title: Endogenous beta-carbolines as clonidine-displacing substances.
abstract: Endogenous beta-carbolines, such as harmane, are known to occur in mammalian species including humans. Radioligand binding studies have revealed that certain beta-carbolines display high affinity for both I(1) and I(2) imidazoline-binding sites (IBS). Functional studies have shown that the beta-carboline harmane elicits many characteristics expected of an endogenous ligand IBS. This article discusses the evidence relating to beta-carbolines as endogenous ligands and presents a case for harmane and related compounds as endogenous ligands for IBS.
authors.affiliation: Psychopharmacology Unit, School of Medical Sciences, University Walk, Bristol BS8 1TD, UK.
authors.forename: E S J
authors.initials: ES
authors.lastname: Robinson
authors.forename: N J
authors.initials: NJ
authors.lastname: Anderson
authors.forename: J
authors.initials: J
authors.lastname: Crosby
authors.forename: D J
authors.initials: DJ
authors.lastname: Nutt
authors.forename: A L
authors.initials: AL
authors.lastname: Hudson
mesh_terms: D000316:Adrenergic alpha-Agonists / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D002243:Carbolines / Q000737:chemistry / Q000378:metabolism*; D003000:Clonidine / Q000031:analogs & derivatives* / Q000378:metabolism*; D006247:Harmine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D011869:Radioligand Assay; D015398:Signal Transduction
chemical_list: D000316:Adrenergic alpha-Agonists; D002243:Carbolines; D008024:Ligands; D006247:Harmine; C005010:harman; D003000:Clonidine