@article {Gonzalez-Maeso:2009:0929-8673:1017,
title = "Agonist-Trafficking and Hallucinogens",
journal = "Current Medicinal Chemistry",
parent_itemid = "infobike://ben/cmc",
publishercode ="ben",
year = "2009",
volume = "16",
number = "8",
publication date ="2009-03-01T00:00:00",
pages = "1017-1027",
itemtype = "ARTICLE",
issn = "0929-8673",
url = "https://www.ingentaconnect.com/content/ben/cmc/2009/00000016/00000008/art00008",
doi = "doi:10.2174/092986709787581851",
keyword = "lysergic acid diethylamide (LSD), G protein-coupled receptors (GPCRs), hallucinogenic drugs, Hallucinogens, Agonist-Trafficking",
author = "Gonzalez-Maeso, Javier and Sealfon, Stuart C.",
abstract = "Seven transmembrane domain receptors, also termed G protein-coupled receptors (GPCRs), represent the most common molecular target for therapeutic drugs. The generally accepted pharmacological model for GPCR activation is the ternary complex model, in which GPCRs exist in a dynamic equilibrium between the active and inactive conformational states. However, the demonstration that different agonists sometimes elicit a different relative activation of two signaling pathways downstream of the same receptor has led to a revision of the ternary complex model. According to this agonist- trafficking model, agonists stabilize distinct activated receptor conformations that preferentially activate specific signaling pathways. Hallucinogenic drugs and non-hallucinogenic drugs represent an attractive experimental system with which to study agonist-trafficking of receptor signaling. Thus many of the behavioral responses induced by hallucinogenic drugs, such as lysergic acid diethylamide (LSD), psilocybin or mescaline, depend on activation of serotonin 5-HT2A receptors (5-HT2ARs). In contrast, this neuropsychological state in humans is not induced by closely related chemicals, such as lisuride or ergotamine, despite their similar in vitro activity at the 5-HT2AR. In this review, we summarize the current knowledge, as well as unresolved questions, regarding agonist-trafficking and the mechanism of action of hallucinogenic drugs.",
}