Identification
NameHistrelin
Accession NumberDB06788
TypeSmall Molecule
GroupsApproved
Description

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.

Structure
Thumb
Synonyms
[(im-Bzl)-D-His6,Pro9-NEt]-gonadotropin releasing hormone
5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide
5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Nτ-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide
histrelina
histreline
histrelinum
L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-Nim-benzyl-histidyl-L-leucyl-L-arginyl-L-proline ethylamide
External IDs ORF 17070 / ORF-17070 / ORF17070 / RWJ 17070 / RWJ-17070 / RWJ17070
Product Ingredients
IngredientUNIICASInChI KeyDetails
Histrelin acetateNot AvailableNot AvailableNot applicableDetails
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Supprelin LAImplant50 mg/1SubcutaneousEndo Pharmaceuticals Solutions Inc.2007-05-31Not applicableUs
VantasImplant; Kit50 mgSubcutaneousPaladin Labs Inc2006-07-142017-04-07Canada
VantasImplant50 mg/1SubcutaneousEndo Pharmaceuticals Solutions Inc.2004-11-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIIH50H3S3W74
CAS number76712-82-8
WeightAverage: 1443.632
Monoisotopic: 1442.709519019
Chemical FormulaC70H94N18O16
InChI KeyBKEMVGVBBDMHKL-VYFXDUNUSA-N
InChI
InChI=1S/C66H86N18O12.2C2H4O2/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47;2*1-2(3)4/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71);2*1H3,(H,3,4)/t47-,48-,49-,50-,51-,52-,53+,54-,55-;;/m0../s1
IUPAC Name
(2S)-1-[(2S)-2-{[(2S)-2-{[(2R)-3-(1-benzyl-1H-imidazol-4-yl)-2-{[(2S)-2-{[(2S)-1,3-dihydroxy-2-{[(2S)-1-hydroxy-2-{[(2S)-1-hydroxy-2-({hydroxy[(2S)-5-hydroxy-3,4-dihydro-2H-pyrrol-2-yl]methylidene}amino)-3-(1H-imidazol-5-yl)propylidene]amino}-3-(1H-indol-3-yl)propylidene]amino}propylidene]amino}-1-hydroxy-3-(4-hydroxyphenyl)propylidene]amino}-1-hydroxypropylidene]amino}-1-hydroxy-4-methylpentylidene]amino}-5-carbamimidamidopentanoyl]-N-ethylpyrrolidine-2-carboximidic acid; bis(acetic acid)
SMILES
CC(O)=O.CC(O)=O.[H][[email protected]@](CO)(N=C(O)[[email protected]]([H])(CC1=CNC2=CC=CC=C12)N=C(O)[[email protected]]([H])(CC1=CN=CN1)N=C(O)[[email protected]]1([H])CCC(O)=N1)C(O)=N[[email protected]@]([H])(CC1=CC=C(O)C=C1)C(O)=N[[email protected]]([H])(CC1=CN(CC2=CC=CC=C2)C=N1)C(O)=N[[email protected]@]([H])(CC(C)C)C(O)=N[[email protected]@]([H])(CCCNC(N)=N)C(=O)N1CCC[[email protected]@]1([H])C(O)=NCC
Pharmacology
Indication

As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.

Structured Indications
Pharmacodynamics

Long-term treatment with histrelin acetate suppresses the LH response to GnRH causing LH levels to decrease to prepubertal levels within 1 month of treatment. As a result, serum concentrations of sex steroids (estrogen or testosterone) also decrease. In the treatment of Central Precocious Puberty, this is relevant as secondary sexual development ceases to progress in most patients. Additionally, linear growth velocity is slowed which improves the chance of attaining predicted adult height.

Mechanism of action

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

TargetKindPharmacological actionActionsOrganismUniProt ID
Gonadotropin-releasing hormone receptorProteinyes
agonist
HumanP30968 details
Related Articles
Absorption

Following subcutaneous insertion of one histrelin implant as the product Vantas in advanced prostate cancer patients (n = 17), peak serum concentrations of 1.10 ± 0.375 ng/mL (mean ± SD) occurred at a median of 12 hours. Continuous subcutaneous release was evident, as serum levels were sustained throughout the 52 week dosing period (see Figure 1). The mean serum histrelin concentration at the end of the 52 week treatment duration was 0.13 ± 0.065 ng/mL.

Volume of distribution

The apparent volume of distribution of histrelin following a subcutaneous bolus dose of histrelin as the product Vantas (500 mcg) in healthy volunteers was 58.4 ± 7.86 L

Protein binding

For the product Vantas, the fraction of drug unbound in plasma measured in vitro was 29.5% ± 8.9% (mean ± SD).

Metabolism

An in vitro drug metabolism study using human hepatocytes identified a single histrelin metabolite resulting from C-terminal dealkylation. Peptide fragments resulting from hydrolysis are also likely metabolites.

Route of eliminationNot Available
Half lifeNot Available
Clearance

The apparent clearance following a 50 mg (as histrelin acetate) Vantas implant in 17 prostate cancer patients was 174 mL/min.

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Histrelin.Investigational
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Histrelin.Approved, Investigational
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Histrelin.Withdrawn
AICA ribonucleotideThe therapeutic efficacy of Aicar can be decreased when used in combination with Histrelin.Experimental
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Histrelin.Approved
AmiodaroneHistrelin may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AnagrelideHistrelin may increase the QTc-prolonging activities of Anagrelide.Approved
Arsenic trioxideHistrelin may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherHistrelin may increase the QTc-prolonging activities of Artemether.Approved
AsenapineHistrelin may increase the QTc-prolonging activities of Asenapine.Approved
AzithromycinHistrelin may increase the QTc-prolonging activities of Azithromycin.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Histrelin.Investigational
BedaquilineHistrelin may increase the QTc-prolonging activities of Bedaquiline.Approved
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Histrelin.Withdrawn
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Histrelin.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Histrelin.Experimental
CeritinibHistrelin may increase the QTc-prolonging activities of Ceritinib.Approved
ChloroquineHistrelin may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineHistrelin may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Histrelin.Approved
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Histrelin.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Histrelin.Experimental
CiprofloxacinHistrelin may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideHistrelin may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramHistrelin may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinHistrelin may increase the QTc-prolonging activities of Clarithromycin.Approved
ClozapineHistrelin may increase the QTc-prolonging activities of Clozapine.Approved
Corifollitropin AlfaThe therapeutic efficacy of Corifollitropin Alfa can be increased when used in combination with Histrelin.Approved
CrizotinibHistrelin may increase the QTc-prolonging activities of Crizotinib.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Histrelin.Investigational
DisopyramideHistrelin may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideHistrelin may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronHistrelin may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneHistrelin may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DronedaroneHistrelin may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolHistrelin may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Histrelin.Approved
EliglustatHistrelin may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Histrelin.Approved
ErythromycinHistrelin may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramHistrelin may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Histrelin.Approved, Investigational
FlecainideHistrelin may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluoxetineHistrelin may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolHistrelin may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
Gadobenic acidHistrelin may increase the QTc-prolonging activities of Gadobenic acid.Approved
GemifloxacinHistrelin may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Histrelin.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Histrelin.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Histrelin.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Histrelin.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Histrelin.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Histrelin.Approved
GoserelinHistrelin may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronHistrelin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Histrelin.Investigational
HaloperidolHistrelin may increase the QTc-prolonging activities of Haloperidol.Approved
IbutilideHistrelin may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidoneHistrelin may increase the QTc-prolonging activities of Iloperidone.Approved
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Histrelin.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Histrelin.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Histrelin.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Histrelin.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Histrelin.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Histrelin.Approved
LenvatinibHistrelin may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideHistrelin may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevofloxacinHistrelin may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Histrelin.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Histrelin.Approved
LopinavirHistrelin may increase the QTc-prolonging activities of Lopinavir.Approved
LumefantrineHistrelin may increase the QTc-prolonging activities of Lumefantrine.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Histrelin.Approved
MethadoneHistrelin may increase the QTc-prolonging activities of Methadone.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Histrelin.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Histrelin.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Histrelin.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Histrelin.Approved, Investigational
MoxifloxacinHistrelin may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Histrelin.Approved, Investigational
NilotinibHistrelin may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
OfloxacinHistrelin may increase the QTc-prolonging activities of Ofloxacin.Approved
OndansetronHistrelin may increase the QTc-prolonging activities of Ondansetron.Approved
PaliperidoneHistrelin may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatHistrelin may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PazopanibHistrelin may increase the QTc-prolonging activities of Pazopanib.Approved
PentamidineHistrelin may increase the QTc-prolonging activities of Pentamidine.Approved
PerflutrenHistrelin may increase the QTc-prolonging activities of Perflutren.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Histrelin.Approved, Withdrawn
PimozideHistrelin may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Histrelin.Approved, Investigational
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Histrelin.Approved, Investigational
PrimaquineHistrelin may increase the QTc-prolonging activities of Primaquine.Approved
ProcainamideHistrelin may increase the QTc-prolonging activities of Procainamide.Approved
PromazineHistrelin may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneHistrelin may increase the QTc-prolonging activities of Propafenone.Approved
QuetiapineHistrelin may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineHistrelin may increase the QTc-prolonging activities of Quinidine.Approved
QuinineHistrelin may increase the QTc-prolonging activities of Quinine.Approved
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Histrelin.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Histrelin.Approved, Investigational
SaquinavirHistrelin may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Histrelin.Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Histrelin.Approved, Investigational
SotalolHistrelin may increase the QTc-prolonging activities of Sotalol.Approved
SulfisoxazoleHistrelin may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Histrelin.Approved, Investigational
TelavancinHistrelin may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinHistrelin may increase the QTc-prolonging activities of Telithromycin.Approved
TetrabenazineHistrelin may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineHistrelin may increase the QTc-prolonging activities of Thioridazine.Withdrawn
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Histrelin.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Histrelin.Approved
ToremifeneHistrelin may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Histrelin.Withdrawn
VandetanibHistrelin may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibHistrelin may increase the QTc-prolonging activities of Vemurafenib.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Histrelin.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Histrelin.Approved, Investigational
ZiprasidoneHistrelin may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolHistrelin may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Lewis KA, Eugster EA: Experience with the once-yearly histrelin (GnRHa) subcutaneous implant in the treatment of central precocious puberty. Drug Des Devel Ther. 2009 Sep 21;3:1-5. [PubMed:19920916 ]
  2. Shore N, Cookson MS, Gittelman MC: Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU Int. 2012 Jan;109(2):226-32. doi: 10.1111/j.1464-410X.2011.10370.x. Epub 2011 Aug 18. [PubMed:21851539 ]
  3. Djavan B, Schlegel P, Salomon G, Eckersberger E, Sadri H, Graefen M: Analysis of testosterone suppression in men receiving histrelin, a novel GnRH agonist for the treatment of prostate cancer. Can J Urol. 2010 Aug;17(4):5265-71. [PubMed:20735905 ]
  4. Link [Link]
External Links
ATC CodesL02AE05 — Histrelin
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.03 MB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
2RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
3CompletedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer2
3CompletedTreatmentCentral Precocious Puberty (CPP)1
Not AvailableRecruitingNot AvailableGender Dysphoria1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
ImplantSubcutaneous50 mg/1
Implant; kitSubcutaneous50 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8062652 No2006-06-162026-06-16Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.162 mg/mLALOGPS
logP2.21ALOGPS
logP3.39ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)2.71ChemAxon
pKa (Strongest Basic)11.9ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count26ChemAxon
Hydrogen Donor Count16ChemAxon
Polar Surface Area478.27 Å2ChemAxon
Rotatable Bond Count34ChemAxon
Refractivity365.33 m3·mol-1ChemAxon
Polarizability139.23 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentOligopeptides
Alternative ParentsTyrosine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Leucine and derivatives / N-acyl-alpha amino acids and derivatives / Proline and derivatives / Tryptamines and derivatives / Serine and derivatives / Alpha amino acid amides / Amphetamines and derivatives
SubstituentsAlpha-oligopeptide / Tyrosine or derivatives / Phenylalanine or derivatives / Histidine or derivatives / Leucine or derivatives / N-acyl-alpha amino acid or derivatives / Proline or derivatives / Triptan / Alpha-amino acid amide / Serine or derivatives
Molecular FrameworkNot Available
External Descriptorsacetate salt (CHEBI:63530 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Peptide binding
Specific Function:
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
Gene Name:
GNRHR
Uniprot ID:
P30968
Uniprot Name:
Gonadotropin-releasing hormone receptor
Molecular Weight:
37730.355 Da
Drug created on September 14, 2010 10:21 / Updated on September 01, 2017 11:31