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 |
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| Authors: | Altenbach Robert J Khilevich Albert Meyer Michael D Buckner Steven A Milicic Ivan Daza Anthony V Brune Michael E O'Neill Alyssa B Gauvin Donna M Cain John C Nakane Masaki Holladay Mark W Williams Michael Brioni Jorge D Sullivan James P |
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| Affiliation: | Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. Robert.j.altenbach@abbott.com |
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| 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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