Pharmacological characterisation of imidazoline receptors in the human central nervous system and cell lines

Project Details

Description

Certain alpha2-adrenergic lipands are also capable to bind to imidazoline receptors. These are divided into 2 groups: l1 and l2 receptors. The role of the l1 receptors in the homeostesis of blood pressure is well documented and the antihypertensive action of l1 lipands such as clonidine and rilmenidine has been highlighted in various clinical trials. The implication of l1 receptors in the antihypertensive action of moxonidine has been suggested but in vitro studies have not provided solid evidence for this. The role of the l2 receptors and their relation to the l1 receptors remains until today uncertain as well. The purpose of our project is to elucidate~the pharmacological profile and thepotential heterogeneity of both binding sites as well as their molecular relationship in the human as follows: a.) comparative pharmacological characterisation of both receptors in different brain regions of the humar; and in human cell lines by radiolipand binding (competitions, saturation, kinetics). b.) investipation of the regional distribution of receptor subtypes in the human CNS by autoradiography (making use of the discriminating power of subtype- selectieve liga nds) c.) comparison of different theoretical models (o.a. allosteric interactions) to unravel the relationship between l1 en l2 receptors.
AcronymOZR231
StatusFinished
Effective start/end date1/01/9831/12/99

Flemish discipline codes

  • Basic sciences
  • Biological sciences

Keywords

  • medicine
  • biology