SM-130,686 je lek koji deluje kao potentan, oralno aktivan stimulator izlučivanja hormona rasta,[3] sa aproksimativno polovinom potentnosti endogenog agonista grelina.[4][5] On proizvodi povećanje mišićne mase i umanjenje telesne masnoće koje je zavisno od doze. SM-130,686 se ispituje za potencijalnu primenu u lečenju nedostatka hormona rasta i drugih oboljenja.[6]

SM-130,686
(IUPAC) ime
(+)-(3S)-3-(2-hlorofenil)-1-[2-(dietilamino)etil]-3-hidrokso-2-okso-4-(trifluorometil)indolin-6-karboksamid
Klinički podaci
Identifikatori
ATC kod ?
PubChem[1][2] 9890863
Hemijski podaci
Formula C22H23ClF3N3O3 
Mol. masa 469.884 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Zabrinutost oko njegove potencijalne upotrebe za povećanje performance atletičara je dovela do razvoja urinskog testa za SM-130,686 i druge izlučivače hormona rasta, mada lekovi iz ove klase još uvek nisu u kliničkoj upotrebi.[7]

Vidi još uredi

Reference uredi

  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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  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. Tokunaga T, Hume WE, Nagamine J, Kawamura T, Taiji M, Nagata R. Structure-activity relationships of the oxindole growth hormone secretagogues. Bioorganic and Medicinal Chemistry Letters. 2005 Apr 1;15(7):1789-92. PMID 15780607
  4. Nagamine J, Nagata R, Seki H, Nomura-Akimaru N, Ueki Y, Kumagai K, Taiji M, Noguchi H. Pharmacological profile of a new orally active growth hormone secretagogue, SM-130686. Journal of Endocrinology. 2001 Dec;171(3):481-9. PMID 11739014
  5. Tokunaga T, Hume WE, Umezome T, Okazaki K, Ueki Y, Kumagai K, Hourai S, Nagamine J, Seki H, Taiji M, Noguchi H, Nagata R. Oxindole derivatives as orally active potent growth hormone secretagogues. Journal of Medicinal Chemistry. 2001 Dec 20;44(26):4641-9. PMID 11741481
  6. Nagamine J, Kawamura T, Tokunaga T, Hume WE, Nagata R, Nakagawa T, Taiji M. Synthesis and pharmacological profile of an orally-active growth hormone secretagogue, SM-130686. Combinatorial Chemistry and High Throughput Screening. 2006 Mar;9(3):187-96. PMID 16533152
  7. Thevis M, Wilkens F, Geyer H, Schänzer W. Determination of therapeutics with growth-hormone secretagogue activity in human urine for doping control purposes. Rapid Communications in Mass Spectrometry. 2006;20(22):3393-402. PMID 17051614

Spoljašnje veze uredi

Šablon:Neuropeptidni ligandi