The binding properties of the 5-hydroxytryptamine2 (5-HT2) receptor have been the subject of much interest and debate in recent years. The hallucinogenic amphetamine derivative 4-bromo-2,5-dimethoxyphenylisopropylamine (DOB) has been shown to bind to a small number of binding sites with properties very similar to [3H]ketanserin-labeled 5-HT2 receptors, but with much higher agonist affinities....
Abstract N1‐([ 11 C]‐Methyl)‐2‐Br‐LSD ([ 11 C]‐MBL) has been developed as a positron emission tomography (PET) imaging agent for serotonin 5‐HT 2 receptors. In vitro receptor binding assays with nonradioactive MBL show high‐affinity binding to serotonin 5‐HT 2 receptors (K i = 0.5 nM), a secondary interaction of 8‐fold lower affinity with dopamine D 2 receptors, and low‐affinity interactions...
3H-Lysergic acid diethylamide (3H-LSD) is irreversibly incorporated into bovine caudate membranes during ultraviolet light illumination. The incorporated radioligand apparently forms a covalent bond with a subpopulation of the membrane proteins. Although the photolabeling pattern differs significantly from the Coomassie blue staining pattern on SDS gels, the photolabeling is apparently not...