SM-130,686
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| Systematic (IUPAC) name | |
|---|---|
|
(+)-(3S)-3-(2-chlorophenyl)-1-[2-(diethylamino)ethyl]-3-hydroxo-2-oxo-4-(trifluoromethyl)indoline-6-carboxamide | |
| Identifiers | |
| ATC code | None |
| PubChem | CID 9890863 |
| Chemical data | |
| Formula | C22H23ClF3N3O3 |
| Molar mass | 469.884 g/mol |
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| (verify) | |
SM-130,686 is a small-molecule drug which acts as a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue,[1] with around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release.[2][3] It produces dose-dependent increases in muscle mass and decrease in body fat, and is under investigation for the treatment of growth hormone deficiency and other medical conditions.[4] Concerns about its potential use as a performance-enhancing drug for athletes have led to the development of urine tests for SM-130,686 and other GHSR agonists, even though no drugs from this class have yet progressed to clinical use.[5]
See also
- Anamorelin
- Capromorelin
- Examorelin (hexarelin)
- GHRP-6 (SKF-110679)
- Ibutamoren (MK-677)
- Ipamorelin
- Macimorelin
- Pralmorelin (GHRP-2)
- Relamorelin
- Tabimorelin
References
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
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