Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.

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  • Author(s): Whitlock GA;Whitlock GA; Brennan PE; Roberts LR; Stobie A
  • Source:
    Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Jun 01; Vol. 19 (11), pp. 3118-21. Date of Electronic Publication: 2009 Apr 07.
  • Publication Type:
    Journal Article
  • Language:
    English
  • Additional Information
    • Source:
      Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
    • Publication Information:
      Publication: Oxford : Elsevier Science Ltd
      Original Publication: Oxford ; New York : Pergamon Press, c1991-
    • Subject Terms:
      Adrenergic alpha-1 Receptor Agonists*; Imidazoles/*chemistry; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Adrenergic alpha-2 Receptor Agonists ; Animals ; Cell Line ; Dogs ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/pharmacokinetics ; Receptors, Adrenergic, alpha-1/metabolism ; Receptors, Adrenergic, alpha-2/metabolism
    • Abstract:
      Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity.
    • Accession Number:
      0 (ADRA1A protein, human)
      0 (ADRA1B protein, human)
      0 (ADRA1D protein, human)
      0 (ADRA2A protein, human)
      0 (ATP Binding Cassette Transporter, Subfamily B, Member 1)
      0 (Adrenergic alpha-1 Receptor Agonists)
      0 (Adrenergic alpha-2 Receptor Agonists)
      0 (Imidazoles)
      0 (Receptors, Adrenergic, alpha-1)
      0 (Receptors, Adrenergic, alpha-2)
    • Publication Date:
      Date Created: 20090428 Date Completed: 20090717 Latest Revision: 20181201
    • Publication Date:
      20240829
    • Accession Number:
      10.1016/j.bmcl.2009.03.162
    • Accession Number:
      19394220