| 15664867 |
Tran JA, Pontillo J, Arellano M, White NS, Fleck BA, Marinkovic D, Tucci FC, Lanier M, Nelson J, Saunders J, Foster AC, Chen C: Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines. Bioorg Med Chem Lett. 2005 Feb 1;15(3):833-7.
SAR studies of a series of piperazinebenzylamines resulted in identification of potent agonists and antagonists of the human melanocortin-4 receptor. Thus, the 1,2,3,4-tetrahydroisoquinolin-1-ylacetyl compound 12e and the quinolin-3-ylcarbonyl analogue 12l possessed K (i) values of 6.3 and 4.5 nM, respectively. Interestingly, 12e was a full agonist with an EC (50) value of 31 nM, and 12l was a weak partial agonist (IA=17%) and functioned as an antagonist (IC (50)=300 nM). |
2(0,0,0,2) |