Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Carpino, P.A. et al.

Carpino, Lefker, Toler, Pan, Hadcock, Cook, DiBrino, Campeta, DeNinno, Chidsey-Frink, Hada, Inthavongsay, Mangano, Mullins, Nickerson, Ng, Pirie, Ragan, Rose, Tess, Wright, Yu, Zawistoski, DaSilva-Jardine, Wilson, Thompson,

Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.

Novel pyrazolinone-piperidine dipeptide derivatives were synthesized and evaluated as growth hormone secretagogues (GHSs). Two analogues, capromorelin (5, CP-424391-18, hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM) and the des-methyl analogue 5c (hGHS-R1a K(i)=17 nM, rat pituicyte EC(50)=3 nM), increased plasma GH levels in an anesthesized rat model, with ED(50) values less than 0.05 mg/kg iv. Capromorelin showed enhanced intestinal absorption in rodent models and exhibited superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%]. This short-duration GHS was orally active in canine models and was selected as a development candidate for the treatment of musculoskeletal frailty in elderly adults.[1]

References

Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Carpino, P.A., Lefker, B.A., Toler, S.M., Pan, L.C., Hadcock, J.R., Cook, E.R., DiBrino, J.N., Campeta, A.M., DeNinno, S.L., Chidsey-Frink, K.L., Hada, W.A., Inthavongsay, J., Mangano, F.M., Mullins, M.A., Nickerson, D.F., Ng, O., Pirie, C.M., Ragan, J.A., Rose, C.R., Tess, D.A., Wright, A.S., Yu, L., Zawistoski, M.P., DaSilva-Jardine, P.A., Wilson, T.C., Thompson, D.D. Bioorg. Med. Chem. (2003) [Pubmed]

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