Page last updated: 2024-12-11

ay 25,205

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

Description

alarelin: gonadotropin-releasing hormone analog widely used in China for the treatment of endometriosis and uterine leiomyoma [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

surfagon: potent LHRH agonist; RN given refers to (D-Ala-L-Pro)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

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

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Also, the basic pharmacokinetic parrameters were determined."( Distribution and pharmacokinetics of the gonadotrophin releasing hormone analogue (Gn-RH analogue) dalarelin in rats.
Dolinska, B; Ryszka, F; Suszka-Switek, A,
)
0.13

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of LHRH-A and sGnRH-A alone and in combination with the dopamine receptor antagonists pimozide (PIM) and domperidone (DOM) on stimulation of gonadotropin (GtH) secretion and ovulation in Chinese loach (Paramisgurnus dabryanus) and common carp (Cyprinus carpio) were studied."( 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
Liang, JY; Lin, HR; Peter, RE; Rivier, JE; Vale, WW; Van der Kraak, G; Zhou, XJ, 1988
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Dalarelin bioavailability was 1651."( Bioavailability of dalarelin--a superactive GnRH analogue--in rats.
Dolińska, B; Ryszka, F; Suszka-Switek, A,
)
0.13
" It was found that the 125I labelled dalarelin in the form of microcapsules had better bioavailability and was active longer in the rat when compared with the 125I labelled dalarelin solution injections."( Sustained release and biological availability of dalarelin from the biodegradable coacervate microcapsules.
Dolińska, B; Ryszka, F; Waleczek, D, 2002
)
0.31
"Performed studies indicate that GnRH analogs in the form of suspension have higher bioavailability than their solution counterparts."( Pharmacokinetics and Bioavailability of the GnRH Analogs in the Form of Solution and Zn
Danch, A; Dec, R; Dolińska, B; Filipczyk, Ł; Ryszka, F; Suszka-Świtek, A; Wiaderkiewicz, R, 2017
)
0.46
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"3 ng/ml of medium of LH-RH on isolated rat pituitaries, at a dosage of 10 mug."( Inhibitors of the luteinizing hormone-releasing hormone based upon modifications in the 2, 3, and 6 positions.
Bowers, CY; Fisher, G; Folkers, K; Humphries, J; Wan, YP, 1976
)
0.26
" Dose-response analysis indicated that the actions of these hormones were additive, suggesting the presence of subpopulations of granulosa cells."( Identification of subpopulations of rat granulosa cells: sedimentation properties and hormonal responsiveness.
Davoren, JB; Hsueh, AJ; Kasson, BG; Meidan, R, 1985
)
0.27
" Dose-response studies showed that 1 microgram (4 micrograms/kg) of GnRH-A was sufficient to inhibit ovulation completely in cycling rats, while 500 micrograms (135 micrograms/kg) were required to inhibit mating induced ovulation in 8 of 11 rabbits."( Species differences in the sensitivity to a GnRH antagonist.
Bardin, CW; Ladishenskaya, A; Limonta, P; Pavlou, S; Sundaram, K; Thau, RB, 1985
)
0.27
" Dose-response curves were similar for each steroid, and the GnRH analogue and GnRH gave parallel curves with minimal effective concentrations being 1 and 10 ng/ml, respectively."( Effect of gonadotrophin releasing hormone upon the pattern of steroidogenesis in isolated preovulatory rat follicles.
Ekholm, C; Hedin, L; Hillensjö, T, 1984
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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
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
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
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
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
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
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
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
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

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
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.91

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.91 (24.57)
Research Supply Index5.04 (2.92)
Research Growth Index3.95 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews5 (3.27%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies2 (1.31%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other14 (100.00%)84.16%
Other146 (95.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]