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36 results about "Dopamine transporter" patented technology
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The dopamine transporter (also dopamine active transporter, DAT, SLC6A3) is a membrane-spanning protein that pumps the neurotransmitter dopamine out of the synaptic cleft back into cytosol. In the cytosol, other transporters sequester the dopamine into vesicles for storage and later release. Dopamine reuptake via DAT provides the primary mechanism through which dopamine is cleared from synapses, although there may be an exception in the prefrontal cortex, where evidence points to a possibly larger role of the norepinephrine transporter.
GLP-1 receptor modulation of addiction, neuropsychiatric disorders and erectile dysfunction
InactiveUS20120021979A1Reducing a subject's dependence on an addictive substanceReduce chanceBiocideNervous disorderAddictive drugsTHC receptor
The present invention involves the use of GLP-1 and its analogs or GLP-1 receptor agonists to modulate dopamine transporter signaling. The implications of this ability include the use of MT-1 and its analogs or GLP-1 receptor agonists, such as exendin-4, to blunt behavioral response to addictive drugs, to decrease drug dependence, to prevent drug abuse relapse, and to treat brain disorders such as neuropsychiatric disorders including ADHD. The present invention also involves the use of GLP-1 and its analogs or GLP-1 receptor agonists to activate GLP-1R in penile tissue, such as for the treatment of erectile dysfunction either as a monotherapy or in combinations with other treatments, such as PDE 5 inhibitors.
Owner:VANDERBILT UNIV
Compositions and methods for the treatment of parkinson disease by the selective delivery of oligonucleotide molecules to specific neuron types
ActiveUS9084825B2Decrease in levelAvoid side effectsOrganic active ingredientsNervous disorderADAMTS ProteinsImaging agent
The invention provides a conjugate comprising (i) a selectivity agent which binds specifically to one or more neurotransmitter transporters selected from the group consisting of a dopamine transporter (DAT), serotonin transporter (SERT) or a norepinephrine transporter (NET) and (ii) a nucleic acid capable of specifically binding to a target molecule which is expressed in the same cell as the neurotransmitter transporter wherein said target molecule is α-synuclein or the mRNA encoding α-synuclein. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interest and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.
Owner:NLIFE THERAPEUTICS
Compositions and Methods for the Treatment of Parkinson Disease by the Selective Delivery of Oligonucleotide Molecules to Specific Neuron Types
ActiveUS20140120158A1Avoid side effectsDecrease in levelOrganic active ingredientsNervous disorderDiseaseImaging agent
The invention provides a conjugate comprising (i) a selectivity agent which binds specifically to one or more neurotransmitter transporters selected from the group consisting of a dopamine transporter (DAT), serotonin transporter (SERT) or a norepinephrine transporter (NET) and (ii) a nucleic acid capable of specifically binding to a target molecule which is expressed in the same cell as the neurotransmitter transporter wherein said target molecule is α-synuclein or the mRNA encoding α-synuclein. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interest and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.
Owner:NLIFE THERAPEUTICS
Sydnonimines-specific dopamine reuptake inhibitors and their use in treating dopamine related disorders
Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake.
Owner:CHEN HAO +3
Boat tropanes
InactiveUS7105678B2Useful in therapyRadioactive preparation carriersRadiation therapyRheniumEnantiomer
Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
Owner:ORGANIX +2
Detecting a Therapeutic Cell
ActiveUS20170056534A1Polypeptide with localisation/targeting motifImmunoglobulin superfamilyCentral nervous systemDopamine transporter
The present invention relates to a method of detecting a therapeutic cell expressing a dopamine transporter (DAT) at a central nervous system (CNS) site in a subject, which comprises the administration of a DAT tracer to the subject, wherein the presence of a therapeutic cell which expresses the DAT is determined.
Owner:UCL BUSINESS PLC
Dopamine transporter inhibitors for use in treatment of movement disorders and other CNS indications
The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
Owner:PREXA PHARMA
Labeled iodinated tropane formulation
A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi / mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.
Owner:LIKEMINDS
Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof
InactiveCN102146041AEarly detection of changesHigh affinityRadioactive preparation carriersAmino preparation by functional substitutionSodium bicarbonateImaging agent
Owner:何玉林 +1
Marker for depression, assay method, method for determining depression, screening method for antidepressants, and kit
InactiveUS20150355204A1High molecular weightReduce functionBioreactor/fermenter combinationsBiological substance pretreatmentsScreening methodDopamine
Disclosed herein are a method and a kit using a novel marker associated with depression. The marker for depression includes one or more selected from a noradrenaline transporter and a dopamine transporter. The method for determining depression includes a step of examining an expression level of the marker for depression in a blood sample collected from a subject.
Owner:MEIJO UNIVERSITY
Detecting a therapeutic cell
ActiveUS10286092B2Polypeptide with localisation/targeting motifImmunoglobulin superfamilyMedicineDopamine
The present invention relates to a method of detecting a therapeutic cell expressing a dopamine transporter (DAT) at a central nervous system (CNS) site in a subject, which comprises the administration of a DAT tracer to the subject, wherein the presence of a therapeutic cell which expresses the DAT is determined.
Owner:UCL BUSINESS PLC
Spirocyclic derivatives
ActiveUS20170253615A1Good choiceUseful in treatmentOrganic active ingredientsNervous disorderDiseaseDopamine
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R5, R6, R9, R10, Q, X, Y, Z, A, L, B, m, n and p are as defined herein.
Owner:CHRONOS THERAPEUTICS
Semi-automatic quantification method based on development specificity extraction ratio of dopamine transporter
InactiveCN104720840AHigh precisionImprove robustnessComputerised tomographsTomographyPattern recognitionSemi automatic
A semi-automatic quantification method based on a development specificity extraction ratio of a dopamine transporter includes the following steps of collecting faulted image data of the dopamine transporter; calibrating a faulted image range where a corpus striatum is located in the collected faulted image data; automatically dividing a corpus striatum area and a reference area in each calibrated faulted image; extracting the grey values of all pixels in the corpus striatum areas to serve as corpus striatum area specificity extraction count values; extracting the grey values of all pixels in the reference areas to serve as reference area specificity extraction count values; summarizing the corpus striatum area specificity extraction count values and the reference area specificity extraction count values in all the calibrated faulted images, and working out the ratio to serve as the development specificity extraction ratio. The semi-automatic quantification method can improve the efficiency, accuracy and robustness of development analysis of the dopamine transporter.
Owner:SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
Application of miR-212 to preparation of addiction treatment drug
InactiveCN110279707AOrganic active ingredientsNervous disorderPsychoactive substanceAddiction treatment
The invention relates to a non-therapeutic application of miR-212 to regulation of DAT (dopamine transporter) gene expression in cells, and further relates to a non-therapeutic method for regulating the DAT gene expression in the cells. The method comprises the step of increasing or reducing the amount of miR-212 in the cells. The invention further relates to an application of miR-212, a miR-212 enhancer or a miR-212 attenuator to preparation of a drug for regulating dopamine uptake of the cells, and further relates to an application of miR-212, the miR-212 enhancer or the miR-212 attenuator to preparation of a drug for treating psychoactive substance addiction.
Owner:SHENZHEN KANGNING HOSPITAL SHENZHEN MENTAL HEALTH INST SHENZHEN MENTAL HEALTH CENT
Substituted bisphenylalkylurea compounds and methods
Disclosed is a composition and method for a therapeutic treatment that is able to combat neuroinflammation caused by diseases and disorders such as Alzheimer's disease, Parkinson's disease, and traumatic brain injury. The class of urea compounds acts by blocking at targeted receptors in the brain that contribute to the increase in inflammation. Combinations of receptors, H1 receptor, H2 receptor, dopamine transporter (DAT), and / or 5HT3C receptor, are individually and / or collectively inhibited by the same compositions of the present disclosure, and this ability leads to a decrease in brain edema. The DAT inhibitory effects additionally maintains dopamine levels in a patient.
Owner:TEXAS TECH UNIV SYST
Diaryl sulfide derivative, preparation method thereof and application thereof as serotonin transporter targeted imaging agent
ActiveCN107200702AImprove specific binding abilityGood biological metabolism in vivoRadioactive preparation carriersIsotope introduction to organic compoundsNorepinephrine transporterSerotonin transporter
The invention belongs to the field of radiopharmaceutical chemistry and relates to a diaryl sulfide derivative, a preparation method thereof and application thereof as a serotonin transporter targeted imaging agent. The diaryl sulfide derivative has a structural formula shown in the description, exhibits high affinity with central SERT (serotonin transporter) and high selectivity for SERT relative to DAT (dopamine transporter) and NET (norepinephrine transporter). Therefore, the [18F]-diaryl sulfide derivative of the invention may act as an SERT / PET (positron emission tomography) imaging agent.
Owner:BEIJING NORMAL UNIVERSITY +1
N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R9a, R9b, R9c, R9d, R9e, R9f, m, n, A, L and B are as defined herein.
Owner:CHRONOS THERAPEUTICS
3-Cyanophenoxyalkylarylpiperazine derivatives and their application in the preparation of medicines
The invention discloses a 3-cyanophenoxyalkylarylpiperazine derivative and its application in the preparation of medicines. The role of the system, especially for 5‑HT 1A Receptor-selective high-affinity effect on dopamine D 1 and D 2 Receptors, adrenergic receptors α1 and α2, SERT (5-HT transporter protein), NET (adrenalin transporter protein), DAT (dopamine transporter protein) and other centrally related receptors and proteins have no obvious affinity effect. It exerts various physiological and pharmacological effects in vivo, and can be used as a pharmaceutical active substance, especially for diseases such as anti-depression, anxiolysis, and anti-neuropathic pain, and can also be used as an intermediate for the preparation of other active pharmaceutical compounds. The compound of the present invention has quick onset of action, small toxic and side effects, and can meet the needs of clinical application, and is a compound with the following structural formula or its free base or salt:
Owner:NHWA PHARMA CORPORATION +1
Labeled pe2i formulation and method
InactiveUS20140079634A1Convenient treatmentIsotope introduction to heterocyclic compoundsRadioactive preparation carriersTropaneDopamine
A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi / mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-N-(3-iodoprop-2E-enyl)-2β-carbomethoxy-3β-(4-methylphenyl) nortropane.
Owner:NAVIDEA BIOPHARMLS
Application of dual inhibitor for dopamine and norepinephrine transfer protein
The invention discloses an application of the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter in the preparation of medicines for treating central nervous degenerative disease and also discloses a medicine combination of the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter. The invention firstly proposes and proves that the double inhibitor of dopamine transporter (DAT) and norepinephrine transporter can protect dopaminergic neuron and provides a new choice for clinical treatment of the central nervous degenerative disease.
Owner:上海国联干细胞技术有限公司
3-cyanophenoxyalkyl aryl piperazine derivative and applications in the preparation of drugs
The invention discloses a 3-cyanophenoxyalkyl aryl piperazine derivative and applications in the preparation of drugs. The 3-cyanophenoxyalkyl aryl piperazine derivative shows the effect on central nervous systems, especially on 5-HT<1A> receptor selective high affinity interaction, but has no obvious affinity interaction on dopamine D1 and D2 receptors, adrenergic receptor alpha 1 and alpha 2, SERT (5-HT transporter protein), NET (adrenergic transporter protein), DAT (dopamine transporter protein) and other central related receptors and proteins. Various physiological and pharmacological effects are brought into play in the body; and the compound can be used as a pharmaceutical active substance, especially used for diseases like anti-depression, anti-anxiety and anti-neuropathic pain, andcan also be used as an intermediate to prepare other pharmaceutical active compounds. The compound is fast in effect and small in toxic and side effect, and can meet demands of clinical applications;and the compound is a compound having the following structural formula or a free base or salt thereof. The structure of the compound is shown in the description.
Owner:NHWA PHARMA CORPORATION +1
Dopamine transporter imaging medicine and preparation method thereof
InactiveCN101874899BImprove targetingOrganic chemistryRadioactive preparation carriersPyridineCompanion animal
The invention relates to a medicine for developing a dopamine transporter and a preparation method thereof. The medicine has the structure described in the specification, wherein X= -CH2 or -C=O, and R=Br or F18. Novel serial 2 beta amide / amino-3 beta chlorobenzene tropine derivatives containing pyridine groups are designed and synthesized by using 2 beta-carboxyl-3beta chlorobenzene tropine as alead compound, have higher targeting, can be specifically combined with DAT, can be used for marking F-18 by introducing a pyridine ring structure, can be used for carrying out PET development research, and are PD diagnosis developer with favorable application potential.
Owner:BEIJING NORMAL UNIVERSITY
The new function of the active ingredients of Dictatoria radiata in promoting the incremental expression of dopamine transporter
Owner:山东中科绿碳科技有限公司
Flavonoid derivatives and their use in the preparation of pharmaceutical compositions
InactiveCN101591319BOrganic active ingredientsNervous disorderFlavone derivativesDopamine transporter
The invention belongs to the field of medicinal chemistry, and relates to flavonoid derivatives and their application in the preparation of pharmaceutical compositions for treating diseases related to dopamine transporters. The flavonoid derivatives of the present invention have the structure of general formula (I). The results of biological evaluation show that the compound of the present invention shows better stimulant effect on dopamine transporter than the prior art, can regulate the transport of dopamine by promoting the transport function of dopamine transporter, maintain the balance of extracellular dopamine concentration, and can prepare A dopamine transporter agonist for the treatment of psychiatric and neurological disorders. R1 is selected from hydroxyl, C1-C8 alkoxy, C1-C8 ester, glycoside, halogen; R2 is selected from hydrogen, C7 hydroxyl, C7 alkoxy, C7 ester, C7 halogen; R3 They are respectively selected from hydrogen, or contain one or more substituents on the benzene ring, and the substituents are respectively selected from hydroxyl, alkoxy, ester, aryl (hetero) group, halogen, and glycoside.
Owner:FUDAN UNIV
Substituted bisphenylalkylurea compounds and methods
ActiveUS20200181069A1Combat neuroinflammationImprove inflammationNervous disorderOrganic chemistryReceptorTherapeutic treatment
Disclosed is a composition and method for a therapeutic treatment that is able to combat neuroinflammation caused by diseases and disorders such as Alzheimer's disease, Parkinson's disease, and traumatic brain injury. The class of urea compounds acts by blocking at targeted receptors in the brain that contribute to the increase in inflammation. Combinations of receptors, H1 receptor, H2 receptor, dopamine transporter (DAT), and / or 5HT3C receptor, are individually and / or collectively inhibited by the same compositions of the present disclosure, and this ability leads to a decrease in brain edema. The DAT inhibitory effects additionally maintains dopamine levels in a patient.
Owner:TEXAS TECH UNIV SYST
Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof
InactiveCN102146041BEarly detection of changesHigh affinityRadioactive preparation carriersAmino preparation by functional substitutionSodium bicarbonateImaging agent
The invention relates to a radioactive compound labeling technology in the field of positron imaging agents, in particular to a method for synthesizing carbon-11 labeled N-methyldopamine hydrochloride. The preparation method comprises the following steps of: A, fully reacting 200 to 300mCi of carbon-11 methyl iodide (II) with 3 to 6mg of dopamine hydrochloride (III) dissolved and neutralized by excessive 0.1mol / L sodium bicarbonate solution at the temperature of between 70-85DEG C, and cooling to room temperature to obtain reaction liquid; and B, blowing the reaction liquid in the step A to dryness, separating, collecting a substance with a radioactive component, wherein the radioactive component is the carbon-11 labeled N-methyldopamine hydrochloride (I). The carbon-11 labeled N-methyldopamine hydrochloride has strong affinity with a dopamine transporter and a norepinephrine transporter, can early discover the change of cardiac sympathetic nerves, and provides a strong evidence for early diagnosis and treatment of heart disease; and the preparation method is simple and practicable, good in repeatability, low in synthetic cost and stable in yield.
Owner:何玉林 +1
Novel function of active ingredients of cortex dictamni for promoting increment expression of dopamine transporter
Cortex dictamni is an important traditional Chinese medicinal material. The invention introduces a novel function of active ingredients of cortex dictamni. The action experiment of the active ingredients of cortex dictamni for primary neuron of rats discovers that overexpression of a dopamine transporter gene DAT can be promoted by adding the active ingredients of cortex dictamni, dopaminergic neuron has an important influence on motion, addiction, motion control and other behaviors, and results indicate that changes of human body pleasant sensation, motion control and other functions can be promoted by means of application of the active ingredients of cortex dictamni.
Owner:山东中科绿碳科技有限公司
Full-automatic dopamine transporter semi-quantitative value detection method based on image processing
PendingCN110992332AEffective segmentationImprove detection accuracyImage enhancementImage analysisImaging processingImage segmentation
The invention relates to a full-automatic dopamine transporter semi-quantitative value detection method based on image processing. The method comprises the following steps: (1) constructing an MRI image segmentation network, and segmenting a caudal nucleus region, a shell nucleus region and a pale globe region in a brain MRI image; (2) registering the MRI image to a PET image to obtain a segmentation result of the PET image; (3) performing clustering fine segmentation on the segmentation result of the PET image to obtain a plurality of label structures; (4) acquiring the characteristic statistics of each label structure; (5) correspondingly acquiring characteristic statistics of a top pillow leaf area in the PET image, and standardizing the characteristic statistics in each label structureby taking the characteristic statistics of the top pillow leaf area as a reference to obtain a semi-quantitative value of each characteristic statistics; and (6) performing T test on the semi-quantitative value of each label structure to finish saliency sorting of the semi-quantitative values. Compared with the prior art, the method is high in detection precision, convenient to implement and flexible in application.
Owner:FUDAN UNIV
Brain dopamine transporter examination system and operation method thereof
PendingCN114429440AImprove diagnosis rateImprove treatment outcomesImage enhancementImage analysisTreatment resultsMeasurement evaluation
The invention provides an operation method of a brain dopamine transporter examination system. The operation method comprises the following steps of: 1, detecting a brain dopamine transporter; acquiring a scanning image of the brain of the testee from the scanner, wherein the scanning image is a three-dimensional image; aligning the scanning image to a standard brain space to obtain a normalized scanning image; performing image intensity standardization on the normalized scanning image; converting the normalized scanning image after the image intensity standardization into a two-dimensional image; cutting out a plurality of image data for at least one region of interest of the two-dimensional image, wherein the region of interest comprises a left side tail core, a left side shell core, a right side tail core and a right side shell core; based on a plurality of image data, a dopaminergic neuron loss degree measurement evaluation model is established by transfer learning, so that the images are classified in the most probable neuron loss stage, an additional auxiliary diagnosis mode is provided for nuclear medical doctors to interpret brain dopamine transporter examination every time, and the accuracy of brain dopamine transporter examination is improved. And the diagnosis rate and the treatment result of clinicians are improved.
Owner:TAIPEI MEDICAL UNIV
Diaryl sulfide derivatives, methods for their preparation and use as targeting imaging agents for serotonin transporters
ActiveCN107200702BImprove specific binding abilityGood biological metabolism in vivoRadioactive preparation carriersIsotope introduction to organic compoundsNorepinephrine transporterSerotonin transporter
Disclosed are a class of diarylsulfide derivatives, a preparation method therefor, and the use thereof as a serotonin transporter-targeted imaging agent, belonging to the field of radiopharmaceutical chemistry. The diarylsulfide derivative has the structural formula (1) below, this class of compounds exhibits a high affinity for central SERT, and at the same time exhibits a high selectivity for SERT relative to DAT (a dopamine transporter) and to NET (a norepinephrine transporter). Therefore, [18F]-diarylsulfide derivatives can be used as an SERT / PET imaging agent.
Owner:BEIJING NORMAL UNIVERSITY +1
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