RTI-121
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| RTI-121
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| Systematic (IUPAC) name | |
| propan-2-yl (1R,2S,3S)-3-(4-iodophenyl) -8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C18H24INO2 |
| Mol. mass | 413.29 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Legal |
| Routes | ? |
(-)-2β-Carboisopropoxy-3β-(4-iodophenyl)tropane (RTI-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 of a strictly controlled 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 is legal in all countries throughout the world as of 2007. Some jurisdictions such as the USA, Canada, Australia and New Zealand might however consider RTI-121 to be a controlled substance analogue of cocaine on the grounds of its related chemical structure.
References
- ↑ Scheffel U, Dannals RF, Wong DF, Yokoi F, Carroll FI, Kuhar MJ. Dopamine transporter imaging with novel, selective cocaine analogs. Neuroreport. 1992 Nov;3(11):969-72.
- ↑ Boja JW, Cadet JL, Kopajtic TA, Lever J, Seltzman HH, Wyrick CD, Lewin AH, Abraham P, Carroll FI. Selective labeling of the dopamine transporter by the high affinity ligand 3 beta-(4-[125I]iodophenyl)tropane-2 beta-carboxylic acid isopropyl ester. Molecular Pharmacology. 1995 Apr;47(4):779-86.
- ↑ Fleckenstein AE, Kopajtic TA, Boja JW, Carroll FI, Kuhar MJ. Highly potent cocaine analogs cause long-lasting increases in locomotor activity. European Journal of Pharmacology. 1996 Sep 12;311(2-3):109-14.
- ↑ Stathis M, Scheffel U, Lever SZ, Boja JW, Carroll FI, Kuhar MJ. Rate of binding of various inhibitors at the dopamine transporter in vivo. Psychopharmacology (Berlin). 1995 Jun;119(4):376-84.
- ↑ Scanley BE, al-Tikriti MS, Gandelman MS, Laruelle M, Zea-Ponce Y, Baldwin RM, Zoghbi SS, Hoffer PB, Charney DS, Wang S, et al. 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. 1995 Jan;22(1):4-11.
- ↑ Scanley BE, Gandelman MS, Laruelle M, Al-Tikriti MS, Baldwin RM, Zoghbi SS, Hoffer PB, Wang S, Neumeyer JL, Innis RB. [123I]IPCIT and [123I]beta-CIT as SPECT tracers for the dopamine transporter: a comparative analysis in nonhuman primates. Nuclear Medicine and Biology. 2000 Jan;27(1):13-21.
- ↑ Chen NH, Ding JH, Wang YL. Characterization of [125I]RTI-121 binding to dopamine transporter in vitro. Zhongguo Yao Li Xue Bao. 1997 Mar;18(2):115-20.
- ↑ Lever JR, Scheffel U, Stathis M, Seltzman HH, Wyrick CD, Abraham P, Parham K, Thomas BF, Boja JW, Kuhar MJ, Carroll FI. Synthesis and in vivo studies of a selective ligand for the dopamine transporter: 3 beta-(4-[125I]iodophenyl) tropan-2 beta-carboxylic acid isopropyl ester ([125I]RTI-121). Nuclear Medicine and Biology. 1996 Apr;23(3):277-84.
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