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MK-677 Ibutamoren Mesylate is a compound which acts as a potent, orally active GH (growth hormone) secretagogue, mimicking the action of endogenous ghrelin (ghrelin mimetic). Investigational names: Ibutamoren (MK-677, Ibutamoren Mesylate, L-163,191)
In normal subjects dietary energy restriction results in catabolic response associated with the loss of nitrogen, decrease in IGF-I, increase in GH, and GH resistance. However, this resistance is not absolute since administration of exogenous GH will stimulate increase in IGF-I levels and nitrogen retention.
MK-677 is a non-peptide spiropiperidine and is functionally indistinguishable in vitro and in vivo from the GHRP-6. However, MK-677 stimulates GH release through a pituitary and hypothalamic receptors (different from the GH-releasing hormone receptors), and is able to sustain GH plasma levels and IGF-I release without affecting endogenous cortisol. This compound is being developed as a potential therapy in growth hormone deficient children or elderly adults. It was shown to be able to increase muscle mass and bone mineral density therefore can be used to treat frailty in the elderly. In addition, MK-677 alters metabolism of body fat so may be applied in the treatment of obesity.
Short-term oral administration of Ibutamoren may be used as adjunctive therapy in certain catabolic states: MK-677 is able to reverse protein catabolism caused by dietary caloric restriction since the degree of growth hormone stimulation is sufficient to improve nitrogen balance. In healthy adult males, Ibutamoren is more effective than GHRH, producing a mean peak GH concentration of 22.1μg/L after an oral dose of 25mg.
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