These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


PUBMED FOR HANDHELDS

Search MEDLINE/PubMed


  • Title: Structural determinants of selective affinity for brain D-1 dopamine receptors within a series of 1-phenyl-1H-3-benzazepine analogues of SK&F 38393 and SCH 23390.
    Author: O'Boyle KM, Waddington JL.
    Journal: Eur J Pharmacol; 1985 Sep 24; 115(2-3):291-5. PubMed ID: 2866103.
    Abstract:
    A series of 1-phenyl-1H-3 benzazepine analogues of the D-1 agonist SK&F 38393 and of the D-1 antagonist SCH 23390 were compared for their relative abilities to displace the binding of [3H]piflutixol and [3H]spiperone to striatal D-1 and D-2 receptors respectively. The benzazepine analogues varied in substitutions at the 3- and 7-positions which distinguish SK & 38393 from SCH 23390. Substitutions at these positions critically influenced affinity for D-1 receptors over a 2000-fold range but influenced affinity for D-2 receptors over only a 30-fold range. 7-Substituents prominently increased affinity and selectivity for D-1 receptors with a rank order of Br = Cl much greater than CH3 greater than H greater than OH. 3-Methylation had a less marked and less selective action to increase affinity for D-1 receptors. Such structural relationships may aid the definition of the topography of brain D-1 receptors and the development of improved selective agents.
    [Abstract] [Full Text] [Related] [New Search]