Historique
Périodique
Beta-carboline binding to imidazoline receptors
(Fixation des Béta-carbolines aux récepteurs d'imidazoline)
Auteur(s) :
HUSBAND, S. M. ;
GLENNON, R. A. ;
GORGERAT S. ;
GOUGH R. ;
TYACKE R. ;
CROSBY, J. ;
NUTT, D. J. ;
LEWIS, J. W. ;
HUDSON, A. L.
Année
2001
Page(s) :
203-208
Langue(s) :
Anglais
Domaine :
Drogues illicites / Illicit drugs
Discipline :
PRO (Produits, mode d'action, méthode de dépistage / Substances, action mode, screening methods)
Note générale :
Drug and Alcohol Dependence, 2001, 64, (2), 203-208
Résumé :
A series of beta-carbolines were prepared and their affinities for imidazoline (i1, and i2) sites evaluated. Selected compounds were also examined at x2-adrenoceptors. Some of the beta-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 x2-adrenoceptors. The hallucinogenic properties of beta-carbolines have been linked to activity at 5-HT2 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. (Author's abstract.)
Affiliation :
Dept Pharmacy Pharmacol., Univ. Bath, BA2 7AY
Royaume-Uni. United Kingdom.
Royaume-Uni. United Kingdom.