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PRC200-SS is an arylalkanolamine TRI being developed by the Mayo Clinic.〔Y. Liang, E. Richelson. Triple Reuptake Inhibitors: Next-Generation Antidepressants. (Primary Psychiatry. 2008;15(4):50-56. )〕 Sympathomimetic PRC200-SS is the PRC050 eutomer, whereas PRC201 is the distomer. These compounds are preceded by venlafaxine, which Wyeth claims is the first SNRI. Venlafaxine was originally developed as an "opioid" although original screening returned negative results.〔 The authors were not satisfied just to drop venlafaxine from development and continued with their study of the compounds biological activity data. Herein, they discovered that venlafaxine exerts its biological actions via interaction with the monoamine receptors. In particular, the actions of the drug on increasing the amount of 5-HT and NE were documented,〔 although with "potentiated" analogs such as the pm-dichlorophenyl ring substituted derivative, it might be expected to behave as a SNDRI also (but no data was available to support this inference). Venlafaxine itself has been said to behave as a SNDRI at very high doses. This would be more likely to be the case in drug naїve subjects than in users that have already built up significant tolerance. Silicon containing analog of venlafaxine was prepared and demonstrated to be an active SNRI. ==Chirality== For venlafaxine there is only one chiral centre, although for the PRC compounds, there is a diastereoisomeric pair of racemers to consider. The exact choice of conditions (e.g. temperature and choice of solvent, etc.) can be altered to try to increase the dia/stereo-selectivity. PRC050 is racemic SS/RR, PRC025 is racemic SR/RS,〔 venlafaxine is racemic; PRC050 was further resolved into its constituent enantiomers, PRC200 (SS) and PRC201 (RR), respectively.〔 As can be seen in the above table, a high eudysmic ratio exists for PRC050 with activity residing in the SS enantiomer (PRC200). 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「PRC200」の詳細全文を読む スポンサード リンク
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