10 results about "Norepinephrine transporter" patented technology

Provided are macromolecular prodrugs in which 7-hydroxymethylcamptothecin (CPT-MeOH) is covalently bonded to a polymer via ester bonds that are labile under physiological conditions. The CPT-MeOH may be functionalized with a norepinephrine transporter (NET) ligand. Also provided are methods of treating cancer, especially neuroblastoma with the macromolecular prodrugs.

The invention relates to the technical field of biological medicines, in particular to a noradrenaline transporter-targeting phenoxy alkyl guanidine derivative as well as a preparation method and application of the noradrenaline transporter-targeting phenoxy alkyl guanidine derivative. The structure of the phenoxyalkyl guanidine derivative is shown as a formula (I): # imgabs0 #, wherein R1 is 19F, 18F or 131I; r2 is hydrogen, a hydroxyl group, fluorine, chlorine, bromine, a C1-C6 alkoxy group or a C1-C6 substituted alkoxy group; l is a linker and is C2-C10 alkyl, C2-C10 substituted alkyl, C3-C10 cycloalkyl or C3-C10 substituted cycloalkyl. The F-18 or I-131 labeled phenoxy alkyl guanidine derivative provided by the invention can be used as a NET targeted radioactive diagnosis or treatment drug with higher affinity and better targeting property, and can be used for myocardial sympathetic nerve imaging and NET positive tumor diagnosis or treatment in nuclear medicine.

The invention relates to pharmaceutical compositions comprising the compound of Formula I,and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and / or pathways involving dopamine D2 receptor signaling, sodium channel activity, and / or norepinephrine transporter activity.

The present invention discloses a derivative containing an arylpiperazine structure, a composition and its application. The derivative is a compound having the structure as shown in general formula (I) or a pharmaceutically acceptable salt thereof; the composition includes a derivative containing an arylpiperazine structure or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers. The present invention also provides the application of a derivative containing an arylpiperazine structure or a pharmaceutically acceptable salt thereof in the preparation of an antidepressant drug. The derivative can not only have a high affinity for 5-HT 1A receptor and 5-HT 2A receptor, but also have a good affinity for 5-HT transporter (SERT) and norepinephrine transporter (NET); when it is applied to the treatment of depression, it can have the characteristics of high response rate, short onset time, and small side effects, so as to meet the needs of clinical medication.

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.

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.

The invention discloses an indole piperidine compound with double / multi-target analgesic activity as well as a preparation method and application thereof. The compound has double-target activity of a mu opioid receptor (MOR) / noradrenaline transporter (NET) and a MOR / 5-serotonin transporter (SERT), has multi-target activity of MOR / NET / SERT, and can be used for preparing medicines for preventing or treating pain-related diseases. Experimental results show that the indole piperidine compound provided by the invention has relatively high affinity to MOR / NET, MOR / SERT or MOR / NE / SERT, and meanwhile, the indole piperidine compound shows good analgesic activity in an experiment of neuralgia induced by acetic acid twisting and paclitaxel. Good safety is shown in an acute toxicity experiment and an open field experiment. # imgabs0 #

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.

The invention relates to a particular substituted heterocycle fused gamma-carboline, the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and / or pathways involving dopamine D2 receptor signaling, sodium channel activity, and / or norepinephrine transporter activity.