41 results about "Dopamine receptor D1" patented technology

The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

The invention provides a new method of treating diseases or conditions characterized by reduced dopamine D1 receptor signaling activity, such as Parkinson's disease, depression, and cognitive impairment of schizophrenia, comprising administering an effective amount of a 1,3,5,-substituted, 6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one to a patient in need thereof.

This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant.

The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.

The present invention relates to a long-acting sustained-release dosage form for treatment of Parkinson Disease, comprising a dopamine receptor agonist and a pharmaceutically acceptable biodegradable polymer accessories, wherein the content of the dopamine receptor agonist in the sustained-release dosage form is 5-50% by weight, and the content of the pharmaceutically acceptable polymer accessories is 50-95% by weight.

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and / or on the cAMP pathway.

The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

The invention features combinations of dopaminergic agents and analgesic agents useful for treating pain. In particular, the combinations feature a low ratio of dopaminergic agent to analgesic agent. The dopaminergic agent can be an agonist of the dopamine receptor D1-like family or the dopamine receptor D2-like family. Such combinations potentiate analgesia to 1) alleviate acute pain, 2) prevent the transition from acute pain to chronic pain, and 3) manage chronic pain.

The present invention provides a panel of at least five clinical analyses or tests (using serum samples) to determine the risk of pediatric acute-onset neuropsychiatric syndrome (PANS) and / or pediatric autoimmune neuropsychiatric disorder associated with streptococcal infection (PANDAS) in an individual. These include enzyme linked immunosorbent assays (ELISAs) to measure antibody titers against neuronal antigens present in the brain; the neuronal antigens include lysoganglioside, tubulin, dopamine receptor D1, dopamine receptor D2, serotonin receptor 5HT2A, and serotonin receptor 5HT2C. Antibody titers against at least four of these neuronal antigens are required in the present methods; preferably antibody tiers against all of these neuronal antigens are measured. A final assay is used to quantify calcium / calmodulin-dependent protein kinase activity using a neuronal cell line. The results of these analyses or tests are then combined using an algorithm to determine whether a PANS or PANDAS diagnosis is appropriate for the individual. Depending on the diagnosis, an appropriate treatment can be determined.

The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.

The present invention relates to novel functionally selective ligands of dopamine D2 receptors, including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.

The invention belongs to the field of pharmacy, relates to medicinal use of an indole piperazine derivative, and in particular relates to appetency of the indole piperazine derivative to dopamine D3 receptor and 5-HT1A and 5-HT2A receptors, function characteristics and use in preparation of medicines for nervous system disease; adrenergic beta-2 receptor crystal structure is used as a template for the construction of a dopamine 5-HT1A receptor model; by accuracy verification on the receptor model and molecular dynamics simulation, a flexible receptor conformation can be obtained; active sites of the flexible receptor conformation can be detected; detection results are superimposed and a dynamic receptor effective-mass model is constructed; an existing compound database is screened and the activity is tested; and results show that the screened compound FDFWHF003 and its derivatives have good activity to the dopamine receptor and 5-HT receptors, can be used for preparation of anti-schizophrenia medicines, and especially is suitable for the preparation of medicines for treating schizophrenia caused by dopamine system and 5-HT system functional disorders.

The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.

The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula IwhereinAr is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and / or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description;X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2;Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond;E is CH2 or NR3;R1 is H, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl;R1a is H, C1C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl,R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3;R3 is H or C1C4-alkyl;R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring;R6 and R7 independently of each other are H or halogen;and the physiologically tolerated acid addition salts thereof.

The invention belongs to the field of pharmacy, relates to medicinal use of an indole piperazine derivative, and in particular relates to appetency of the indole piperazine derivative to dopamine D3 receptor and 5-HT1A and 5-HT2A receptors, function characteristics and use in preparation of medicines for nervous system disease; adrenergic beta-2 receptor crystal structure is used as a template for the construction of a dopamine 5-HT1A receptor model; by accuracy verification on the receptor model and molecular dynamics simulation, a flexible receptor conformation can be obtained; active sites of the flexible receptor conformation can be detected; detection results are superimposed and a dynamic receptor effective-mass model is constructed; an existing compound database is screened and the activity is tested; and results show that the screened compound FDFWHF003 and its derivatives have good activity to the dopamine receptor and 5-HT receptors, can be used for preparation of anti-schizophrenia medicines, and especially is suitable for the preparation of medicines for treating schizophrenia caused by dopamine system and 5-HT system functional disorders.

The present invention relates to a long-acting sustained-release dosage form for treatment of Parkinson Disease, comprising a dopamine receptor agonist and a pharmaceutically acceptable biodegradable polymer accessories, wherein the content of the dopamine receptor agonist in the sustained-release dosage form is 5-50% by weight, and the content of the pharmaceutically acceptable polymer accessories is 50-95% by weight.

The invention provides a new method of treating diseases or conditions characterized by reduced dopamine D1 receptor signaling activity, such as Parkinson's disease, depression, and cognitive impairment of schizophrenia, comprising administering an effective amount of a 1,3,5,-substituted, 6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one to a patient in need thereof.

The invention provides a method for inducing retina to generate and release dopamine and activate a dopamine receptor D1. The method for controlling the wave length of a light ray irradiating to the retina, the power of the light ray irradiating to the retina, time gaps of the light ray irradiating to the retina and a space region of the light ray irradiating to the retina is used to achieve the aim of inducing cells on the retina to generate and release the dopamine for inhibiting shortsightedness and amblyopia development to achieve the treating aim. The invention also provides an instrumentof treating the shortsightedness and the amblyopia, and the instrument at least comprises a base, a control unit and an Internet of Things unit so that it can be achieved that treatment of the shortsightedness and the amblyopic is remotely controlled.

The invention discloses a fluoride-18 marked dopamine D4 receptor developing agent and a preparation method thereof. The fluoride-18 marked dopamine D4 receptor developing agent is 2-[4-(4-[<18>F] fluorobenzyl) piperazine-1-yl methyl] pyrazolo [1, 5-alpha] pyridine, and the structural formula of the developing agent is shown in a formula (I). The preparation method comprises three steps of: step one, reacting pyrazolo [1, 5-alpha] pyridine-2-formaldehyde with N-formoxyl piperazine to generate 2-[4-piperazine formaldehyde-1-yl methyl) pyrazolo [1, 5-alpha] pyridine; step two, hydrolyzing 2-[4-piperazine formaldehyde-1-base methyl) pyrazolo [1, 5-alpha] pyridine under a strong acidic condition to generate 2-[4-piperazine-1-yl methyl) pyrazolo [1, 5-alpha] pyridine; and step three, reacting 2-[4-piperazine-1-yl methyl) pyrazolo [1, 5-alpha] pyridine with 4-[<18>F] fluorobenzaldehyde to generate a target molecule. 2-[4-(4-[<18>F] fluorobenzyl) piperazine-1-yl methyl] pyrazolo [1, 5-alpha] pyridine prepared by the method can be used for dopamine D4 receptor development and is a specific dopamine D4 receptor developing agent.

The present invention provides compounds, compositions and methods for inhibiting D2R-DISC1 interaction. Specifically, the present invention provides a polypeptide comprising the amino acid sequence KIYIVLRRRRKRVNT (SEQ ID NO: 1) or SEQ ID NO:5, a fragment thereof, or a polypeptide comprising an amino acid sequence that is at least 80% identical to SEQ ID NO: 1 or 5, or a fragment thereof, wherein the polypeptide is not a naturally occurring dopamine receptor. Also provided is a method of identifying an agent that inhibits the interaction of D2R with DISC1, a method of identifying an agent that binds to the polypeptide sequence defined by SEQ ID NO: 1 or 5, and a method of inhibiting D2R interaction with DISC1 in a mammal comprising administering an agent that inhibits the interaction of D2R with DISC1 to the mammal.

The invention relates to flavanone derivatives, and preparation method and use thereof, particularly relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for preventing or treating a mental disorder or a nervous system disease. The compound of the invention exerts significant activity of inhibiting microglial activation and neuroinflammation, can antagonize dopamine D2 receptor, improve the ethological change in multiple animal models for mental disorders, effectively inhibit neuroinflammation and demyelination, and can be used to prevent or treat a mental disorder and a nervous system disease.

The invention provides an application of a partial agonist of a dopamine (DA) D2 receptor to preparation of drugs for inhibiting myopia and a using method of the partial agonist. The application and the using method have the beneficial effects that the functions of the DA D2 receptor in myopia are stabilized by applying the partial agonist aripiprazole of the DA D2 R; aripiprazole has the effect of inhibiting lengthening of vitreous cavities and oculi axes in the form deprivation myopia process, thus inhibiting formation of experimental myopia of animals.

The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R6 and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.