Neveu, Cindy; Lefranc, Benjamin; Tasseau, Olivier; Do-Rego, Jean-Claude; Bourmaud, Adele; Chan, Philippe; Bauchat, Patrick; Marec, Olivier Le; Chuquet, Julien; Guilhaudis, Laure; Boutin, Jean A.; Segalas-Milazzo, Isabelle; Costentin, Jean; Vaudry, Hubert; Baudy-Floc’h, Michele; Vaudry, David; Leprince, Jerome published the artcile< Rational design of a low molecular weight, stable, potent, and long-lasting GPR103 aza-β3-pseudopeptide agonist>, Recommanded Product: 2-(1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidin-4-yl)acetic acid, the main research area is RFamide neuropeptide analog aza pseudopeptide GPR103 agonist synthesis conformation; peptide RFamide neuropeptide aza beta pseudopeptide agonist drug design; calcium mobilizing structure activity appetite depressants hydrogen bond.
26RFa, a novel RFamide neuropeptide, is the endogenous ligand of the former orphan receptor GPR103. Intracerebroventricular injection of 26RFa and its C-terminal heptapeptide, 26RFa(20-26), stimulates food intake in rodents. To develop potent, stable ligands of GPR103 with low mol. weight, we have designed a series of aza-β3-containing 26RFa(20-26) analogs for their propensity to establish intramol. hydrogen bonds, and we have evaluated their ability to increase [Ca2+]i in GPR103-transfected cells. We have identified a compound, [Cmpi21,aza-β3-Hht23]26RFa(21-26), which was 8-fold more potent than 26RFa(20-26) in mobilizing [Ca2+]i. This pseudopeptide was more stable in serum than 26RFa(20-26) and exerted a longer lasting orexigenic effect in mice. This study constitutes an important step toward the development of 26RFa analogs that could prove useful for the treatment of feeding disorders.
Journal of Medicinal Chemistry published new progress about Appetite depressants. 180181-05-9 belongs to class piperidines, and the molecular formula is C22H23NO4, Recommanded Product: 2-(1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidin-4-yl)acetic acid.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem