SYNTHESIS AND IN-VITRO CHARACTERIZATION OF 6,7,8-TETRAHYDRONAPHTHALEN-1-YL]METHANESULFONAMIDE AND ITS ENANTIOMERS - A NOVEL SELECTIVE ALPHA(1A) RECEPTOR AGONIST

The existence of multiple subtypes of the alpha(1) adrenergic receptor has been demonstrated both pharmacologically and by molecular biologi cal cloning techniques. The development of subtype selective antagonis ts has been the focus of much research within the pharmaceutical indus try, and clinical evidence now exists that alpha-1A selective antagoni sts will have utility in the treatment of benign prostatic hyperplasia . However, highly subtype selective agonists are not known. Herein we report the synthesis and pharmacological characterization of 6,7,8-tet rahydronaphthalen-1-yl]methanesulfonamide and its enantiomers, a highl y potent full agonist with excellent selectivity for the alpha(1A) rec eptor subtype.