| Literature DB >> 14723969 |
Graham S Poindexter1, Marc A Bruce, J Guy Breitenbucher, Mendi A Higgins, S-Y Sit, Jeffrey L Romine, Scott W Martin, Sally A Ward, Rachel T McGovern, Wendy Clarke, John Russell, Ildiko Antal-Zimanyi.
Abstract
Structure-activity studies around the urea linkage in BMS-193885 (4a) identified the cyanoguanidine moiety as an effective urea replacement in a series of dihydropyridine NPY Y(1) receptor antagonists. In comparison to urea 4a (K(i)=3.3 nM), cyanoguanidine 20 (BMS-205749) displayed similar binding potency at the Y(1) receptor (K(i)=5.1 nM) and full functional antagonism (K(b)=2.6 nM) in SK-N-MC cells. Cyanoguanidine 20 also demonstrated improved permeability properties in Caco-2 cells in comparison to urea 4a (43 vs 19 nm/s).Entities:
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Year: 2004 PMID： 14723969 DOI： 10.1016/j.bmc.2003.10.016
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641