SM-130686 explained

SM-130686 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-130686 and other GHSR agonists, even though no drugs from this class have yet progressed to clinical use.^[5]

See also

• List of growth hormone secretagogues

Notes and References

1. Tokunaga T, Hume WE, Nagamine J, Kawamura T, Taiji M, Nagata R . Structure-activity relationships of the oxindole growth hormone secretagogues . Bioorganic & Medicinal Chemistry Letters . 15 . 7 . 1789–92 . April 2005 . 15780607 . 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 . 6 . Pharmacological profile of a new orally active growth hormone secretagogue, SM-130686 . The Journal of Endocrinology . 171 . 3 . 481–9 . December 2001 . 11739014 . 10.1677/joe.0.1710481 . free .
3. Tokunaga T, Hume WE, Umezome T, Okazaki K, Ueki Y, Kumagai K, Hourai S, Nagamine J, Seki H, Taiji M, Noguchi H, Nagata R . 6 . Oxindole derivatives as orally active potent growth hormone secretagogues . Journal of Medicinal Chemistry . 44 . 26 . 4641–9 . December 2001 . 11741481 . 10.1021/jm0103763 .
4. 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 & High Throughput Screening . 9 . 3 . 187–96 . March 2006 . 16533152 . 10.2174/138620706776055548 .
5. 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 . 20 . 22 . 3393–402 . 17051614 . 10.1002/rcm.2758 . 2006 . 2006RCMS...20.3393T .