Page last updated: 2024-11-11

win 51708

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

Description

WIN 51708: neurokinin-1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9803245
CHEMBL ID2206331
MeSH IDM0228314

Synonyms (15)

Synonym
win51,708
gtpl339
win 51,708
(3s,4s,7s,8r,11s,12r,15s)-8-ethynyl-3,7-dimethyl-18,20,27-triazaheptacyclo[15.11.0.0^{3,15}.0^{4,12}.0^{7,11}.0^{19,27}.0^{21,26}]octacosa-1(28),17,19,21,23,25-hexaen-8-ol
win-51708
win 51708
CHEMBL2206331
144177-30-0
win51708
NCGC00485262-01
Q27089224
(1r,3as,3br,5as,15as,15bs,17as)-1-ethynyl-2,3,3a,3b,4,5,5a,6,15,15a,15b,16,17,17a-tetradecahydro-15a,17a-dimethyl-1h-benzimidazo[2,1-b]cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-ol
(3s,4s,7s,8r,11s,12r,15s)-8-ethynyl-3,7-dimethyl-18,20,27-triazaheptacyclo[15.11.0.03,15.04,12.07,11.019,27.021,26]octacosa-1(28),17,19,21,23,25-hexaen-8-ol
DTXSID801098830
AKOS040749792

Research Excerpts

Overview

WIN 51708 is a nonpeptide antagonist of the neurokinin (NK)-1 (substance P) receptor. It possesses a dramatically higher affinity for the rat NK-1 receptor, compared with the human NK- 1 receptor.

ExcerptReferenceRelevance
"WIN 51708 is a nonpeptide antagonist of the neurokinin (NK)-1 (substance P) receptor that possesses a dramatically higher affinity for the rat NK-1 receptor, compared with the human NK-1 receptor. "( Both extracellular and transmembrane residues contribute to the species selectivity of the neurokinin-1 receptor antagonist WIN 51708.
Krause, JE; Sachais, BS, 1994
)
1.94

Bioavailability

ExcerptReferenceRelevance
"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
" The dose-response curves (0."( Substance P-(1-7) and substance P-(5-11) locally modulate dopamine release in rat striatum.
Brooks, N; Khan, S; Michael-Titus, AT; Whelpton, R, 1995
)
0.29
" The dose-response curves (0."( Evidence for modulatory effects of substance P fragments (1-4) and (8-11) on endogenous dopamine outflow in rat striatal slices.
Khan, S; Michael-Titus, AT; Whelpton, R, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))2002Molecular pharmacology, Dec, Volume: 62, Issue:6
Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))2002Molecular pharmacology, Dec, Volume: 62, Issue:6
Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))2002Molecular pharmacology, Dec, Volume: 62, Issue:6
Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))2002Molecular pharmacology, Dec, Volume: 62, Issue:6
Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
AID714450Allosteric modulation of EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 4 hrs by FRET assay in presence of para-LRB-AC422012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (46)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (21.74)18.2507
2000's24 (52.17)29.6817
2010's9 (19.57)24.3611
2020's3 (6.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.74

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 Index10.74 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other46 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]