharmaceutically acceptable salt or solvate thereof. The application finds that, under a chronic pain state, kainate receptor-mediated synaptic plasticity in an anterior cingulate cortex (ACC) is significantly impaired, and is manifested as loss of long-term depression ability, and selective activation of a kainate receptor subtype GluK1 can reverse the abnormality. After chronic pain, GluK1 expression in the ACC is up-regulated, and activation of GluK1 by using a GluK1 receptor agonist ATPA has a significant therapeutic effect on neuropathic pain and inflammatory pain. The results show that, targeted activation of GluK1 can produce an analgesic effect by restoring the homeostasis of synaptic plasticity in the ACC, and the GluK1 receptor agonist can be used for treating chronic pain.

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.

TIFF2025538049000047.tif38119 The present invention relates to novel compounds of formula (I), wherein P, Q, A, B, m, n, R 1 , R 2 and R 3 are defined as in Formula (I); which are negative allosteric modulators of metabotropic glutamate receptor subtype 7 (mGlu7) and are useful for treating or preventing neurological, otic, and psychiatric disorders associated with glutamate dysfunction, and disorders involving the mGlu7 subtype of metabotropic receptor. The present invention is also directed to pharmaceutical compositions comprising such compounds, processes for preparing such compounds and such compositions, and the use of such compounds for the prevention or treatment of neurological, otic, and psychiatric disorders involving mGlu7.

The present disclosure concerns the novel compounds 3α-ethyl-3β-hydroxy-5α-androstan-17-one and 3α-ethyl-3β-hydroxy-5α-androstan-17-one, the medical use thereof and in particular use in the treatment of diseases and disorders associated with an α3 subtype of the GABAA receptor, for example 5 treatment of obesity, hyperphagia disorder, Prader-Willi's syndrome, polycystic ovarian syndrome, and / or diabetes. Said disclosure is also concerned with reducing and / or preventing overweight. Additionally, related pharmaceutical and cosmetic compositions are disclosed as well as treatment against alcoholism and substance abuse.

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.

TIFF2025538047000051.tif32114 The present invention relates to novel compounds of formula (I), wherein P, Q, A, B, m, n and R 1 are defined as in Formula (I); which are negative allosteric modulators of metabotropic glutamate receptor subtype 7 (mGlu7) and are useful for treating or preventing neurological, otic, and psychiatric disorders associated with glutamate dysfunction, and disorders involving the mGlu7 subtype of metabotropic receptor. The present invention is also directed to pharmaceutical compositions comprising such compounds, processes for preparing such compounds and such compositions, and the use of such compounds for the prevention or treatment of neurological, otic, and psychiatric disorders involving mGlu7.

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).