Stereospecific receptor sites for d-lysergic acid diethylamide in rat brain: effects of neurotransmitters, amine antagonists, and other psychotropic drugs.
Molecular Pharmacology July 1, 1976 Richard A. Lovell, Daniel X. Freedman 54 citations
Rat brain particulates show high- and low-affinity stereospecific binding of d-lysergic acid diethylamide (LSD). The high-affinity binding is saturable (half-saturation at 4 nM) and varies by brain region and subcellular fraction, with highest binding in the striatum and microsomal fractions. The subcellular distribution suggests the acceptor may not be limited to neuronal soma or terminal membranes. Among drugs tested, methiothepin most effectively blocked high-affinity LSD binding. The pattern of drug effects indicates that the high-affinity binding site may not be identical to a serotonin (5-HT) or dopamine receptor, but LSD and its congeners can bind to such receptors while also attaching to nearby membrane points, consistent with LSD acting agonistically or antagonistically at central 5-HT and possibly dopamine receptors in vivo.