| 18674898 |
Hilfiker MA, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ: Aminomethylpiperazines as selective urotensin antagonists. . Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. Epub 2008 Jul 20.
Aminomethylpiperazines, reported previously as being kappa-opioid receptor agonists, were identified as lead compounds in the development of selective urotensin receptor antagonists. Optimized substitution of the piperazine moiety has provided high affinity urotensin receptor antagonists with greater than 100-fold selectivity over the kappa-opioid receptor. Select compounds were found to inhibit urotensin-induced vasoconstriction in isolated rat aortic rings consistent with the hypothesis that an urotensin antagonist may be useful for the treatment of hypertension. |
82(1,1,1,2) |