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…

Index: 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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Citation Number: 4

Abstract

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 ...