(–)-2β-Carboisopropoxy-3β-(4-iodophenyl)tropane (RTI-4229-121, IPCIT) is a stimulant drug used in scientific research, which was developed in the early 1990s.[1] RTI-121 is a phenyltropane based, highly selective dopamine reuptake inhibitor[2] and is derived from methylecgonidine. RTI-121 is a potent and long-lasting stimulant, producing stimulant effects for more than 10 hours after a single dose in mice[3] which would limit its potential uses in humans, as it might have significant abuse potential if used outside a medical setting. However RTI-121 occupies the dopamine transporter more slowly than cocaine, and so might have lower abuse potential than cocaine itself.[4]
Uses
RTI-121 is mainly used in scientific research into the dopamine reuptake transporter. It is more selective for the dopamine transporter than other DAT radioligands such as β-CIT, and so has less nonspecific binding and produces "cleaner" images.[5][6] Various radiolabelled forms of RTI-121 (with different radioactive isotopes of iodine used depending on the application) are used in both humans and animals to map the distribution of dopamine transporters in the brain.[7][8]
Legal status
RTI-121 not specified as controlled substance in any country as of 2007. Some jurisdictions such as the United States, Australia, and New Zealand, however, might however consider RTI-121 to be a controlled substance analogue of cocaine on the grounds of its related chemical structure.
↑Scanley BE, al-Tikriti MS, Gandelman MS, Laruelle M, Zea-Ponce Y, Baldwin RM, etal. (January 1995). "Comparison of [123I]beta-CIT and [123I]IPCIT as single-photon emission tomography radiotracers for the dopamine transporter in nonhuman primates". European Journal of Nuclear Medicine. 22 (1): 4–11. doi:10.1007/BF00997241. PMID7698153. S2CID20406294.
↑Chen NH, Ding JH, Wang YL (March 1997). "Characterization of [125I]RTI-121 binding to dopamine transporter in vitro". Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica. 18 (2): 115–20. PMID10072960.
