Page last updated: 2024-08-01 19:55:11

ay 25,205

Description

alarelin: gonadotropin-releasing hormone analog widely used in China for the treatment of endometriosis and uterine leiomyoma [MeSH]

Cross-References

ID SourceID
PubMed CID9855027
PubMed CID5484741
CHEMBL ID3272561
SCHEMBL ID11315269
MeSH IDM0056323

Synonyms (32)

Synonym
alarelin acetate
79561-22-1
alarelin
A839717
SCHEMBL11315269
njs328sua7 ,
dalareline
lhrh-a2
dalarelin
L-4513 ,
CHEMBL3272561
gtpl9342
AKOS030213241
AKOS030260542
NCGC00485985-01
DTXSID40873497
glp-his-trp-ser-tyr-d-ala-leu-arg-pro-nhet
AMY25366
CCG-270649
wy-18481
tap-127
alarelin [who-dd]
ay-25205
CS-0015083
HY-P0048
tap 127
surfagon
ay-25,205
brn 0906592
wy 18481
(d-ala(sup 6)-des-gly-nh2(sup 10))lhrh ethylamide
unii-njs328sua7

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1148725Induction of LH release in immature rat administered as infusion relative to LH-RH1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
ISSN: 0022-2623
Inhibitors of the luteinizing hormone-releasing hormone based upon modifications in the 2, 3, and 6 positions.
AID1148726Induction of FSH release in immature rat administered as infusion relative to LH-RH1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
ISSN: 0022-2623
Inhibitors of the luteinizing hormone-releasing hormone based upon modifications in the 2, 3, and 6 positions.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346002Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors)2016British journal of pharmacology, Jan, Volume: 173, Issue:1
ISSN: 1476-5381
Characterization of 12 GnRH peptide agonists - a kinetic perspective.

Research

Studies (156)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990115 (73.72)18.7374
1990's19 (12.18)18.2507
2000's10 (6.41)29.6817
2010's9 (5.77)24.3611
2020's3 (1.92)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (2.99%)6.00%
Case Studies2 (1.20%)4.05%
Observational0 (0.00%)0.25%
Other160 (95.81%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
buserelinoligopeptide201620168.0low000010
fertirelinoligopeptide1976201628.0low010010
deslorelinoligopeptide201620168.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
pyrrolidonecarboxylic acid5-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid
algal metabolite202020204.0low000010
diphenylaminearomatic amine;
bridged diphenyl fungicide;
secondary amino compound
antifungal agrochemical;
antioxidant;
carotogenesis inhibitor;
EC 1.3.99.29 [phytoene desaturase (zeta-carotene-forming)] inhibitor;
ferroptosis inhibitor;
radical scavenger
202020204.0low000010
buserelinoligopeptide201720177.0low000010
pd 0325901difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound
antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
202020204.0low000010
trelstar201920195.0low000010
cetrorelixoligopeptideantineoplastic agent;
GnRH antagonist
2012201411.0low000020
gamma-aminobutyric acidamino acid zwitterion;
gamma-amino acid;
monocarboxylic acid
human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
1990199034.0low001000
chlordeconecyclic ketone;
organochlorine compound
insecticide;
persistent organic pollutant
1986198638.0low010000
lactic acid2-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
1998199826.0low001000
inositolcyclitol;
hexol
1988198836.0low010000
valproic acidbranched-chain fatty acid;
branched-chain saturated fatty acid
anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
1990199034.0low001000
domperidonebenzimidazoles;
heteroarylpiperidine
antiemetic;
dopaminergic antagonist
1988198836.0low010000
flutamide(trifluoromethyl)benzenes;
monocarboxylic acid amide
androgen antagonist;
antineoplastic agent
2001200123.0low000100
indomethacinaromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole
analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
1982198440.8low040000
1-methyl-3-isobutylxanthine3-isobutyl-1-methylxanthine1983198341.0low010000
metoclopramidebenzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound
antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
1984201126.5low010010
octopaminephenylethanolamines;
tyramines
neurotransmitter1984198440.0low010000
proadifendiarylmethane1985198539.0low010000
propranololnaphthalenes;
propanolamine;
secondary amine
anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
1984198440.0low010000
reserpinealkaloid ester;
methyl ester;
yohimban alkaloid
adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
1988198836.0low010000
phentolamineimidazoles;
phenols;
substituted aniline;
tertiary amino compound
alpha-adrenergic antagonist;
vasodilator agent
1984198440.0low010000
alloxanpyrimidonehyperglycemic agent;
metabolite
1980198044.0low010000
estrone17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols
antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
1983198639.5low020000
alaninealanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid
EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
1997199727.0low001000
9,10-dimethyl-1,2-benzanthraceneortho-fused polycyclic arene;
tetraphenes
carcinogenic agent1981198143.0low010000
apomorphineaporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
1984198639.0low020000
methyltestosterone17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
enone
anabolic agent;
androgen;
antineoplastic agent
1983198341.0low010000
uridineuridinesdrug metabolite;
fundamental metabolite;
human metabolite
1983198539.7low030000
leucineamino acid zwitterion;
L-alpha-amino acid;
leucine;
proteinogenic amino acid;
pyruvate family amino acid
algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
1985198539.0low020000
androstenedione17-oxo steroid;
3-oxo-Delta(4) steroid;
androstanoid
androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
1984198639.0low020000
phenylalanineamino 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
1985198539.0low010000
cycloheximideantibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol
anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
1980198541.5low020000
17-alpha-hydroxyprogesterone17alpha-hydroxy-C21-steroid;
17alpha-hydroxy steroid;
tertiary alpha-hydroxy ketone
human metabolite;
metabolite;
mouse metabolite;
progestin
1984198539.5low040000
3-mercaptopropionic acidmercaptopropanoic acidalgal metabolite1990199034.0low001000
pyrrolidonecarboxylic acid5-oxoproline;
L-proline derivative;
non-proteinogenic L-alpha-amino acid
algal metabolite1984198638.7low030000
pregnenolone20-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
C21-steroid
human metabolite;
mouse metabolite
1984198539.5low020000
20-alpha-dihydroprogesterone20-hydroxypregn-4-en-3-onehuman metabolite;
mouse metabolite
1984198539.5low020000
testosterone enanthateheptanoate ester;
sterol ester
androgen1985198539.0low010000
dihydrotestosterone17beta-hydroxy steroid;
17beta-hydroxyandrostan-3-one;
3-oxo-5alpha-steroid
androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
1983199138.2low051000
pimozidebenzimidazoles;
heteroarylpiperidine;
organofluorine compound
antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
1983199836.6low072000
mirexchlorocarbon;
organochlorine insecticide
persistent organic pollutant1986198638.0low010000
tetradecanoylphorbol acetateacetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester
antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
1985198638.3low030000
danazol17beta-hydroxy steroid;
terminal acetylenic compound
anti-estrogen;
estrogen antagonist;
geroprotector
1983198341.0low020000
bromocriptineindole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
1984198440.0low010000
8-bromo cyclic adenosine monophosphate3',5'-cyclic purine nucleotide;
adenyl ribonucleotide;
organobromine compound
antidepressant;
protein kinase agonist
1985198539.0low010000
methyldopaL-tyrosine derivative;
non-proteinogenic L-alpha-amino acid
alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
1988198836.0low010000
colforsinacetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol
adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
1985198539.0low010000
buserelinoligopeptide1980199439.0low041000
phorbolsditerpene;
terpenoid fundamental parent
1985198539.0low010000
oxytocinheterodetic cyclic peptide;
peptide hormone
oxytocic;
vasodilator agent
1984198440.0low010000
cortodoxonedeoxycortisol;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
human metabolite;
mouse metabolite
1998199826.0low001000
arachidonic acidicosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
1982198640.0low020000
diethylstilbestrololefinic compound;
polyphenol
antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen
1982198540.7low030000
phorbol-12,13-didecanoate1985198539.0low010000
lypressincyclic peptide1984198440.0low010000
leuprolideoligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist
1980198541.5low020000
enclomiphene1985198539.0low010000
dinoprostmonocarboxylic acid;
prostaglandins Falpha
human metabolite;
mouse metabolite
1985198837.5low020000
6-ketoprostaglandin f1 alphaprostaglandins Falphahuman metabolite;
mouse metabolite
1982198242.0low010000
11-ketotestosterone11-oxo steroid;
17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
androstanoid
androgen;
human metabolite;
marine xenobiotic metabolite
1991199829.5low002000
morphinemorphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound
anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
1985198539.0low010000
goserelinorganic molecular entity1985198539.0low010000
naltrexonecyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound
antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
1985198539.0low010000
lhrh, ala(6)-1988198836.0low010000
lhrh, n-et-alanh2(6)-1983198341.0low010000
medrogestonecorticosteroid hormone1982198242.0low010000
calcimycinbenzoxazole1985198638.5low040000
iturelix1994199430.0low001000
phosphatidylcholines1,2-diacyl-sn-glycero-3-phosphocholine1982198242.0low010000
menotropins1985198539.0low010000
bucladesine3',5'-cyclic purine nucleotide1985198638.3low030000
lhrh, ac-dehydro-pro(1)-4-f-phe(2)-trp(3,6)-1985198539.0low010000
trelstar1980198044.0low030000
nafarelinoligopeptideanti-estrogen;
gonadotropin releasing hormone agonist
1985198539.0low010000
lutrelin acetate1982198242.0low010000
lhrh, pglu(1)-phe(2)-trp(3,6)-1984198639.0medium020000
n-ac-(4-cl-phe)(1)-(4-cl-phe)(2)-trp(3)-lys(6)-alanh2(10)-lhrh1984198639.0high020000
lhrh, phe(2)-trp(3)-phe(6)-1983198341.0medium010000
vasoactive intestinal peptide1985199832.5low011000
epidermal growth factor1986198638.0low010000
5-oxo-pro-his-trp-ser-tyr-gly-trp-leu-pro-glynh21988198836.0medium020000
guanylyl imidodiphosphatenucleoside triphosphate analogue1983198540.0low020000
phosphorus radioisotopes1984198838.0low020000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
48,XXYY Syndrome01985198539.0low010000
Ache01985198539.0low010000
Adenoma01994199430.0low001000
Adenoma, Basal Cell01994199430.0low001000
Aggression01991199133.0low001000
Aging01984200529.5low010100
Alcohol Drinking01991199730.3low003000
Alloxan Diabetes01980198044.0low010000
Anovulation01983199037.5low011000
Anxiety0201920195.0low000010
Atrophy01982198242.0low010000
Body Weight01980198641.0low020000
Bone Cancer01988198836.0low010000
Bone Neoplasms01988198836.0low010000
Bovine Diseases01985198539.0low010000
Breast Cancer01988198836.0low010000
Breast Neoplasms01988198836.0low010000
Cancer of Ovary01986198638.0low010000
Cancer of Pelvis01983198341.0low010000
Cancer of Pituitary01994199430.0low001000
Cancer of Prostate01984198837.7low030000
Compensatory Hyperinsulinemia01986198638.0low010000
Dermoid01986198638.0low010000
Endometrioma01983198341.0low020000
Endometriosis01983198341.0low020000
Experimental Mammary Neoplasms01981198143.0low010000
Familial Precocious Puberty01986198638.0low010000
Hormone-Dependent Neoplasms01982198242.0low010000
Hypergonadotropic Hypogonadism01985198539.0low010000
Hyperinsulinism01986198638.0low010000
Hypogonadism01985198539.0low010000
Infertility, Female01983198540.0low020000
Insulin Resistance01986198638.0low010000
Insulin Sensitivity01986198638.0low010000
Klinefelter Syndrome01985198539.0low010000
Orbital Neoplasms01988198836.0low010000
Osteogenic Sarcoma01988198836.0low010000
Osteosarcoma01988198836.0low010000
Ovarian Neoplasms01986198638.0low010000
Pain01985198539.0low010000
Pituitary Neoplasms01994199430.0low001000
Polycystic Ovarian Syndrome01985198638.3low030000
Polycystic Ovary Syndrome01985198638.3low030000
Pregnancy01980199539.5medium0103000
Prostatic Neoplasms01984198837.7low030000
Puberty, Precocious01986198638.0low010000
Sterility, Female01983198540.0low020000
Body Weight02012201212.0low000010
Congenital Zika Syndrome0202020204.0low000010
Disease Models, Animal0201620206.0low000020
Liver Diseases0201620168.0low000010
Liver Dysfunction0201620168.0low000010
Zika Virus Infection0202020204.0low000010

Long-term Use (5)

ArticleYear
Expression of cytochrome P450 2C and 3A in female rat liver after long-term administration of gonadoliberin analogs.
International journal of occupational medicine and environmental health, , Volume: 29, Issue:2
2016
Changes in the subcellular and tissue location of estrogen and progesterone receptors in rat uterus after long-term treatment with analogs of gonadoliberin.
Ginekologia polska, , Volume: 85, Issue:4
2014
Kinetics of steroid responsiveness to hCG during chronic inhibition of testicular function by GnRH analogue.
Acta endocrinologica, , Volume: 107, Issue:4
1984
Dissociation between the direct stimulatory and inhibitory effects of a gonadotropin-releasing hormone analog on ovarian functions.
Molecular and cellular endocrinology, , Volume: 31, Issue:2-3
1983
Lack of a direct effect of gonadotropin hormone-releasing hormone agonist on human testicular steroidogenesis.
The Journal of clinical endocrinology and metabolism, , Volume: 64, Issue:1
1987

Pharmacokinetics (1)

ArticleYear
Distribution and pharmacokinetics of the gonadotrophin releasing hormone analogue (Gn-RH analogue) dalarelin in rats.
Bollettino chimico farmaceutico, , Volume: 139, Issue:5

Bioavailability (4)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5
2019
Pharmacokinetics and Bioavailability of the GnRH Analogs in the Form of Solution and Zn
European journal of drug metabolism and pharmacokinetics, , Volume: 42, Issue:2
2017
Sustained release and biological availability of dalarelin from the biodegradable coacervate microcapsules.
Farmaco (Societa chimica italiana : 1989), , Volume: 57, Issue:12
2002
Bioavailability of dalarelin--a superactive GnRH analogue--in rats.
Farmaco (Societa chimica italiana : 1989), , Volume: 54, Issue:11-12

Dosage (6)

ArticleYear
Effect of gonadotrophin releasing hormone upon the pattern of steroidogenesis in isolated preovulatory rat follicles.
Acta endocrinologica, , Volume: 105, Issue:1
1984
Effects of LH-RH and des-Gly10[D-Ala6]LH-RH-ethylamide on plasma gonadotropin levels and oocyte maturation in adult female coho salmon (Oncorhynchus kisutch).
General and comparative endocrinology, , Volume: 49, Issue:3
1983
Species differences in the sensitivity to a GnRH antagonist.
Contraception, , Volume: 32, Issue:1
1985
Simultaneous measurement of hormone release and secretagogue binding by individual pituitary cells.
Proceedings of the National Academy of Sciences of the United States of America, , Volume: 84, Issue:15
1987
Identification of subpopulations of rat granulosa cells: sedimentation properties and hormonal responsiveness.
Endocrinology, , Volume: 117, Issue:3
1985
Inhibitors of the luteinizing hormone-releasing hormone based upon modifications in the 2, 3, and 6 positions.
Journal of medicinal chemistry, , Volume: 19, Issue:2
1976

Interactions (1)

ArticleYear
Effects of [D-Arg6, Trp7, Leu8, Pro9NEt]-luteinizing hormone-releasing hormone (sGnRH-A) and [D-Ala6, Pro9NEt]-luteinizing hormone-releasing hormone (LHRH-A), in combination with pimozide or domperidone, on gonadotropin release and ovulation in the Chines
General and comparative endocrinology, , Volume: 69, Issue:1
1988