852319-26-7Relevant academic research and scientific papers
Melanocortin receptor ligands
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Page/Page column 12; 13, (2008/06/13)
The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W1 is a carbocyclic unit, and W2 is a heteroatom comprising unit.
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 (2007/10/03)
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.
