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32 results about "Norepinephrine transporter" patented technology
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The norepinephrine transporter (NET), also known as solute carrier family 6 member 2 (SLC6A2), is a protein that in humans is encoded by the SLC6A2 gene. NET is a monoamine transporter and is responsible for the sodium-chloride (Na⁺/Cl⁻)-dependent reuptake of extracellular norepinephrine (NE), which is also known as noradrenaline. NET can also reuptake extracellular dopamine (DA). The reuptake of these two neurotransmitters is essential in regulating concentrations in the synaptic cleft. NETs, along with the other monoamine transporters, are the targets of many antidepressants and recreational drugs. In addition, an overabundance of NET is associated with ADHD. There is evidence that single-nucleotide polymorphisms in the NET gene (SLC6A2) may be an underlying factor in some of these disorders.
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Owner:SEPACOR INC
2-substituted piperidines that are ligands for monoamine receptors and transporters
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Owner:SEPACOR INC
3,5 - substituted indole compounds having nos and norepinephrine reuptake inhibitory activity
InactiveUS20090131503A1Diminishment of extentAvoid spreadingBiocideNervous disorderNorepinephrine transporterAdrenergic
The present invention relates to novel 3,5-substituted indole compounds of Formula (I) having nitric oxide synthase (NOS) inhibitory activity together with inhibitory activity at the norepinephrine transporter (NET), to pharmaceutical and diagnostic compositions containing them, and to their medical use.
Owner:NEURAXON INC
Use of isoindoles for the treatment of neurobehavioral disorders
InactiveUS20090318520A1Organic active ingredientsBiocideBehavioural disordersNorepinephrine transporter
The present invention generally relates to the use of drugs for the treatment of neurobehavioral disorders or symptoms of a neurobehavioral disorder associated with dysfunction of the trimonoamine modulating system (TMMS). More specifically, the invention describes methods for the treatment of a neurobehavioral disorder and / or treatment or prevention of symptoms of a neurobehavioral disorder by administering suitable Isoindole derivatives alone or in combination with other agents so as to provide relatively equal inhibitory effect on serotonin, dopamine and norepinephrine transporters.
Owner:LAPKO FOUND +1
Genetic and pharmacological regulation of antidepressant-sensitive biogenic amine transporters through PKG/p38 map kinase
The invention relates to the observation that the p38 mitogen-activated protein kinase pathway is an important regulator of biogenic amine transporter (BAT) function. By using modulator of p38 MAPK, one can alter BAT function in a specific manner. This recognition of the pathway and its interaction with the serotonin transporter (SERT) and the norepinephrine transporter (NET), along with the PPA, PKG and PDE pathways, also provides the opportunity to identify polymorphisms that will impact the efficacy of drugs that act though on these enzymes or their pathways.
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
Genetic screening for predicting antidepressant drug response based on the monoamine transporter gene polymorphism combination
The present invention discloses is a method of selecting a drug based on personal genetic information when prescribing an antidepressant for a depressed patient. According to the invention, either a noradrenaline reuptake inhibitor (NRI) antidepressant or a selective serotonin reuptake inhibitor (SSRI) antidepressant can be selected based on the combination of monoamine transporter gene polymorphisms, that is, NET G1287A polymorphism in a norepinephrine transporter (NET) gene, serotonin transporter gene (5-HTT) promoter polymorphism and 5-HTT gene intron 2 polymorphism. Also, based on the norepinephrine transporter gene NET G1287A polymorphism alone, the noradrenaline reuptake inhibitor (NRI) antidepressant can be selected.
Owner:RES & BUSINESS FOUND SUNGKYUNKWAN UNIV
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
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Owner:SEPACOR INC
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
Method for preparation of n-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, and use therof
InactiveUS20110313183A1Simplify separationEasy to purifyTin organic compoundsOrganic compound preparationNorepinephrine transporterLeaving group
A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [123Iodine](R)—N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([123I]MIPP) with a leaving group Bu3Sn.
Owner:INST NUCLEAR ENERGY RES ROCAEC
Tropane analogs and methods for inhibition of monoamine transport
New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
Owner:ORGANIX +1
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
Tropane analogs and methods for inhibition of monoamine transport
New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
Owner:ORGANIX
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
Methods of use and formulations of allosteric modulators of the serotonin, dopamine and other receptor systems for medical, recreational, religious, research and other uses.
PendingUS20220265601A1Lower Level RequirementsHydroxy compound active ingredientsAmide active ingredientsIonic ChannelsMuscarinics
The invention involves the use of formulations of positive, negative, inverse agonist, or neutral allosteric modulators of receptors such as, but not limited to: 5ht1a / b / c / d, 5ht2a / b / c, 5ht3, 5ht4, 5ht5, 5ht6, 5ht7, dopamine receptors (D1, D2, D3, D4, D5), adrenergic receptors (α1A, α1B, α2A, α2B, α2C, β1, β2), serotonin transporter (SERT), DA transporter (DAT), norepinephrine transporter (NET), imidazoline1 receptor (I1), Sigma receptors (σ1, σ2), delta opioid receptor (DOR), kappa opioid receptor (KOR), mu opioid receptor (MOR), muscarinic receptors (M1, M2, M3, M4, M5), histamine receptors (H1, H2), calcium ion channel (Ca+) and N-methyl D-aspartate (NMDA) glutamate receptor; alone or in combination with items such as, but not limited to: cannabinoids, terpenes, flavonoids, minerals, psychedelic and psychoactive compounds such as, but not limited to 5ht2a receptor agonists or other compounds; for medical, recreational, religious, research and other uses.
Owner:HELDRETH JR DAVID ALAN
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
(hetero)arylalkylamino-pyrazolopyridazine derivatives having multimodal activity against pain
InactiveUS20200199127A1Nervous disorderOrganic chemistryVoltage-gated calcium channel (VGCC)Norepinephrine transporter
The present invention relates to (hetero)arylalkylamino-pyrazolopyridazine derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the Noradrenaline transporter (NET), to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
Owner:ESTEVE PHARMA SA
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
Alcoxyamino derivatives for treating pain and pain related conditions
ActiveUS11401270B2Organic chemistryAntipyreticVoltage-gated calcium channel (VGCC)Norepinephrine transporter
The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
Owner:ESTEVE PHARMA SA
New tetrahydropyrimidodiazepin and tetrahydropyridodiazepin compounds for treating pain and pain related conditions
PendingCN113166147AOrganic active ingredientsNervous disorderVoltage-gated calcium channel (VGCC)Norepinephrine transporter
Owner:ESTEVE PHARMA SA
Use of isoindoles for the treatment of neurobehavioral disorders
InactiveUS20180098970A1Organic active ingredientsNervous disorderNorepinephrine transporterIsoindoles
Owner:AFECTA PHARMA INC
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
Owner:BEIJING NORMAL UNIVERSITY +1
MIBG analogs and uses thereof
ActiveUS10874752B2Safety managementOrganic active ingredientsIsotope introduction to heterocyclic compoundsNorepinephrine transporterAdrenergic
Owner:BOARD OF RGT UNIV OF NEBRASKA
New alcoxyaminopyridine derivatives for treating pain and pain related conditions
PendingCN113195489AOrganic active ingredientsNervous disorderVoltage-gated calcium channel (VGCC)Norepinephrine transporter
The present invention relates to new compounds of formula (I) that show dual activity towards the subunit [alpha]2[delta] of voltage-gated calcium channels (VGCC), especially the [alpha]2[delta]-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
Owner:ESTEVE PHARMA SA
Method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, and use therof
InactiveUS8258331B2High yieldImprove solubilityTin organic compoundsOrganic compound preparationNorepinephrine transporterLeaving group
A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [123Iodine](R)—N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([123I]MIPP) with a leaving group Bu3Sn.
Owner:INST NUCLEAR ENERGY RES ROCAEC
N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof
PendingCN113444002AHigh affinityAutomated synthesisOrganic compound preparationRadioactive preparation carriersChemical synthesisEthyl group
![N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/eff4d4ba-cdef-4098-baab-756807761911/200505215448.png "N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof")
![N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/eff4d4ba-cdef-4098-baab-756807761911/2005051710432.png "N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof")
![N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/eff4d4ba-cdef-4098-baab-756807761911/2005051710433.png "N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof")
Owner:何玉林
Mibg analogs and uses thereof
ActiveUS20180256761A1Safety managementOrganic active ingredientsIsotope introduction to heterocyclic compoundsNorepinephrine transporterAdrenergic
Compounds and compositions for targeting cells expressing norepinephrine transporter, and methods of making and using the same. The compounds comprise MIBG analogs conjugated to active agents for treatment and / or diagnosis of various conditions, including neuroblastoma.
Owner:BOARD OF RGT UNIV OF NEBRASKA
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