32 results about "Norepinephrine transporter" patented technology

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.

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.

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.

Various compounds, compositions, and methods for binding to β-amyloid plaque and norepinephrine transporters are presented. Especially preferred compounds include those with a PET-detectable label.

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.

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.

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.

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.

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.

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.

The invention relates to an N-(2-fluorine [18F] ethyl) dopamine developer and a preparation method thereof. The preparation method comprises the following steps: (1) transferring fluorine ions (18F <->) produced by a cyclotron into a chemical synthesizer, capturing in anion capturing, eluting, adding acetonitrile, and azeotropic to remove water; (2) adding an acetonitrile solution as shown in a formula (II) to react; (3) adding a dimethyl sulfoxide solution of dopamine to react; and (4) performing high-performance liquid phase separation and purification, and collecting the required radioactive component N-(2-fluorine [18F] ethyl) dopamine. The developer has strong affinity with a dopamine transporter and a noradrenaline transporter, and can be used for discovering changes of heart sympathetic nerves at an early stage, so that powerful evidence is provided for early diagnosis and treatment of heart diseases; the preparation method is good in repeatability and stable in synthesis yield.

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.