beta-carboline binding to imidazoline receptors

Drug Alcohol Depend. 2001 Oct 1;64(2):203-8. doi: 10.1016/s0376-8716(01)00123-5.


A series of beta-carbolines were prepared and their affinities for imidazoline (I(1) and I(2)) sites evaluated. Selected compounds were also examined at alpha(2)-adrenoceptors. Some of the beta-carbolines were found to bind with high affinity to I(2)-sites and this affinity was dependent on both the planarity of the molecule and the presence of the aryl ring substituents. Good I(1)-affinity was observed with two of the compounds but none of the tested compounds bound to alpha(2)-adrenoceptors. The hallucinogenic properties of beta-carbolines have been linked to activity at 5-HT receptors, in particular 5-HT(2), 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 I(2)-ligands, suggests that imidazoline sites may be interesting new targets in drug abuse research.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Carbolines / pharmacokinetics*
  • Culture Techniques
  • Imidazoline Receptors
  • Kidney
  • Male
  • Rats
  • Rats, Wistar
  • Receptors, Adrenergic, alpha-2 / metabolism
  • Receptors, Drug / metabolism*
  • Structure-Activity Relationship


  • Carbolines
  • Imidazoline Receptors
  • Receptors, Adrenergic, alpha-2
  • Receptors, Drug
  • imidazoline I1 receptors