Growth Hormone-Releasing Peptide (GHRP) binding to porcine anterior pituitary and hypothalamic membranes
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Cited by (49)
Targeting appetite and satiety in diabetes and obesity, via G protein-coupled receptors
2022, Biochemical PharmacologyCitation Excerpt :In this setting there has been considerable effort to target GHSR1a to alter food intake and thus modulate body weight. [ d-Lys3]-GHRP-6 is a synthetic peptide identified as a GHSR1a antagonist (prior to GHSR1a cloning) due to its ability to inhibit GHRP-6 dependent growth hormone release [75]. In acute studies [d-Lys3]-GHRP-6 decreases food intake and body weight in mice, however long-term treatment of non-obese diabetic mice (MKR model) with [d-Lys3]-GHRP-6 exacerbates glucose intolerance and increases food intake, acting more like a GHSR1a agonist [76].
History to the Discovery of Ghrelin
2012, Methods in EnzymologyCitation Excerpt :These assay results included specific binding of GHRH, GHRPs, as well as partial and nonpeptide GHSs. GHRP-6 did not bind in the GHRH RRA; however, GHRP-6-specific binding was demonstrated in the hypothalamus and pituitary (Bitar et al., 1991; Codd et al., 1989; Howard et al., 1996, vide infra; Sethumadhavan et al., 1991; Smith et al., 1996, vide infra; Van der Ploeg et al., 1998, vide infra; Veeraragavan et al., 1992). In general, receptor-binding results and GH-releasing results parallel each other.
Ghrelin as a novel locally produced relaxing peptide of the iris sphincter and dilator muscles
2006, Experimental Eye ResearchCitation Excerpt :The results of the present study also suggest that the relaxing effects of ghrelin on the iris sphincter muscle are not mediated by GHSR-1a, as they were also observed in response to des-octanoyl-ghrelin. Furthermore, in presence of D-Lys3 GHRP6, an inhibitor of that receptor (Veeraragavan et al., 1992), the relaxing effect of ghrelin was not inhibited, but rather enhanced more than threefold. It should be, however, stressed that even if GHSR-1a does not seem to mediate the relaxing effect of ghrelin, it presumably modulates it, as inhibition of this receptor enhanced the degree of active tension decline.
Ghrelin - A hormone with multiple functions
2004, Frontiers in Neuroendocrinology4 Growth Hormone Secretagogues: Discovery of Small Orally Active Molecules by Peptidomimetic Strategies
2002, Progress in Medicinal ChemistryGrowth hormone secretagogues: Recent advances and applications
1999, Drug Discovery Today