363191-04-2Relevant articles and documents
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.
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1- dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl] -2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin su
Ye, Zhixiong,Guo, Liangqin,Barakat, Khaled J.,Pollard, Patrick G.,Palucki, Brenda L.,Sebhat, Iyassu K.,Bakshi, Raman K.,Tang, Rui,Kalyani, Rubana N.,Vongs, Aurawan,Chen, Airu S.,Chen, Howard Y.,Rosenblum, Charles I.,MacNeil, Tanya,Weinberg, David H.,Peng, Qianping,Tamvakopoulos, Constantin,Miller, Randy R.,Stearns, Ralph A.,Cashen, Doreen E.,Martin, William J.,Metzger, Joseph M.,Strack, Alison M.,MacIntyre, D. Euan,Van Der Ploeg, Lex H. T.,Patchett, Arthur A.,Wyvratt, Matthew J.,Nargund, Ravi P.
, p. 3501 - 3505 (2007/10/03)
A novel isoquinuclidine containing selective melanocortin subtype-4 receptor small molecule agonist, 3 (RY764), is reported. Its in vivo characterization revealed mechanism-based food intake reduction and erectile activity augmentation in rodents.