RTI-83

RTI-83

Systematic (IUPAC) name
methyl (1R,2S,3S,5S)-3-(4-ethylphenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
Clinical data
Identifiers
CAS Registry Number	155337-52-3
PubChem	CID 9882384
Chemical data
Formula	C18H25NO2
Molecular mass	287.396 g/mol
SMILES CCc3ccc(cc3)C(C1C(=O)OC)CC2CCC1N2C

(–)-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 (K_i) 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 K_i values of 15 nM at DAT and 7.1 nM at SERT, vs 28,000 nM at NET.^[1][2]

cis-propenyl analogue (RTI-11w)

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,^[3] its pharmacology in vivo has not been studied in detail.

See also

• UWA-101

References