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

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Abstract

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 (K D=0.19 nM) but low density (B max=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.

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Author notes

  1. Chester A. Mathis

    Present address: Donner Laboratory, Lawrence Berkeley Laboratory, University of California, 94720, Berkeley, CA, USA

Authors and Affiliations

  1. Departments of Neurology and Pharmacology, Stanford University, 94305, Stanford, CA, USA

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

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  1. Samuel S. -H. Wang
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  2. Chester A. Mathis
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  3. Stephen J. Peroutka
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Wang, S.S.H., Mathis, C.A. & Peroutka, S.J. R(−)-2,5-Dimethoxy-4-77bromoamphetamine [77Br-R(−)DOB]: a novel radioligand which labels a 5-HT binding site subtype. Psychopharmacology 94, 431–432 (1988). https://doi.org/10.1007/BF00174703

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  • DOI: https://doi.org/10.1007/BF00174703

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