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Phenyltropanes are a family of chemical compounds originally derived from structural modification of cocaine. These compounds present many different avenues of research into therapeutic applications, particularly in addiction treatment. Uses vary depending on their construction and structure-activity relationship ranging from the treating of cocaine dependency to understanding the dopamine reward system in the human brain to treating Alzheimer's & Parkinson's diseases. ((Since 2008 ) there have been continual additions to the list and enumerations of the plethora of types of chemicals that fall into the category of this substance profile.) Many of the compounds were first elucidated in published material by the Research Triangle Institute and are thus named with "RTI" serial-numbers. Similarly, a number of others are named for Sterling-Winthrop pharmaceuticals ("WIN" serial-numbers) and Wake Forest University ("WF" serial-numbers). ==2-Carboxymethyl esters== Cocaine is considered a 'typical' or 'classical' (i.e. "cocaine-like") DAT re-uptake pump ligand in that it stabilizes an "open-to-out" conformation on the dopamine transporter; despite the extreme similarity of phenyltropanes, many of them (incl. β-CFT, β-CPT, 2β-carbomethoxy-3β-(4-fluorophenyl)tropane & 2β-carbomethoxy-3β-phenyltropane) are in suchwise not considered "cocaine-like" and are instead considered atypical inhibitors insofar as they stabilize what is considered a more inward-facing (closed-to-out) conformational state.〔(J Pharmacol Exp Ther. 2013 Jul; 346(1): 2–10. Fig. 1. Published online 2013 Jul. doi: 10.1124/jpet.111.191056 )〕 Certain phenyltropanes can be used as a smoking cessation aid. Blank spacings within tables for omitted data use "no data", "?", "-" or "—" interchangeably. * ɑ''Ki'' value for displacement of ()DA uptake. * b''Ki'' value for displacement of ()5-HT uptake. * c''Ki'' value for displacement of ()NE uptake. * d()5-HT uptake to ()DA uptake ratio. * e()NE uptake to ()DA uptake ratio. * fIC50 for displacement of ()cocaine. 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「List of phenyltropanes」の詳細全文を読む スポンサード リンク
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