1. Academic Validation
  2. N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine

N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine

  • J Med Chem. 2002 Sep 26;45(20):4395-7. doi: 10.1021/jm025550h.
Robert J Altenbach 1 Albert Khilevich Michael D Meyer Steven A Buckner Ivan Milicic Anthony V Daza Michael E Brune Alyssa B O'Neill Donna M Gauvin John C Cain Masaki Nakane Mark W Holladay Michael Williams Jorge D Brioni James P Sullivan
Affiliations

Affiliation

  • 1 Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. Robert.j.altenbach@abbott.com
Abstract

N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1) is a novel alpha(1) agent having the unique profile of alpha(1A) (rabbit urethra, EC(50) = 0.60 microM) agonism with alpha(1B) (rat spleen, pA(2) = 5.4) and alpha(1D) (rat aorta, pA(2) = 6.2) antagonism. An in vivo dog model showed 1 to be more selective for the urethra over the vasculature than A-61603 (2), ST-1059 (3, the active metabolite of midodrine), and phenylpropanolamine (4).

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