748808-87-9Relevant academic research and scientific papers
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines
Tran, Joe A.,Pontillo, Joseph,Arellano, Melissa,White, Nicole S.,Fleck, Beth A.,Marinkovic, Dragan,Tucci, Fabio C.,Lanier, Marion,Nelson, Jodie,Saunders, John,Foster, Alan C.,Chen, Chen
, p. 833 - 837 (2007/10/03)
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 Ki 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 (IC50 = 300 nM).
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor
Pontillo, Joseph,Tran, Joseph A.,Arellano, Melissa,Fleck, Beth A.,Huntley, Rajesh,Marinkovic, Dragan,Lanier, Marion,Nelson, Jodie,Parker, Jessica,Saunders, John,Tucci, Fabio C.,Jiang, Wanlong,Chen, Caroline W.,White, Nicole S.,Foster, Alan C.,Chen, Chen
, p. 4417 - 4423 (2007/10/03)
SAR studies on a series of piperazinebenzenes directed toward the human melanocortin-4 receptor resulted in potent MC4R agonists. Replacement of the triazole moiety of an initial lead 4 by a basic nitrogen baring a lipophilic side-chain increased the binding affinities of these compounds. Analogs bearing an additional hetero-atom in the side-chain possessed good agonist potency. Thus, 11h had a Ki of 11 nM, and 13g exhibited an EC50 of 3.8 nM and a Ki of 6.4 nM.
