Endogenous beta-carbolines as clonidine-displacing substances.
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.
Robinson
E S J
ES
Psychopharmacology Unit, School of Medical Sciences, University Walk, Bristol BS8 1TD, UK.
Anderson
N J
NJ
Crosby
J
J
Nutt
D J
DJ
Hudson
A L
AL
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
D000316:Adrenergic alpha-Agonists; D002243:Carbolines; D008024:Ligands; D006247:Harmine; C005010:harman; D003000:Clonidine