N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),<SUP>1</SUP> a Novel α<INF>1</INF>-Adrenoceptor Ligand with an Enhanced in Vitro and in Vivo Profile Relative to Phenylpropanolamine and Midodrine

Authors :: Altenbach, R. J.
Khilevich, A.
Meyer, M. D.
Buckner, S. A.
Milicic, I.
Daza, A. V.
Brune, M. E.
O'Neill, A. B.
Gauvin, D. M.
Cain, J. C.
Nakane, M.
Holladay, M. W.
Williams, M.
Brioni, J. D.
Sullivan, J. P.
Source :: Journal of Medicinal Chemistry; September 2002, Vol. 45 Issue: 20 p4395-4397, 3p
Publication Year :: 2002
Abstract: N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, <BO>1</BO>) is a novel α<INF>1</INF> agent having the unique profile of α<INF>1A</INF> (rabbit urethra, EC<INF>50</INF> = 0.60 μM) agonism with α<INF>1B</INF> (rat spleen, pA<INF>2</INF> = 5.4) and α<INF>1D</INF> (rat aorta, pA<INF>2</INF> = 6.2) antagonism. An in vivo dog model showed <BO>1</BO> to be more selective for the urethra over the vasculature than A-61603 (<BO>2</BO>), ST-1059 (<BO>3</BO>, the active metabolite of midodrine), and phenylpropanolamine (<BO>4</BO>).

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