Synthesis and Structure-Activity Studies on N-[5-(1 H-Imidazol-4-yl)-5, 6, 7, 8-tetrahydro-1-naphthalenyl] methanesulfonamide, an Imidazole-Containing α1A- …

…, XB Searle, F Yang, WH Bunnelle, K Tietje…

文献索引：Altenbach, Robert J.; Khilevich, Albert; Kolasa, Teodozyj; Rohde, Jeffrey J.; Bhatia, Pramila A.; Patel, Meena V.; Searle, Xenia B.; Yang, Fan; Bunnelle, William H.; Tietje, Karin; Bayburt, Erol K.; Carroll, William A.; Meyer, Michael D.; Henry, Rodger; Buckner, Steven A.; Kuk, Jane; Daza, Anthony V.; Milicic, Ivan V.; Cain, John C.; Kang, Chae H.; Ireland, Lynne M.; Carr, Tracy L.; Miller, Thomas R.; Hancock, Arthur A.; Nakane, Masaki; Esbenshade, Timothy A.; Brune, Michael E.; O'Neill, Alyssa B.; Gauvin, Donna M.; Katwala, Sweta P.; Holladay, Mark W.; Brioni, Jorge D.; Sullivan, James P. Journal of Medicinal Chemistry, 2004 , vol. 47, # 12 p. 3220 - 3235

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被引用次数: 4

摘要

Structure-activity studies were performed on the α1A-adrenoceptor (AR) selective agonist N- [5-(1 H-imidazol-4-yl)-5, 6, 7, 8-tetrahydro-1-naphthalenyl] methanesulfonamide (4). Compounds were evaluated for binding activity at the α1A, α1b, α1d, α2a, and α2B subtypes. Functional activity in tissues containing the α1A (rabbit urethra), α1B (rat spleen), α1D (rat aorta), and α2A (rat prostatic vas deferens) was also evaluated. A dog in vivo ...