46 results about "GABA receptor" patented technology

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and / or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

Methods for using pesticidal compositions containing a pesticidally acceptable carrier, at least one GABA receptor modulator compound as a pesticidally active ingredient and optionally an additional compounds, such as a synergist, and methods for using same.

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and / or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

The present invention provides for a method for inducing sterility in fish by administering at least one compound that disrupts the establishment of the gonadotropin-releasing hormone system during early development thereby inhibiting sexual maturity in the treated fish. Effective compounds include GABA, GABA receptor agonists, or GABA receptor antagonists.

The present invention relates to compositions for treating insomnia or sleeplessness. The compositions of the present invention comprise jujube extract and at least one of white peony extract, radix polygala extract, and passion flower extract. The extracts used in the compositions of the present invention bind strongly to GABA receptors and work synergistically to shorten the time needed to fall asleep and to improve the quality of sleep by reducing awakenings during sleep and increasing the duration of sleep.

The present invention relates to the use of cannabidiol (CBD) in the treatment of patients with childhood-onset epilepsy who are concurrently taking one or more antiepileptic drugs that works via GABA receptor agonism. Preferably the AED is stiripentol. Preferably the CBD used is in the form of a highly purified extract of cannabis such that the CBD is present at greater than 98% of the total extract (w / w) and the other components of the extract are characterised. In particular the cannabinoid tetrahydrocannabinol (THC) has been substantially removed, to a level of not more than 0.15% (w / w) and the propyl analogue of CBD, cannabidivarin, (CBDV) is present in amounts of up to 1%. Alternatively, the CBD may be a synthetically produced CBD.

The present invention relates to a method of preventing or treating in a subject a disorder characterized in a reduced GABA receptor function by administering to the subject a therapeutically effective amount of a pharmacologically active blood serum product obtainable by a method comprising electrostimulation of a non-human animal, withdrawal of blood from said animal isolation of serum from said blood, and gamma irradiation of said serum.

The invention provides the use of a non-steroid compound which acts on the GABA receptor for the treatment of disorders relating to reduced neurosteroid activity. The non-steroid compounds may be GABA agonists, GABA uptake inhibitors or enhancers of GABAergic activity.

The present invention relates to novel compounds having a positive allosteric GÀBAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). A compound of the general formula I

The present invention provides for a method for inducing sterility in fish by administering at least one compound that disrupts the establishment of the gonadotropin-releasing hormone system during early development thereby inhibiting sexual maturity in the treated fish. Effective compounds include GABA, GABA receptor agonists, or GABA receptor antagonists.

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.

The present invention relates to compositions and methods relating to the characterization and function of GABRR2. Specifically, the present invention provides transgenic animals and methods of treating disease states or conditions in which the GABRR2 is implicated. The present invention also provides agents and method of identifying agents that modulate GABRR2. Such agents may be useful in treating and preventing conditions associated with pain.

The present invention relates to compositions for treating insomnia or sleeplessness. The compositions of the present invention comprise extracts of white peony root and in particular comprise paeoniflorin, either alone or in combination with at least one of jujube extract, radix polygala extract, and passion flower extract. The compositions of the present invention bind to GABA receptors and work synergistically to shorten the time needed to fall asleep and to improve the quality of sleep by reducing awakenings during sleep and increasing the duration of sleep.

Embodiments of the disclosure include methods and compositions related to treatment of one or more medical conditions with one or more negative modulators of GABAA receptors. In specific embodiments, depression and / or suicidability is treated or ameliorated or prevented with one or more negative modulators of GABAA receptors, such as a partial inverse agonist of a GABAA receptor comprising an alpha5 subunit.

The present invention relates to the use of cannabidiol (CBD) in the treatment of patients with childhood-onset epilepsy who are concurrently taking one or more antiepileptic drugs that works via GABA receptor agonism. Preferably the AED is stiripentol. Preferably the CBD used is in the form of a highly purified extract of cannabis such that the CBD is present at greater than 98% of the total extract (w / w) and the other components of the extract are characterized. In particular the cannabinoid tetrahydrocannabinol (THC) has been substantially removed, to a level of not more than 0.15% (w / w) and the propyl analogue of CBD, cannabidivarin, (CBDV) is present in amounts of up to 1%. Alternatively, the CBD may be a synthetically produced CBD.

The invention provides new 1H-quinolin-4-one compounds of formula (I), wherein R1, R2, R3, R4 and R5 have different meanings, and pharmaceutically acceptable salts and hydrates thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds.

The present invention relates to compositions for treating insomnia or sleeplessness. The compositions of the present invention comprise jujube extract and at least one of white peony extract, radix polygala extract, and passion flower extract. The extracts used in the compositions of the present invention bind strongly to GABA receptors and work synergistically to shorten the time needed to fall asleep and to improve the quality of sleep by reducing awakenings during sleep and increasing the duration of sleep.

The human body is mediated by a large number of chemicals and chemical processes where imbalances can result in abnormal conditions affecting part or all of the human body. Artificial drugs addressing specific diseases by targeting specific chemical imbalance(s) and / or process(es). For example, tofactinib is a JAK-STAT signaling pathway inhibitor beneficial for treating autoimmune diseases whilst baclofen acts as an agonist of GABA receptors. However, these are each prescribed in oral form leading to reduced efficacy or absorption by other regions of the patient. Accordingly, the inventor has established alternate dosing formats such a topical creams allowing local direct application allowing specific targeted delivery to the appropriate region of the patient's body as well their use, in the instances of tofactinib and baclofen, for the treatment of other diseases or conditions.

The present invention relates to a method of treatment of Parkinson's disease, and to the use of antisense oligonucleotides or triplex oligonucleotides introduced into targeted brain structures to decrease the function of brain circuits known to be overactive in the Parkinsonian brain. Antisense or triplex oligonucleotides are targeted to the internal globus pallidus and / or substantia nigra pars reticulata (SNr) where the expression of glutamic acid decarboxylase (GAD67, GAD65, or a combination of the two isoforms) is downregulated. The present invention also relates to a method of treatment of Parkinson's disease where antisense or triplex oligonucleotides are targeted to the internal globus pallidus and / or substantia nigra pars reticulata for the downregulation of glutamate receptors. The present invention further relates to a method of treatment of Parkinson's disease where antisense or triplex oligonucleotides are targeted to the thalamic motor nuclei for the downregulation of GABA receptors.

The invention relates to an affinity chromatography medium for separating and purifying a GABA receptor and a preparation method thereof. The technological process comprises the following steps: carrying out chemical modification on fipronil to obtain an affinity ligand; by taking agarose gel as a matrix, after activating by an epoxy activating agent, coupling the fipronil affinity ligand to obtain an affinity medium; packing the affinity medium so as to be used for separating and purifying fish GABA receptor protein. The affinity chromatography medium synthesized according to the invention has the advantages of being good in selectivity, strong in specificity, high in mechanical strength and good in separation effect; in addition, the preparation process is simple and the magnifying is easy.

A buccal lozenge containing the extracts of Chinese-medicinal amterials is prepared from 10 Chinese-medicinal materials including chrysanthemum flower 15-20 wt.%, pueraria root 15-20 wt%, black plum 5-10 wt%, Chinese olive 3-5 wt%, etc. through decocting in water, filtering, concentrating, adding lactose and granulated sugar, mixing, drying, breaking, adding flavouring, granulating and tabletting. Its advantages are high nutritive value and high effect on limiting absorption to alcohol and protecting liver, stomach and cardiac blood vessel.

The invention belongs to the field of preparation of cell membrane surface GABA receptor fluorescent probes, relates to application of coumarin derivatives as cell membrane surface GABA receptor fluorescent probes, in particular to a targeted cell membrane surface GABA receptor fluorescent probe and a preparation method and application thereof. The structural formula of the fluorescent probe is shown in the specification. The probe is easy to synthesize, high in yield, capable of quickly targeting receptors of corresponding cell membranes, good in specificity, high in signal-to-noise ratio andcapable of targeting the cell membranes for a long time. In a confocal imaging experiment, the probe can well target a GABA receptor on the surface of the cell membrane.

The present invention relates to the field of GABA receptor structure and function. In one aspect, the present invention relates to impairment of the gamma-aminobutyric acid (GABA) receptors in parasitic nematodes, for the purpose of crop protection and / or soil treatment. The invention includes mutated nematode GABA receptor subunits, nematode GABA neuromuscular junction receptor complexes, nucleic acids which encode the mutated and functional receptor complexes, antibodies which selectively bind the GABA receptor complexes and / or subunits, and assays for compounds which adversely affect nematode GABA neuromuscular junction receptor function. The present invention therefore relates broadly to recombinant DNA technology, molecular biology tools, and crop protection and / or soil treatment.

The invention discloses a nutritional composition containing a GABA receptor stimulant and a CB1 receptor stimulant, and a preparation method thereof. The nutritional composition comprises the GABA and the CB1 receptor stimulant in a mass ratio of 100: (3-40), and the sum of the mass of the GABA receptor stimulant and the mass of the CB1 receptor stimulant is not lower than 47% of the total mass of the nutritional composition. The preparation method comprises the following steps: uniformly mixing the components in proportion, and then filling, tabletting or filling. The invention also provides application of the nutritional composition in preparation of medicines and health-care products for relieving anxiety, relieving difficulty in falling asleep, improving sleep quality and / or treating fatigue, anxiety, hypomnesis, slow response and reduced motility caused by insomnia and mental stress, and application in oral preparations.

The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones with at least one substituent on the 4-pyridinyl ring having the chemical structure of formula I: The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula I in to modulate GABA and GABA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and / or GABA receptors.

The present invention provides an isolated GABAB receptor protein comprising at least one GABABR1a subunit and at least one GABABR2a subunit, characterized in that said GABAB receptor has one high affinity agonist binding site and one low affinity agonist binding site. In particular the isolated recombinant GABAB receptor protein expressed by the hGABABR1a / GABABR2 CHO cell line deposited at the Belgian Coordinated Collections of Microorganisms (BCCM) as CHO-K1 h-GABA-b R1a / R2 clone on Aug. 22, 2003 with the accession number LMBP 6046CB. It is thus an object of the present invention to provide the hGABABR1a / GABABR2 CHO cell line deposited at the Belgian Coordinated Collections of Microorganisms (BCCM) as CHO-K1 h-GABA-b R1a / R2 clone on Aug. 22, 2003 with the accession number LMBP 6046CB. The invention also provides the use of the aforementioned cell line in a method to identify GABAB receptor agonists using a functional or a binding assay. In particular in a radioligand-binding assay comprising the use of radiolabeled agonists such as for example 3H-GABA or 3H-baclofen. In a particular embodiment the present invention provides the use of the aforementioned GABAB receptor in a method to identify a high affinity GABAB receptor agonist using a functional or a binding assay. In particular in a radioligand-binding assay comprising the use of radiolabeled agonists such as for example 3H-GABA or 3H-baclofen. Alternatively, the aforementioned binding assays are performed on cellular extracts, in particular cellular membrane preparations of the aforementioned cells.

The present invention relates to the field of GABA receptor structure and function. In one aspect, the present invention relates to impairment of the gamma-aminobutyric acid (GABA) receptors in parasitic nematodes, for the purpose of crop protection and / or soil treatment. The invention includes mutated nematode GABA receptor subunits, nematode GABA neuromuscular junction receptor complexes, nucleic acids which encode the mutated and functional receptor complexes, antibodies which selectively bind the GABA receptor complexes and / or subunits, and assays for compounds which adversely affect nematode GABA neuromuscular junction receptor function. The present invention therefore relates broadly to recombinant DNA technology, molecular biology tools, and crop protection and / or soil treatment.

The present invention relates to applications of intestinal flora in preparation of drugs for treatment of depression caused by Dcf1 deficiency. According to the present invention, the manure of the Dcf1 knockout mouse model and the normal mouse model are detected by 16S rRNA gene sequencing, the difference between the intestinal flora compositions of the Dcf1 knockout mouse model and the normal mouse model is compared, and the results show that the intestinal flora compositions of the Dcf1 knockout mouse model and the normal mouse model are different, the normal mouse model transplanted withthe manure of the Dcf1 knockout mouse model shows the depression-like behavior, the depression-like behavior of the Dcf1 knockout mouse model being subjected to bifidobacteria and lactobacillus intragastric administration treatment can be released, and the contents of Glu, GABA and GABA receptors in the brain of the mouse models transplanted with the flora are changed, such that the change in theintestinal flora of the Dcf1 knockout mouse model can induce the depression-like behavior, and can cause the imbalances of neurotransmitters such as Glu and GABA and the dysfunction of GABA receptorsso as to involve the occurrence of depression.

The present invention relates to novel compounds having a positive allosteric GÀBAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). A compound of the general formula I.