475095-05-7Relevant academic research and scientific papers
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1- (4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl) piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist
Sebhat, Iyassu K.,Martin, William J.,Ye, Zhixiong,Barakat, Khaled,Mosley, Ralph T.,Johnston, David B. R.,Bakshi, Raman,Palucki, Brenda,Weinberg, David H.,MacNeil, Tanya,Kalyani, Rubana N.,Tang, Rui,Stearns, Ralph A.,Miller, Randy R.,Tamvakopoulos, Constantin,Strack, Alison M.,McGowan, Erin,Cashen, Doreen E.,Drisko, Jennifer E.,Hom, Gary J.,Howard, Andrew D.,MacIntyre, D. Euan,Van der Ploeg, Lex H. T.,Patchett, Arthur A.,Nargund, Ravi P.
, p. 4589 - 4593 (2002)
Synthetic and natural peptides that act as nonselective melanocortin receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity.
Melanocortin subtype 4 receptor agonists: Structure-activity relationships about the 4-alkyl piperidine core
Sebhat, Iyassu K.,Lai, Yingjie,Barakat, Khaled,Ye, Zhixiong,Tang, Rui,Kalyani, Rubana N.,Vongs, Aurawan,MacNeil, Tanya,Weinberg, David H.,Cabello, M. Angeles,Maroto, Marta,Teran, Ana,Fong, Tung M.,Van der Ploeg, Lex H.T.,Patchett, Arthur A.,Nargund, Ravi P.
, p. 5720 - 5723 (2008/04/03)
SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.
