Endogenous β-Carbolines as Clonidine-Displacing Substances

: Endogenous β‐carbolines, such as harmane, are known to occur in mammalian species including humans. Radioligand binding studies have revealed that certain β‐carbolines display high affinity for both I1 and I2 imidazoline‐binding sites (IBS). Functional studies have shown that the β‐carboline harma...

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Bibliographic Details
Published in:Annals of the New York Academy of Sciences 2003-12, Vol.1009 (1), p.157-166
Main Authors: ROBINSON, ESJ, ANDERSON, NJ, CROSBY, J, NUTT, DJ, HUDSON, AL
Format: Article
Language:English
Subjects:
Adrenergic alpha-Agonists - chemistry
Adrenergic alpha-Agonists - metabolism
Animals
b-carboline
Carbolines - chemistry
Carbolines - metabolism
Clonidine - analogs & derivatives
Clonidine - metabolism
clonidine-displacing substance (CDS)
harmane
Harmine - analogs & derivatives
Harmine - chemistry
Harmine - metabolism
Humans
Ligands
Molecular Structure
Radioligand Assay
Signal Transduction
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Summary:: Endogenous β‐carbolines, such as harmane, are known to occur in mammalian species including humans. Radioligand binding studies have revealed that certain β‐carbolines display high affinity for both I1 and I2 imidazoline‐binding sites (IBS). Functional studies have shown that the β‐carboline harmane elicits many characteristics expected of an endogenous ligand IBS. This article discusses the evidence relating to β‐carbolines as endogenous ligands and presents a case for harmane and related compounds as endogenous ligands for IBS.
ISSN:0077-8923
1749-6632
DOI:10.1196/annals.1304.018