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).
MeSH terms
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Adrenergic alpha-Agonists / chemical synthesis*
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Adrenergic alpha-Agonists / chemistry
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Adrenergic alpha-Agonists / pharmacology
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / pharmacology
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Animals
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Aorta / drug effects
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Aorta / physiology
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Blood Pressure / drug effects
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Dogs
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Female
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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In Vitro Techniques
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Ligands
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Midodrine / pharmacology*
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Phenylpropanolamine / pharmacology*
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Rabbits
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Radioligand Assay
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Rats
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Receptors, Adrenergic, alpha-1 / drug effects*
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Spleen / drug effects
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Spleen / physiology
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Urethra / drug effects
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Urethra / physiology
Substances
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ABT 866
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Adrenergic alpha-Agonists
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Adrenergic alpha-Antagonists
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Imidazoles
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Ligands
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Receptors, Adrenergic, alpha-1
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Sulfonamides
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Phenylpropanolamine
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Midodrine