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N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1), a Novel α1-Adrenoceptor Ligand with an Enhanced in Vitro and in Vivo Profile Relative to Phenylpropanolamine and Midodrine
- Source :
- Journal of Medicinal Chemistry. 45:4395-4397
- Publication Year :
- 2002
- Publisher :
- American Chemical Society (ACS), 2002.
-
Abstract
- N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1) is a novel α1 agent having the unique profile of α1A (rabbit urethra, EC50 = 0.60 μM) agonism with α1B (rat spleen, pA2 = 5.4) and α1D (rat aorta, pA2 = 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).
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 45
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi...........fed10e7e73c83c20fec4310ac0df29e9