Antagonist properties of d-LSD at 5-hydroxytryptamine2 receptors.
The hallucinogenic agent d-lysergic acid diethylamide (d-LSD) interacts with a number of serotonin (5-hydroxytryptamine [5-HT]) receptor subtypes in the central nervous system. It has been hypothesized that hallucinosis is produced by agonist activity at 5-HT2 receptors. There exist, however, numerous data from radioligand binding, cellular, smooth muscle, and behavioral studies that suggest that d-LSD is a potent 5-HT2 antagonist. These data are reviewed in this report. In addition, d-LSD displays agonist activity at 5-HT1A and 5-HT1C receptor subtypes, as determined in biochemical studies. At the present time, agonist interactions at 5-HT1C receptors, as opposed to 5-HT2 receptors, appears to be a more likely "common mechanism of action" of hallucinogenic agents.
Pierce
P A
PA
Department of Neurology, Stanford University Medical Center, CA 94305.
Peroutka
S J
SJ
D000818:Animals; D006801:Humans; D008238:Lysergic Acid Diethylamide / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D008238:Lysergic Acid Diethylamide