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Growth hormone secretagogues or GH secretagogues (GHSs) are a class of
drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...
s which act as
secretagogue In endocrinology, secretagogue is a substance that causes another substance to be secreted. The word contains the suffix '' -agogue'', which refers to something that ''leads'' to something else; a secretagogue thus leads to secretion. One example ...
s (i.e., induce the
secretion Secretion is the movement of material from one point to another, such as a secreted chemical substance from a cell or gland. In contrast, excretion is the removal of certain substances or waste products from a cell or organism. The classical mec ...
) of
growth hormone Growth hormone (GH) or somatotropin, also known as human growth hormone (hGH or HGH) in its human form, is a peptide hormone that stimulates growth, cell reproduction, and cell regeneration in humans and other animals. It is thus important in ...
(GH). They include
agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
s of the ghrelin/growth hormone secretagogue receptor (GHSR), such as
ghrelin Ghrelin (; or lenomorelin, INN) is a hormone primarily produced by enteroendocrine cells of the gastrointestinal tract, especially the stomach, and is often called a "hunger hormone" because it increases the drive to eat. Blood levels of ghrel ...
(lenomorelin),
pralmorelin Pralmorelin (INN) (brand name GHRP Kaken 100; former developmental code names KP-102, GPA-748, WAY-GPA-748), also known as pralmorelin hydrochloride ( JAN) and pralmorelin dihydrochloride (USAN), as well as, notably, growth hormone-releasing pept ...
(GHRP-2),
GHRP-6 Growth hormone-releasing peptide 6 (GHRP-6) (developmental code name SKF-110679), also known as growth hormone-releasing hexapeptide, is one of several synthetic met-enkephalin analogues that include unnatural D-amino acids, were developed for ...
, examorelin (hexarelin),
ipamorelin Ipamorelin (INN; development code NNC 26-0161) is a peptide selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS) and a growth hormone secretagogue. It is a pentapeptide with the amino acid sequence Aib-His-D-2-Nal-D-Phe-L ...
, and
ibutamoren Ibutamoren (; developmental code MK-677, MK-0677, LUM-201, L-163,191; former tentative brand name Oratrope) is a potency (pharmacology), potent, long-acting, oral administration, orally-active, binding selectivity, selective, and small molecule, ...
(MK-677), and agonists of the
growth hormone-releasing hormone receptor The growth-hormone-releasing hormone receptor (GHRHR) is a G-protein-coupled receptor that binds growth hormone-releasing hormone. The GHRHR activates a Gs alpha subunit, Gs protein that causes a cascade of Cyclic adenosine monophosphate, cAMP vi ...
(GHRHR), such as
growth hormone-releasing hormone Growth may refer to: Biology * Auxology, the study of all aspects of human physical growth * Bacterial growth *Cell growth *Growth hormone, a peptide hormone that stimulates growth *Human development (biology) *Plant growth *Secondary growth, gro ...
(GHRH, somatorelin),
CJC-1295 CJC-1295 DAC, also known as DAC:GRF (short for drug affinity complex:growth hormone-releasing factor), is a synthetic analogue of growth hormone-releasing hormone (GHRH) (also known as ''growth hormone-releasing factor'' (''GRF'')) and a growth ...
,
sermorelin Sermorelin acetate (; brand names Geref, Gerel), also known as GHRH (1-29), is a peptide analogue of growth hormone-releasing hormone (GHRH) which is used as a diagnostic agent to assess growth hormone (GH) secretion for the purpose of diagnos ...
, and
tesamorelin Tesamorelin (INN; trade name Egrifta SV) is a synthetic form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of HIV-associated lipodystrophy, approved initially in 2010. It is produced and developed by Theratechnologies ...
. Many of them also induce the secretion of
insulin-like growth factor 1 Insulin-like growth factor 1 (IGF-1), also called somatomedin C, is a hormone similar in tertiary structure, molecular structure to insulin which plays an important role in childhood growth, and has Anabolism, anabolic effects in adults. In the ...
(IGF-1), as well as of other hypothalamic-pituitary hormones such as
prolactin Prolactin (PRL), also known as lactotropin and mammotropin, is a protein best known for its role in enabling mammals to produce milk. It is influential in over 300 separate processes in various vertebrates, including humans. Prolactin is secr ...
and
cortisol Cortisol is a steroid hormone in the glucocorticoid class of hormones and a stress hormone. When used as medication, it is known as hydrocortisone. Cortisol is produced in many animals, mainly by the ''zona fasciculata'' of the adrenal corte ...
. The main clinical application of these agents is the treatment of
growth hormone deficiency Growth hormone deficiency (GHD), or hyposomatotropism, is a medical condition resulting from not enough growth hormone (GH). Generally the most noticeable symptom is that an individual attains a short height. Newborns may also present low blood ...
. They also see
black market A black market is a Secrecy, clandestine Market (economics), market or series of transactions that has some aspect of illegality, or is not compliant with an institutional set of rules. If the rule defines the set of goods and services who ...
use, similarly to
anabolic steroid Anabolic steroids, also known as anabolic-androgenic steroids (AAS), are a class of drugs that are structurally related to testosterone, the main male sex hormone, and produce effects by binding to the androgen receptor (AR). Anabolism, Anaboli ...
s, for
bodybuilding Bodybuilding is the practice of Resistance training, progressive resistance exercise to build, control, and develop one's skeletal muscle, muscles via muscle hypertrophy, hypertrophy. An individual who engages in this activity is referred to a ...
purposes.


GHRH receptor agonists


Peptide

* GHRH (Somatocrinin, GRF, GHRF) *
CJC-1295 CJC-1295 DAC, also known as DAC:GRF (short for drug affinity complex:growth hormone-releasing factor), is a synthetic analogue of growth hormone-releasing hormone (GHRH) (also known as ''growth hormone-releasing factor'' (''GRF'')) and a growth ...
(DAC:GRF) * Modified GRF (1-29) (CJC without DAC) * Dumorelin * Rismorelin *
Sermorelin Sermorelin acetate (; brand names Geref, Gerel), also known as GHRH (1-29), is a peptide analogue of growth hormone-releasing hormone (GHRH) which is used as a diagnostic agent to assess growth hormone (GH) secretion for the purpose of diagnos ...
(Geref, Gerel; GHRH (1-29)) * Somatorelin *
Tesamorelin Tesamorelin (INN; trade name Egrifta SV) is a synthetic form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of HIV-associated lipodystrophy, approved initially in 2010. It is produced and developed by Theratechnologies ...
(Egrifta)


Ghrelin (GHS) receptor agonists


Peptide

*
Ghrelin Ghrelin (; or lenomorelin, INN) is a hormone primarily produced by enteroendocrine cells of the gastrointestinal tract, especially the stomach, and is often called a "hunger hormone" because it increases the drive to eat. Blood levels of ghrel ...
(Lenomorelin, GHRL) * GHRP-1 * GHRP-2 (Pralmorelin; GHRP Kaken 100; GHRP-2; KP-102, GPA-748, WAY-GPA-748) * GHRP-3 * GHRP-4 * GHRP-5 *
GHRP-6 Growth hormone-releasing peptide 6 (GHRP-6) (developmental code name SKF-110679), also known as growth hormone-releasing hexapeptide, is one of several synthetic met-enkephalin analogues that include unnatural D-amino acids, were developed for ...
(SKF-110679) * Alexamorelin * Examorelin (hexarelin; EP-23905, MF-6003) *
Ipamorelin Ipamorelin (INN; development code NNC 26-0161) is a peptide selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS) and a growth hormone secretagogue. It is a pentapeptide with the amino acid sequence Aib-His-D-2-Nal-D-Phe-L ...
(NNC 26-0161) * Relamorelin (RM-131, BIM-28131, BIM-28163) * Tabimorelin (NN-703)


Non-peptide

*
Adenosine Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. The molecule consists of an adenine attached to a ribose via a β-N9- glycosidic bond. Adenosine is one of the four nucleoside build ...
*
Anamorelin Anamorelin ( INN) (developmental code names ONO-7643, RC-1291, ST-1291), also known as anamorelin hydrochloride ( USAN, JAN), is a non-peptide, orally-active, centrally-penetrant, selective agonist of the ghrelin/growth hormone secretagogue ...
(ONO-7643, RC-1291, ST-1291) * Capromorelin (CP-424391) *
Ibutamoren Ibutamoren (; developmental code MK-677, MK-0677, LUM-201, L-163,191; former tentative brand name Oratrope) is a potency (pharmacology), potent, long-acting, oral administration, orally-active, binding selectivity, selective, and small molecule, ...
(MK-677, MK-0677, L-163191, LUM-201) * Macimorelin (AEZS-130, JMV 1843) * SM-130686 Note that while
ulimorelin Ulimorelin (INN, USAN) (developmental code name TZP-101) is a drug with a modified cyclic peptide structure which acts as a selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR-1a). Unlike many related drugs, ulimorelin ha ...
is a ghrelin receptor agonist, it is not a GHS as it is peripherally selective and has little or no effect on GH secretion. Likewise, Adenosine is capable of eliciting hunger response as a ghrelin agonist but has little to no effect on GH secretion.


See also

* Hypothalamic–pituitary–somatic axis


References

Growth hormone secretagogues {{systemic-hormonal-drug-stub