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Chemical Compound Review:

Capromorelin 2-amino-N-[(2R)-1-[(1R)-1- benzyl-8-methyl...

Synonyms: CHEMBL113313, SureCN1147592, CHEBI:282843, KST-1A2791, AC1Q5JMA, ...

Kitazawa, T. et al., MacAndrew, J.T. et al., Carpino, P.A. et al., Carpino, P.A. et al., Pan, L.C. et al.

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

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Disease relevance of Capromorelin

Thus, the treatment of rabbits for 7 days with CP-424,391 was cardioprotective against ischemia/reperfusion injury [1].

High impact information on Capromorelin

L-NAME turned EFS induced relaxations into cholinergic contractions that were enhanced by ghrelin, GHRP-6, and capromorelin [2].
RESULTS: Ghrelin, GHRP-6, and capromorelin accelerated gastric emptying in an equipotent manner, with bell-shaped dose-response relationships [2].
There was a trend, albeit not significant, for the left ventricular function to recover to a greater extent in CP-424,391-treated rabbits [1].
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%] [3].
New tert-butyl, picolyl and fluorinated analogues of capromorelin (3), a short-acting growth hormone secretagogue (GHS), were prepared as part of a program to identify long-acting GHSs that increase 24-h plasma IGF-1 levels [4].

Gene context of Capromorelin

Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue [5].

Analytical, diagnostic and therapeutic context of Capromorelin

METHODS: In vivo, the dose dependent effects (1-150 nmol/kg) of ghrelin, GHRP-6, and capromorelin on gastric emptying were measured by the 14C octanoic breath test which was adapted for use in mice [2].

References

Efficacy of a growth hormone-releasing peptide mimetic in cardiac ischemia/reperfusion injury. MacAndrew, J.T., Ellery, S.S., Parry, M.A., Pan, L.C., Black, S.C. Eur. J. Pharmacol. (2001) [Pubmed]
Gastric motor effects of peptide and non-peptide ghrelin agonists in mice in vivo and in vitro. Kitazawa, T., De Smet, B., Verbeke, K., Depoortere, I., Peeters, T.L. Gut (2005) [Pubmed]
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]
Discovery and biological characterization of capromorelin analogues with extended half-lives. Carpino, P.A., Lefker, B.A., Toler, S.M., Pan, L.C., Hadcock, J.R., Murray, M.C., Cook, E.R., DiBrino, J.N., DeNinno, S.L., Chidsey-Frink, K.L., Hada, W.A., Inthavongsay, J., Lewis, S.K., 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., Pettersen, J.C., DaSilva-Jardine, P.A., Wilson, T.C., Thompson, D.D. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue. Pan, L.C., Carpino, P.A., Lefker, B.A., Ragan, J.A., Toler, S.M., Pettersen, J.C., Nettleton, D.O., Ng, O., Pirie, C.M., Chidsey-Frink, K., Lu, B., Nickerson, D.F., Tess, D.A., Mullins, M.A., MacLean, D.B., DaSilva-Jardine, P.A., Thompson, D.D. Endocrine (2001) [Pubmed]

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