Kapromorelin

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Kapromorelin
(IUPAC) ime
N-[(2R)-1-[(3aR)-2-methyl-3-oxo-3a-(phenylmethyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-(phenylmethoxy)propan-2-yl]-2-amino-2-methylpropanamide
Klinički podaci
Identifikatori
CAS broj 193273-66-4
ATC kod nije dodeljen
PubChem[1][2] 216208
Hemijski podaci
Formula C28H35N5O4 
Mol. masa 505.269 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije 2.4 časa[3]
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Kapromorelin (CP-424,391) je lek koji razvija kompanija Pfizer.[4][5] On izaziva izlučivanje hormona rasta. Analogan je grelinu, koji stimuliše telo da izlučuje hormon rasta na način sličan izlučivanja tog hormon tokom puberteta i mladosti. Inicijalna ispitivanja su pokazala da lek direktno povišava nivoe insulinu sličnog faktora rasta 1 (IGF-1) i hormona rasta.[6]

Ovaj lek se razmatra za moguću primenu kod ljudi u poznim godinama kod kojih su nivoi hormona rasta niski i koji imaju manje čiste mišićne mase, što može da dovede do slabosti i krhkosti.[7]

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Literatura[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Khojasteh-Bakht SC, O'donnell JP, Fouda HG, Potchoiba MJ. Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats. Drug Metabolism and Disposition. 2005 Jan;33(1):190-9. PMID 15486077
  4. Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, Cook ER, DiBrino JN, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Lewis SK, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, Pettersen JC, DaSilva-Jardine PA, Wilson TC, Thompson DD. Discovery and biological characterization of capromorelin analogues with extended half-lives. Bioorganic and Medicinal Chemistry Letters. 2002 Nov 18;12(22):3279-82. PMID 12392732
  5. Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorganic and Medicinal Chemistry. 2003 Feb 20;11(4):581-90. PMID 12538023
  6. Pan LC, Carpino PA, Lefker BA, Ragan JA, Toler SM, Pettersen JC, Nettleton DO, Ng O, Pirie CM, Chidsey-Frink K, Lu B, Nickerson DF, Tess DA, Mullins MA, MacLean DB, DaSilva-Jardine PA, Thompson DD. Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine growth hormone secretagogue. Endocrine. 2001 Feb;14(1):121-32. PMID 11322494
  7. Thompson DD. Aging and sarcopenia. Journal of Musculoskeletal and Neuronal Interactions. 2007 Oct-Dec;7(4):344-5. PMID 18094505

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