Drug intelligence / Profile preview

D-Lys3-GHRP-6

Development stage
Preclinical
Lead developer
National Institute on Aging
Modality
Peptides, Small Molecules
Administration
Intraperitoneal, Intranasal
01

Overview

D-Lys3-GHRP-6 is a **synthetic peptide antagonist of the growth hormone secretagogue receptor 1a (GHS-R1a, also known as the ghrelin receptor)**. It was developed as a modified derivative of GHRP-6, replacing alanine with D-lysine at position 3, to reverse the action from agonist to antagonist. D-Lys3-GHRP-6 is used extensively in research to inhibit ghrelin signaling both in vitro and in vivo[2][3][7]. It not only blocks GHS-R1a but also possesses weak antagonistic activity at melanocortin receptors and partial antagonist activity at several GPCRs, including CCR5 and CXCR4 chemokine receptors[3][2][7]. Its effects in animal models include decreased energy intake, altered gastric emptying, reduction of GH secretion, and modulation of behaviors linked to food, ethanol reward, and impulsivity[1][3][5][8]. Research interest has centered on its potential roles in disorders of metabolism, addiction, behavior, and as a research tool in immunology and endocrinology. The compound is not approved for any human therapeutic indications and is intended for laboratory research use.

Other names
[D-Lys3]-GHRP-6
02

Targets

CCR5 (C-C chemokine receptor type 5)CXCR4 (C-X-C motif chemokine receptor 4)GHSR (Growth hormone secretagogue receptor)MCR (Melanocortin receptor family)

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