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3 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.
Diazabicyclic modulators of monoamine transporters
PCT designated stageWO2026033049A1Nervous disorderOrganic chemistryAzabicyclaneNeuro-degenerative disease
Disclosed are compounds of the formulae (II) and (III), and pharmaceutically acceptable salts thereof: (II) (III) wherein * represents the relative cis- or trans- conformations in formulae (II) and (III) respectively and R1, R2, each R3, each R4, n and m are as defined herein. The compounds are modulators of norepinephrine transporters (NET), dopamine transporters (DAT), serotonin transporters (SERT), sigma-1 receptor (σ1R), muscarinic M1 receptors and / or muscarinic M2 receptors and are expected to be useful in the treatment of pain, neuropsychiatric or neurodegenerative diseases, sleep disorders, as a sedative or as an anaesthetic.
Owner:UNIVERSITY OF BERN
Radioactive medical isotope 18F labeled noradrenaline analogue as well as preparation method and application thereof
ActiveCN122036560AOrganic chemistryRadioactive preparation carriersNorepinephrine transporterIsotopic labeling
The invention discloses a radioactive medical isotope 18F labeled noradrenaline analogue as well as a preparation method and application thereof. The noradrenaline analogue comprises a compound shown in a structural formula I, in the formula I, X is independently selected from H, F, Cl and Br, Y is independently selected from H, F, Cl and Br, R is selected from-(CH2CH2O) n-,-(CH2O) m-,-(CH2CH2CH2O) o-,-(CH2CH2CH2CH2O) p-and-(CH2) z-, n = 1-4, m = 1-3, o = 1-3, p = 1-3, and z = 1-6. The radioactive medical isotope < 18 > F labeled noradrenaline analogue has a benzylguanidine core structure, so that the radioactive medical isotope < 18 > F labeled noradrenaline analogue can be endowed with relatively strong noradrenaline transporter affinity, is stable in structure, simple and convenient to label, high in radiochemical purity and good in targeting property, and can meet clinical requirements of cardiac sympathetic nerve imaging. I.
Owner:FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
Prodrugs targeting norepinephrine transporters for cancer therapy
PendingCN122138830APharmaceutical non-active ingredientsHeterocyclic compound active ingredientsCamptothecinNeuroblastoma
Macromolecular prodrugs are provided in which 7-hydroxymethyl camptothecin (CPT-MeOH) is covalently bonded to a polymer through an ester linkage that is unstable under physiological conditions. The CPT-MeOH can be functionalized with a norepinephrine transporter (NET) ligand. Methods of treating cancer, particularly neuroblastoma, with the macromolecular prodrugs are also provided.
Owner:THE CHILDRENS HOSPITAL OF PHILADELPHIA