R(-)-2,5-Dimethoxy-4-77bromoamphetamine [77Br-R(-)DOB]: a novel radioligand which labels a 5-HT binding site subtype

Samuel S.H. Wang, Chester A. Mathis, Stephen J. Peroutka

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


R(-)-2,5-Dimethoxy-4-77Br-amphetamine [77Br-R(-)DOB], a radioligand of high specific activity (1500±200 Ci/mmol), was used to label membrane-associated recognition sites in rat brain. 77Br-R(-)DOB sites were of high affinity (KD=0.19 nM) but low density (Bmax=0.32 pmol/g tissue) in rat brain preparations. Competition experiments show that both 5-hydroxytryptamine (5-HT) and 5-HT2 antagonists display nanomolar potency for these sites. We conclude that 77Br-R(-)DOB labels 5-HT recognition sites in rat brain which do not fit into current classifications of 5-HT binding subtypes. This finding may be of aid in deciphering the mechanism of action of hallucinogens in man.

Original languageEnglish (US)
Pages (from-to)431-432
Number of pages2
Issue number3
StatePublished - Mar 1988
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmacology


  • 5-Hydroxytryptamine
  • R(-)-2,5-Dimethoxy-4-Br-amphetamine
  • Rat


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