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) 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).
Mesh Terms:
Adrenergic alpha-Agonists, Adrenergic alpha-Antagonists, Animals, Aorta, Blood Pressure, Dogs, Female, Imidazoles, In Vitro Techniques, Ligands, Midodrine, Phenylpropanolamine, Rabbits, Radioligand Assay, Rats, Receptors, Adrenergic, alpha-1, Spleen, Structure-Activity Relationship, Sulfonamides, Urethra
Adrenergic alpha-Agonists, Adrenergic alpha-Antagonists, Animals, Aorta, Blood Pressure, Dogs, Female, Imidazoles, In Vitro Techniques, Ligands, Midodrine, Phenylpropanolamine, Rabbits, Radioligand Assay, Rats, Receptors, Adrenergic, alpha-1, Spleen, Structure-Activity Relationship, Sulfonamides, Urethra
J. Med. Chem.
Date: Sep. 26, 2002
PubMed ID: 12238918
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