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
  • 1. Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. [email protected]
PMID: 12238918 DOI: 10.1021/jm025550h
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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