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Research library, mechanism

The growth hormone secretagogue receptor (GHS-R): what the literature says

The growth hormone secretagogue receptor is a G-protein-coupled receptor of the pituitary and hypothalamus. It was cloned in 1996 as the target of synthetic secretagogues, and ghrelin, a peptide purified from stomach, was identified in 1999 as its endogenous ligand.

Written by the Peptency editorial teamLast reviewed 5 studies checked in PubMed on 5 October 2026

Research-use information. This page summarises published literature and regulator records. It is not guidance for use, not medical advice, and not a statement that any material is suitable for use in people or animals.

How was the receptor identified?

A G-protein-coupled receptor of the pituitary and of the arcuate ventro-medial and infundibular hypothalamus of swine and humans was cloned and shown to be the target of synthetic growth hormone secretagogues.

Three years later ghrelin, an acylated peptide purified from stomach, was reported as the natural ligand of the same receptor.[4],[2]

Which research materials in the catalog belong to this class?

Ipamorelin (a pentapeptide) and GHRP-2, also called pralmorelin (a hexapeptide), are synthetic growth hormone secretagogues. Both appear by name in the WADA 2026 Prohibited List under S2.2.4.

The ipamorelin pharmacology paper describes its growth hormone releasing activity in vitro and in animals and its selectivity against other pituitary hormones.[3],[1]

How is this receptor different from the GHRH receptor?

Growth hormone-releasing hormone acts at a separate pituitary receptor, cloned in 1992. The two receptors are described on separate pages because their ligands, sequences and literature differ.[5]

Which compounds in the catalog belong to this group?

Pentapeptide growth hormone secretagogueIpamorelin

C38H49N9O5, 711.9 g/mol

Hexapeptide growth hormone secretagogueGHRP-2

C45H55N9O6, 818 g/mol

Research materials: Ipamorelin, GHRP-2.

Which studies are cited on this page?

  1. [1] Pralmorelin: GHRP 2, GPA 748, growth hormone-releasing peptide 2, KP-102 D, KP-102 LN, KP-102D, KP-102LN. Drugs R D. 2004;5:236-9.

    Drug profile of pralmorelin (GHRP-2): its origin, pharmacology and development history.

    ReviewPMID 15230633DOI 10.2165/00126839-200405040-00011

  2. [2] Kojima M, Hosoda H, Date Y, Nakazato M, Matsuo H, Kangawa K. Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature. 1999;402:656-60.

    Purification of ghrelin from stomach as the endogenous ligand of the growth hormone secretagogue receptor.

    Receptor biologyPMID 10604470DOI 10.1038/45230

  3. [3] Raun K, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, et al.. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998;139:552-61.

    Describes the pharmacology of ipamorelin: growth hormone release in vitro and in animals, and selectivity against other pituitary hormones.

    In vitro and animal studyPMID 9849822DOI 10.1530/eje.0.1390552

  4. [4] Howard AD, Feighner SD, Cully DF, Arena JP, Liberator PA, Rosenblum CI, et al.. A receptor in pituitary and hypothalamus that functions in growth hormone release. Science. 1996;273:974-7.

    Cloning of the pituitary and hypothalamic G-protein-coupled receptor targeted by growth hormone secretagogues.

    Receptor biologyPMID 8688086DOI 10.1126/science.273.5277.974

  5. [5] Mayo KE. Molecular cloning and expression of a pituitary-specific receptor for growth hormone-releasing hormone. Mol Endocrinol. 1992;6:1734-44.

    Cloning and expression of the pituitary GHRH receptor, with ligand binding and cAMP production in transfected cells.

    Receptor biologyPMID 1333056DOI 10.1210/mend.6.10.1333056

Data dates: citations read from PubMed 2026-10-05.