R(−)-2,5-Dimethoxy-4-77bromoamphetamine [77Br-R(−)DOB]: a novel radioligand which labels a 5-HT binding site subtype |
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| Authors: | Samuel S. -H. Wang Chester A. Mathis Stephen J. Peroutka |
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| Affiliation: | (1) Departments of Neurology and Pharmacology, Stanford University, 94305 Stanford, CA, USA;(2) Present address: Donner Laboratory, Lawrence Berkeley Laboratory, University of California, 94720 Berkeley, CA, USA |
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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 (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. |
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| Keywords: | R(– )-2,5-Dimethoxy-4-77Br-amphetamine Rat 5-Hydroxytryptamine |
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