Abstract
Drug and Alcohol Dependence 64 (2001) 203–208
B-carboline binding to imidazoline receptors
Stephen M. Husbands a,*, Richard A. Glennon b, Stephane Gorgerat c,
Rhianon Gough d, Robin Tyacke d, John Crosby c, David J. Nutt d, John W. Lewis
c,
Alan L. Hudson d
a Department of Pharmacy and Pharmacology, Uniersity of Bath, Bath, BA2 7AY,
UK
b Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth
Uniersity, Box 980540, Richmond, VA 23298, USA
c School of Chemistry, Uniersity of Bristol, Bristol, BS8 1TS, UK
d Psychopharmacology Unit, Uniersity of Bristol, Bristol, BS8 1TD, UK
Received 29 September 2000; accepted 24 January 2001
Abstract
A series of -carbolines were prepared and their affinities for imidazoline
(I1 and I2) sites evaluated. Selected compounds were
also examined at 2-adrenoceptors. Some of the -carbolines were found to
bind with high affinity to I2-sites and this affinity was
dependent on both the planarity of the molecule and the presence of the aryl
ring substituents. Good I1-affinity was observed with
two of the compounds but none of the tested compounds bound to 2-adrenoceptors.
The hallucinogenic properties of
-carbolines have been linked to activity at 5-HT receptors, in particular
5-HT2, however, it is apparent from this study that many
of these compounds display substantially higher affinity for the imidazoline
sites. This finding, and those showing modulation of
some behavioural effects of morphine by I2-ligands, suggests that imidazoline
sites may be interesting new targets in drug abuse
research. © 2001 Elsevier Science Ireland Ltd. All rights reserved.
Keywords: -carbolines; Harmine; Harmaline; Hallucinogens; Imidazoline binding
sites; SAR
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