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RTI-83
(–)-2β-Carbomethoxy-3β-(4-ethylphenyl)tropane (RTI-83) is a phenyltropane derivative which represents a rare example of an SDRI or serotonin-dopamine reuptake inhibitor, a drug which inhibits the reuptake of the neurotransmitters serotonin and dopamine, while having little or no effect on the reuptake of the related neurotransmitter noradrenaline. With a binding affinity (Ki) of 55 nM at DAT and 28.4 nM at SERT but only 4030 nM at NET, RTI-83 has reasonable selectivity for DAT/SERT over NET, but further research has shown that by extending the ethyl chain even better selectivity can be achieved, with the 4′-(''cis''-propenyl) analogue having Ki values of 15 nM at DAT and 7.1 nM at SERT, vs 28,000 nM at NET.〔Blough BE, Abraham P, Lewin AH, Kuhar MJ, Boja JW, Carroll FI. Synthesis and transporter binding properties of 3 beta-(4′-alkyl-, 4′-alkenyl-, and 4′-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. ''Journal of Medicinal Chemistry''. 1996 Sep 27;39(20):4027-35. PMID 8831768〕
Such drugs are speculated to be useful as potential antidepressants, but few examples have been reported in the literature as yet. However while RTI-83 has been used for binding studies to model the monoamine transporter proteins,〔Roman DL, Saldaña SN, Nichols DE, Carroll FI, Barker EL. Distinct molecular recognition of psychostimulants by human and Drosophila serotonin transporters. ''Journal of Pharmacology and Experimental Therapeutics''. 2004 Feb;308(2):679-87. PMID 14593087〕 its pharmacology ''in vivo'' has not been studied in detail.
==See also==
* UWA-101
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