R(-)-2,5-dimethoxy-4-77 bromoamphetamine [77Br-R(-)DOB]: a novel radioligand which labels a 5-HT binding site subtype.
S S Wang, C A Mathis, S J Peroutka
Psychopharmacology 1988 DOI: 10.1007/bf00174703 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Peer reviewed |
|---|---|
| Population | Rat brain membrane preparations |
| Key points | The authors conclude that 77Br-R(-)DOB labels 5-HT recognition sites in rat brain with high affinity (KD = 0.19 nM) and low density (Bmax = 0.32 pmol/g tissue), and that these sites do not fit current classifications of 5-HT binding subtypes. They suggest the finding may aid in understanding the mechanism of action of hallucinogens in humans. |
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.