MK-0677, also known as Ibutamoren, is a potent, non-peptide, orally active secretagogue that stimulates the secretion of Growth Hormone (GH) by mimicking the action of the endogenous hormone ghrelin. It functions by binding to the ghrelin receptor (GHS-R1a) in the brain, thereby increasing the pulsatile release of GH and subsequently elevating Insulin-like Growth Factor 1 (IGF-1) concentrations without significantly affecting cortisol levels. Clinically, its exploration has centered on its potential for increasing lean body mass, improving bone density, and enhancing sleep quality.
Origin
MK-0677 was developed in the late 20th century by Merck & Co. as part of a research effort to find an orally active compound that could treat growth hormone deficiency and conditions like osteoporosis. The term is the compound’s laboratory code name. Its clinical interest lies in its selective agonism of the ghrelin receptor, distinguishing it from direct GH administration.
Mechanism
The compound acts as a ghrelin mimetic, potently activating the Growth Hormone Secretagogue Receptor type 1a (GHS-R1a) located in the pituitary gland and hypothalamus. Activation of this receptor bypasses the somatostatin inhibitory pathway and directly stimulates the release of Growth Hormone-Releasing Hormone (GHRH) and GH itself. This results in an amplified and sustained pulsatile GH release pattern, which then drives the liver to produce IGF-1. The elevation of IGF-1 is the primary effector of its anabolic and regenerative properties.
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