SM-130,686

SM-130,686
IUPAC ime
	(+)-(3S)-3-(2-hlorofenil)-1-[2-(dietilamino)etil]-3-hidrokso-2-okso-4-(trifluorometil)indolin-6-karboksamid
Identifikatori
PubChem	CID 9890863
Hemijski podaci
Formula	C22H23ClF3N3O3
Molarna masa	469.884 g/mol
	SMILES FC(F)(F)c3c1c(cc(c3)C(N)=O)N(CCN(CC)CC)C(=O)C1(O)c2ccccc2Cl; ;

SM-130,686 je lek koji deluje kao potentan, oralno aktivan stimulator izlučivanja hormona rasta,^[1] sa približno polovinom potentnosti endogenog agonista grelina.^[2]^[3] 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.^[4]

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.^[5]

Vidi još уреди

Reference уреди

^ Tokunaga, T.; Hume, W. E.; Nagamine, J.; Kawamura, T.; Taiji, M.; Nagata, R. (2005). „Structure-activity relationships of the oxindole growth hormone secretagogues”. Bioorganic & Medicinal Chemistry Letters. 15780607 (7): 1789—1792. PMID 15780607. doi:10.1016/j.bmcl.2005.02.042.
^ Nagamine, J.; Nagata, R.; Seki, H.; Nomura-Akimaru, N.; Ueki, Y.; Kumagai, K.; Taiji, M.; Noguchi, H. (2001). „Pharmacological profile of a new orally active growth hormone secretagogue, SM-130686”. The Journal of Endocrinology. 11739014 (3): 481—489. PMID 11739014. S2CID 46695362. doi:10.1677/joe.0.1710481.
^ Tokunaga, T.; Hume, W. E.; Umezome, T.; Okazaki, K.; Ueki, Y.; Kumagai, K.; Hourai, S.; Nagamine, J.; Seki, H.; Taiji, M.; Noguchi, H.; Nagata, R. (2001). „Oxindole derivatives as orally active potent growth hormone secretagogues”. Journal of Medicinal Chemistry. 11741481 (26): 4641—4649. PMID 11741481. doi:10.1021/jm0103763.
^ Nagamine, J.; Kawamura, T.; Tokunaga, T.; Hume, W. E.; Nagata, R.; Nakagawa, T.; Taiji, M. (2006). „Synthesis and pharmacological profile of an orally-active growth hormone secretagogue, SM-130686”. Combinatorial Chemistry & High Throughput Screening. 16533152 (3): 187—196. PMID 16533152. doi:10.2174/138620706776055548.
^ Thevis, M.; Wilkens, F.; Geyer, H.; Schänzer, W. (2006). „Determination of therapeutics with growth-hormone secretagogue activity in human urine for doping control purposes”. Rapid Communications in Mass Spectrometry : RCM. 17051614 (22): 3393—3702. Bibcode:2006RCMS...20.3393T. PMID 17051614. doi:10.1002/rcm.2758.

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[1] Tokunaga, T.; Hume, W. E.; Nagamine, J.; Kawamura, T.; Taiji, M.; Nagata, R. (2005). „Structure-activity relationships of the oxindole growth hormone secretagogues”. Bioorganic & Medicinal Chemistry Letters. 15780607 (7): 1789—1792. PMID 15780607. doi:10.1016/j.bmcl.2005.02.042.

[2] Nagamine, J.; Nagata, R.; Seki, H.; Nomura-Akimaru, N.; Ueki, Y.; Kumagai, K.; Taiji, M.; Noguchi, H. (2001). „Pharmacological profile of a new orally active growth hormone secretagogue, SM-130686”. The Journal of Endocrinology. 11739014 (3): 481—489. PMID 11739014. S2CID 46695362. doi:10.1677/joe.0.1710481.

[3] Tokunaga, T.; Hume, W. E.; Umezome, T.; Okazaki, K.; Ueki, Y.; Kumagai, K.; Hourai, S.; Nagamine, J.; Seki, H.; Taiji, M.; Noguchi, H.; Nagata, R. (2001). „Oxindole derivatives as orally active potent growth hormone secretagogues”. Journal of Medicinal Chemistry. 11741481 (26): 4641—4649. PMID 11741481. doi:10.1021/jm0103763.

[4] Nagamine, J.; Kawamura, T.; Tokunaga, T.; Hume, W. E.; Nagata, R.; Nakagawa, T.; Taiji, M. (2006). „Synthesis and pharmacological profile of an orally-active growth hormone secretagogue, SM-130686”. Combinatorial Chemistry & High Throughput Screening. 16533152 (3): 187—196. PMID 16533152. doi:10.2174/138620706776055548.

[5] Thevis, M.; Wilkens, F.; Geyer, H.; Schänzer, W. (2006). „Determination of therapeutics with growth-hormone secretagogue activity in human urine for doping control purposes”. Rapid Communications in Mass Spectrometry : RCM. 17051614 (22): 3393—3702. Bibcode:2006RCMS...20.3393T. PMID 17051614. doi:10.1002/rcm.2758.

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