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Fluorescent substrates for monoamine transporters as optical false neurotransmitters

机译:单胺转运蛋白的荧光底物,作为光学假神经递质

摘要

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.; embedded image
机译:本发明涉及具有以下通式的化合物:其中Y为O,X为O,不存在键α且存在键β,或Y为H,X为CH,存在键α,且不存在键; Z原子是碳,并且存在键χ,δ和γ,或者是氮,并且不存在χ,δ和γ。 R 1 是-H,-OH,-O-R 7 ,-N(H)-R 8 ,-N(H) -(CH 2 n -NH 2 ,-N(R 9 )(R 10 )或哌嗪阳离子; R 2 与R 9 共价结合,或者为-H,或者与R 3 共价结合,从而形成取代基或未取代的吡咯或R 2 与R 9 或R 8 或R 7 共价结合;或R 1 和R 2 共价连接形成芳环; R 3 或与R 2 共价结合形成吡咯,或尤其是-H,-OH,烷基或当Z为氮时R 3 是═O; R 4 尤其是-H,-OH或-R 11 NH 2 ; R 5 尤其是-H,-OH或-R 12 NH 2 和R 6 >或者共价结合到R 10 或是-H,或者R 6 共价结合到R 10 或R 8 或R 7 。本发明还提供了制备该化合物的方法以及通过使用该化合物监测单胺转运蛋白的活性或治疗与单胺转运蛋白相关的疾病的方法。 “嵌入式图像”

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