GHS Receptor Agonists are pharmaceutical agents designed to selectively bind to and activate Growth Hormone Secretagogue (GHS) receptors, mimicking the action of endogenous ghrelin. Their clinical utility lies in stimulating the release of Growth Hormone (GH) and potentially modulating appetite regulation pathways. These compounds are pharmacologically potent tools for investigating or therapeutically addressing GH deficiency states. They act as direct activators of the somatotropic axis.
Origin
GHS receptors are G-protein coupled receptors identified as targets for ghrelin and synthetic analogues. Agonists, by definition, are substances that initiate a physiological response when bound to a receptor. The pharmacological development of these agents aimed to decouple the appetite-stimulating effects of ghrelin from its GH-releasing properties for therapeutic specificity. This class represents targeted modulation of pituitary function.
Mechanism
Upon binding, GHS receptor agonists trigger intracellular signaling cascades, primarily involving the activation of the Gq protein pathway, leading to the mobilization of intracellular calcium. This calcium flux acts synergistically with GHRH signaling to promote the transcription and secretion of growth hormone from pituitary somatotrophs. The resulting GH release then stimulates IGF-1 production in the liver, mediating most of the anabolic effects.
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