bms-193885 and 1-4-dihydropyridine

bms-193885 has been researched along with 1-4-dihydropyridine* in 1 studies

Other Studies

1 other study(ies) available for bms-193885 and 1-4-dihydropyridine

Article	Year
Dihydropyridine neuropeptide Y Y1 receptor antagonists 2. bioisosteric urea replacements. Bioorganic & medicinal chemistry, 2004, Jan-15, Volume: 12, Issue:2 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). Topics: Caco-2 Cells; Cell Membrane Permeability; Cells, Cultured; Dihydropyridines; Drug Evaluation, Preclinical; Guanidines; Humans; Phenylurea Compounds; Receptors, Neuropeptide Y; Stereoisomerism; Structure-Activity Relationship; Urea	2004

Article

Year

Dihydropyridine neuropeptide Y Y1 receptor antagonists 2. bioisosteric urea replacements.

Bioorganic & medicinal chemistry, 2004, Jan-15, Volume: 12, Issue:2

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).

Topics: Caco-2 Cells; Cell Membrane Permeability; Cells, Cultured; Dihydropyridines; Drug Evaluation, Preclinical; Guanidines; Humans; Phenylurea Compounds; Receptors, Neuropeptide Y; Stereoisomerism; Structure-Activity Relationship; Urea

2004