• Corpus ID: 26092861

Characterization of subtypes of alpha-2 adrenoceptors in the human brain.

  title={Characterization of subtypes of alpha-2 adrenoceptors in the human brain.},
  author={Gregory A. Ordway and S M Jaconetta and Angelos Halaris},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={264 2},
Radioligand binding studies have demonstrated that oxymetazoline has a high affinity for alpha-2A receptors, but lower affinities for alpha-2B and alpha-2C receptors. In contrast, prazosin has high affinity for alpha-2B and alpha-2C receptors, but relatively lower affinity for alpha-2A receptors. We exploited the respective selectivity of oxymetazoline and prazosin for alpha-2A and alpha-2B/2C adrenoceptors, respectively, to describe pharmacologically and to locate neuroanatomically alpha-2… 
Antipsychotic drug affinities at α2-adrenoceptor subtypes in post-mortem human brain
Assessment of the ability of three classical and four 'atypical' antipsychotic drugs to displace binding of [3H]RX821002 to α2-adrenoceptors in human post-mortem brain tissue found the new antipsychotics showed the greatest selectivity for this receptor site.
Actions of α2 adrenoceptor ligands at α2A and 5-HT1A receptors: the antagonist, atipamezole, and the agonist, dexmedetomidine, are highly selective for α2A adrenoceptors
The agonist DMT and the antagonist atipamezole are the ligands of choice to distinguish α2-mediated from 5- HT1A-mediated actions, whilst several of the other compounds show only low or modest selectivity for α2A over 5-HT1A receptors; caution should be exercised in experimental and clinical interpretation of the actions of traditionally employed α2 ligands.
α2‐Adrenoceptor Subtypes Identified by [3H]RX821002 Binding in the Human Brain: The Agonist Guanoxabenz Does Not Discriminate Different Forms of the Predominant α2A Subtype
The results indicate that in the human brain the predominant α2‐adrenoceptor is of the α2A subtype and that this functionally relevant receptor subtype is not heterogeneous in nature.