Compounds > gonadotropin-releasing hormone
Page last updated: 2024-12-06

gonadotropin-releasing hormone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

relisorm L: Gonadotropin-Releasing Hormone analog [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

gonadorelin : A ten-membered synthetic oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, glycyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID638793
CHEMBL ID1007
CHEBI ID5520
SCHEMBL ID143114
MeSH IDM0012446
PubMed CID13190524
MeSH IDM0012446

Synonyms (91)

Synonym
nialutin
gn-rh
luliberin
luteostimulin
einecs 232-895-0
ay 24034
lh-releasing factor
lh-rf
LRF ,
gonadotropin-releasing factor
gnrh-i
gonadorelin
gonadoliberin i
lh-rh (swine)
synthetic lh-fsh-rh
synthetic lh-rh/fsh-rh
lhfshrh
gonadorelin [inn:ban]
gonadorelinum [inn-latin]
fertagyl
gonadorelina [inn-spanish]
synthetic gn-rh
synthetic lh-rh
p-glu-his-trp-ser-tyr-gly-leu-arg-pro-gly-nh2
mammalian lh-rh
porchine lh-rh
human lh-rh
relefact
dirigestran
lutal
synthetic lrf
luforan
synthetic gonadoliberin
synthetic lh-rf
porcine lh-releasing factor
einecs 251-553-1
mammalian gnrh
lfrh
lh-releasing factor (pig)
ovine lh-rh
synthetic lh-releasing factor
dirigestran spofa
relisorm l
synthetic decapeptide fsh/lh-rh
hoe 471
lutrefact
glycinamide, 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosylglycyl-l-leucyl-l-arginyl-l-prolyl-
5-oxopro-his-trp-ser-tyr-gly-leu-arg-pro-gly-nh2 (human or pig)
CHEMBL1007
human gonadoliberin-i
chebi:5520 ,
gonadorelin decapeptide
D08027
gonadorelin (inn)
fertagyl (tn)
A837181
unii-9o7312w37g
gonadorelina
9o7312w37g ,
gonadorelinum
ay 24031
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosylglycyl-l-leucyl-l-arginyl-l-prolylglycinamide
5-oxo-phwsyglrpgnh2
AKOS015895122
[125i]-gnrh i
[125i]gnrh i (human, mouse, rat)
gtpl3786
bdbm50422274
SCHEMBL143114
HS-2014
XLXSAKCOAKORKW-AQJXLSMYSA-N
l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosylglycyl-l-leucyl-l-arginyl-l-prolylglycinamide
AKOS030213247
gonadotropin-releasing hormone (gnrh) analogue
gonadorelin (gonadorelin decapeptide (gnrh))
luteinising hormone-releasing factor (lnrh) analogue
5-oxopro-his-trp-ser-tyr-gly-leu-arg-pro-gly-nh2
DTXSID20873490
pglu-his-trp-ser-tyr-gly-leu-arg-pro-glynh2
pglu-his-trp-ser-tyr-gly-leu-arg-pro-gly-nh(2)
Q20817116
CCG-270650
v04cm01
gonadorelinum (inn-latin)
gonadoreline
gonadorelin (mart.)
gonadorelina (inn-spanish)
fertelin, ovacyst
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl- glycyl-l-leucyl-l-arginyl-l-prolyl-glycinamide
h01ca01
lhrh (1-5)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
gonadotropin releasing hormone agonistAny drug which binds to gonadotropin-releasing hormone receptors and triggers a response.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
peptide hormoneAny peptide with hormonal activity in animals, whether endocrine, neuroendocrine, or paracrine.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lutropin-choriogonadotropic hormone receptor Rattus norvegicus (Norway rat)Ki0.00130.00130.00130.0013AID102952
Gonadotropin-releasing hormone receptorHomo sapiens (human)IC50 (µMol)0.01000.00010.12895.2000AID102819
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00500.00030.15422.0000AID102815; AID102947; AID74558
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)Ki794,328,028,938,240.00000.00383.51866.5000AID102938
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
gonadotropin secretionGonadotropin-releasing hormone receptorHomo sapiens (human)
cellular response to gonadotropin-releasing hormoneGonadotropin-releasing hormone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayGonadotropin-releasing hormone receptorHomo sapiens (human)
cellular response to hormone stimulusGonadotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
peptide bindingGonadotropin-releasing hormone receptorHomo sapiens (human)
gonadotropin-releasing hormone receptor activityGonadotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGonadotropin-releasing hormone receptorHomo sapiens (human)
membraneGonadotropin-releasing hormone receptorHomo sapiens (human)
plasma membraneGonadotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID170349Effect on GnRH-induced LH secretion in intact male rats at 50 ng of compound; ng of LH/mL1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Design of potent cyclic gonadotropin releasing hormone antagonists.
AID100098Leutinising hormone releasing potency in rats is expressed as negative logarithm of the concentration of compound (agonist)1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.
AID693375Displacement of [125I]-Tyr6, His5 from human LHRH1 receptor expressed in HEK 293 cells after 16 to 19 hrs by gamma counter2012European journal of medicinal chemistry, Dec, Volume: 58Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties.
AID1145189Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 1 ng, sc measured at 30 mins post dose by RIA (Rvb = 5.3 +/- 1.5 ng/ml)1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID197342Tested in vitro for LH release from cultured rat pituitary cells, activity is expressed as pD2 value1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
AID74558Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.
AID102947The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
AID102819The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
AID755721Half life in human plasma2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and in vitro evaluation of glycosyl derivatives of luteinizing hormone-releasing hormone (LHRH).
AID1145194Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 5 ng, sc measured at 60 mins post dose by RIA (Rvb = 6.0+/- 0.4 ng/ml)1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID1136685In vivo activation of LH-RH receptor in immature rat assessed as release of luteinizing hormone in serum at 50 ng, sc measured over 4 hrs by double antibody radioimmunoassay1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Branched-chain analogues of luteinizing hormone-releasing hormone.
AID1145193Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 1 ng, sc measured at 60 mins post dose by RIA (Rvb = 6.0+/- 0.4 ng/ml)1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID1145190Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 5 ng, sc measured at 30 mins post dose by RIA (Rvb = 5.3 +/- 1.5 ng/ml)1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID102815The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
AID102938In vitro binding affinity for rat pituitary LHRH receptor, activity is expressed as pKI value1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
AID102952In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.
AID1136686In vivo activation of LH-RH receptor in immature rat assessed as release of follicle-stimulating hormone in serum at 50 ng, sc measured over 4 hrs by radioimmunoassay1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Branched-chain analogues of luteinizing hormone-releasing hormone.
AID170347Effect on GnRH-induced LH secretion in intact male rats at 20 ng of compound; ng of LH/mL1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Design of potent cyclic gonadotropin releasing hormone antagonists.
AID693376Metabolic stability in mouse renal epithelial cell membranes assessed as compound remaining at 10 nM measured at 30 mins2012European journal of medicinal chemistry, Dec, Volume: 58Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties.
AID755720Apparent permeability across human Caco2 cells at 200 uM up to 120 mins by LC-MS analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and in vitro evaluation of glycosyl derivatives of luteinizing hormone-releasing hormone (LHRH).
AID188019In vitro FSH-release potency of compound was measured in rat hemipituitaries by taking LH-RH as standard1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some analogues of luteinizing hormone-releasing hormone with substituents in position 10.
AID755719Half life in human Caco2 cell homogenates at 200 uM by LC-MS analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and in vitro evaluation of glycosyl derivatives of luteinizing hormone-releasing hormone (LHRH).
AID188020In vitro LH-release potency of compound was measured in rat hemipituitaries by taking LH-RH as standard1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some analogues of luteinizing hormone-releasing hormone with substituents in position 10.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (22.73)18.7374
1990's2 (9.09)18.2507
2000's6 (27.27)29.6817
2010's7 (31.82)24.3611
2020's2 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (9.09%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews3 (27.27%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
Other8 (72.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
leuprolide
Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.940oligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist
t 98475
T 98475: structure in first source		1.9910isopropyl ester;
thienopyridine
deslorelin
deslorelin: Ovuplant is tradename for a short-term-release implant containing deslorelin acetate; RN given refers to D-isomer; RN for cpd without isomeric designation not avail 12/90		2.3720oligopeptide
ovurelin
ovurelin: GnRH agonist		1.9510
lhrh, phe(6)-
LHRH, Phe(6)-: RN given refers to (D)-isomer		1.9510
lhrh, phe(2)-trp(3)-phe(6)-
LHRH, Phe(2)-Trp(3)-Phe(6)-: gonodorelin antagonist; RN given refers to (D-Phe-D-Trp-D-Phe)-isomer		1.9510
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		2.110amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
pyrrolidonecarboxylic acid
Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.. 5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration.		3.84305-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid		algal metabolite
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.110mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.110azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
lhrh, gln(8)-
[no description available]		3.5420
rtki cpd
RTKI cpd: preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors		2.110
batimastat
batimastat: structure given in first source; a synthetic matrix metalloproteinase inhibitor. batimastat : A secondary carboxamide resulting from the formal condensation of the carboxy group of (2S,3R)-5-methyl-3-{[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-[(thiophen-2-ylsulfanyl)methyl]hexanoic acid with the amino group of hydroxylamine. It a broad-spectrum matrix metalloprotease inhibitor.		2.110hydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide		angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor
lhrh, his(5)-trp(7)-tyr(8)-
LHRH, His(5)-Trp(7)-Tyr(8)-: isolated from chicken hypothalamus; also ostrich; RN given refers to all-(L)-isomer		2.0310
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.5120
kiss1 protein, human
Kisspeptins: Intercellular signaling peptides that were originally characterized by their ability to suppress NEOPLASM METASTASIS. Kisspeptins have since been found to play an important role in the neuroendocrine regulation of REPRODUCTION.		2.2510
ConditionIndicatedRelationship StrengthStudiesTrials
Familial Precocious Puberty
[description not available]		03.3911
Puberty, Precocious
Development of SEXUAL MATURATION in boys and girls at a chronological age that is 2.5 standard deviations below the mean age at onset of PUBERTY in the population. This early maturation of the hypothalamic-pituitary-gonadal axis results in sexual precocity, elevated serum levels of GONADOTROPINS and GONADAL STEROID HORMONES such as ESTRADIOL and TESTOSTERONE.		03.3911
Cancer of Endometrium
[description not available]		03.7730
Endometrial Neoplasms
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.		03.7730
Metastase
[description not available]		02.1110
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.1110