159634-93-2Relevant academic research and scientific papers
Synthesis and biological activities of phenyl piperazine- based peptidomimetic growth hormone secretagogues
Barakat, Khaled J.,Cheng, Kang,Chan, Wanda W.-S,Butler, Bridget S.,Jacks, Thomas M.,Schleim, Klaus D.,Hora Jr., Donald F.,Hickey, Gerard J.,Smith, Roy G.,Patchett, Arthur A.,Nargund, Ravi P.
, p. 1431 - 1436 (2007/10/03)
A new class of potent, orally active phenyl piperazine-based GH secretagogues have been discovered from attempts to mimic the arrangement of the phenyl substitutent in the spiroindanyl piperidine and spiroindoline sulfonamide privileged structures of 4 and 1, respectively. The best of these compounds, 18 (EC50 = 2.8 nM) is nearly as potent as MK-0677 for releasing GH from rat pituitary cells.
Tripeptide growth hormone secretagogues
Yang, Lihu,Morriello, Greg,Pan, Yanping,Nargund, Ravi P.,Barakat, Khaled,Prendergast, Kristine,Cheng, Kang,Chan, Wanda W.-S.,Smith, Roy G.,Patchett, Arthur A.
, p. 759 - 764 (2007/10/03)
A series of C-terminus capped dipeptides and tripeptides was synthesized as growth hormone (GH) sccretagogues. Among them, tripeptide Aib-D-Trp-D-homoPhe-OEt showed low nanomolar activity in the rat pituitary assay. Thus, we have demonstrated that the GH secretagogue activity of the hexa- hepta-GH releasing peptides can be mimicked at the tripeptide level.
