Long‐lasting inhibition of in vivo cocaine binding to dopamine transporters by 3β‐(4‐Iodophenyl)Tropane‐2‐Carboxylic acid Methyl Ester: RTI‐55 or βCIT

N. D. Volkow, S. J. Gatley, J. S. Fowler, R. Chen, J. Logan, S. L. Dewey, Y. ‐S Ding, N. Pappas, P. King, R. R.Mac Gregor, M. J. Kuhar, F. I. Carroll, A. P. Wolf

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

Cocaine analogs such as 3β‐(4‐iodophenyl)tropane‐2β‐carboxylic acid methyl ester (RTI‐55 or βCIT) with a higher affinity for the dopamine transporter (DAT) may be potentially useful in interfering with cocaine's actions in brain. This study evaluates the time course of the effects of RTI‐55 on cocaine binding in baboon brain using PET and [11C]cocaine. [11C]Cocaine binding was measured prior to, and 90 minutes, 24 hours, 4–5 days and 11–13 days after RTI‐55 (0.3 mg/kg i.v.). Parallel studies with [3H]cocaine and RTI‐55 (0.5 mg/kg i.v. or 2 mg/kg i.p.) were performed in the mouse. RTI‐55 significalitly inhibited [11C]cocaine binding at 90 minutes and 24 hours after administration.The half‐life for the clearance of RTI‐55 from the DAT was estimated to be 2 to 3 days in the baboon brain. In the mouse brain, RTI‐55 significantly inhibited [3H]cocaine binding at 60 and 180 minutes after administration and recovery was observed at 12 hours. These results document long‐lasting inhibition of cocaine binding by RTI‐55 and corroborate that binding kinetics of RTI‐55 in striatum observed in imaging studies with [123I]RTI‐55 represents binding to DATs. © 1995 Wiley‐Liss, Inc.

Original languageEnglish
Pages (from-to)206-211
Number of pages6
JournalSynapse
Volume19
Issue number3
DOIs
StatePublished - Mar 1995
Externally publishedYes

Keywords

  • Baboon
  • Carbon‐11
  • PET

Fingerprint

Dive into the research topics of 'Long‐lasting inhibition of in vivo cocaine binding to dopamine transporters by 3β‐(4‐Iodophenyl)Tropane‐2‐Carboxylic acid Methyl Ester: RTI‐55 or βCIT'. Together they form a unique fingerprint.

Cite this