Page last updated: 2024-09-25

ly 274614

Description

LY 235959: RN refers to (3S-(3alpha,4aalpha,6beta,8aalpha))-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID131938
CHEMBL ID1448057
SCHEMBL ID195083
MeSH IDM0192936

Synonyms (33)

Synonym
ly 235959
ly-235959
decahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acid
3-isoquinolinecarboxylic acid, decahydro-6-(phosphonomethyl)-, (3s-(3alpha,4aalpha,6beta,8aalpha))-
tocris-1019
NCGC00024942-01
BPBIO1_001216
BIOMOL-NT_000192
NCGC00024942-02
(3s,4ar,6s,8ar)-6-(phosphonomethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
ly274614
ly 274614
136109-04-1
3-isoquinolinecarboxylic acid, decahydro-6-(phosphonomethyl)-, (3alpha,4aalpha,6beta,8aalpha)-
3-isoquinolinecarboxylic acid, decahydro-6-(phosphonomethyl)-, (3s,4ar,6s,8ar)-
ly-274614
unii-ar2bhc0c6p
ar2bhc0c6p ,
137433-06-8
SCHEMBL195083
CHEMBL1448057
[3s-(3?,4a?,6?,8a?)]-decahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acid)
AKOS024456335
SR-01000597462-3
sr-01000597462
J-007021
DTXSID20929264
ly-235959;ly235959
Q6460410
(3s,4ar,6s,8ar)-6-(phosphonomethyl)decahydroisoquinoline-3-carboxylic acid
(3s)-(3-alpha-4-alpha,alpha-6-beta-8-alpha,alpha)-decahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acid
DTXSID101336227
[3s-(3alpha,4aalpha,6beta,8aalpha)]-decahydro-6-(phosp honomethyl)-3-isoquinolinecarboxylic acid)

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (95)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's36 (37.89)18.2507
2000's42 (44.21)29.6817
2010's13 (13.68)24.3611
2020's4 (4.21)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 (%)
Trials0 (0.00%)5.53%
Reviews2 (2.08%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other94 (97.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (2)

ArticleYear
The selective and competitive N-methyl-D-aspartate receptor antagonist, (-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid, prevents synaptic toxicity induced by amyloid-β in mice.
Neuroscience, Sep-29, Volume: 192
2011
Protection against amphetamine-induced neurotoxicity toward striatal dopamine neurons in rodents by LY274614, an excitatory amino acid antagonist.
Neuropharmacology, Volume: 31, Issue: 10
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (6)

ArticleYear
Opioid antinociception, tolerance and dependence: interactions with the N-methyl-D-aspartate system in mice.
Behavioural pharmacology, Volume: 22, Issue: 5-6
2011
Role of morphine maintenance dose in the development of tolerance and its attenuation by an NMDA receptor antagonist.
Psychopharmacology, Volume: 148, Issue: 1
2000
The competitive NMDA receptor antagonist LY235959 modulates the progression of morphine tolerance in rats.
Psychopharmacology, Volume: 142, Issue: 2
1999
Differential effects of LY235959, a competitive antagonist of the NMDA receptor on kappa-opioid receptor agonist induced responses in mice and rats.
Brain research, Feb-07, Volume: 747, Issue: 2
1997
Effect of antagonism of the NMDA receptor on tolerance to [D-Pen2,D-Pen5]enkephalin, a delta 1-opioid receptor agonist.
Peptides, Volume: 17, Issue: 2
1996
Effects of N-methyl-D-aspartate receptor antagonists on the analgesia and tolerance to D-Ala2, Glu4 deltorphin II, a delta 2-opioid receptor agonist in mice.
Brain research, May-06, Volume: 719, Issue: 1-2
1996
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (3)

ArticleYear
Competitive and non-competitive NMDA antagonists block the development of antinociceptive tolerance to morphine, but not to selective mu or delta opioid agonists in mice.
Pain, Volume: 68, Issue: 2-3
1996
Modulation of morphine tolerance by the competitive N-methyl-D-aspartate receptor antagonist LY274614: assessment of opioid receptor changes.
The Journal of pharmacology and experimental therapeutics, Volume: 268, Issue: 1
1994
The NMDA receptor antagonists, LY274614 and MK-801, and the nitric oxide synthase inhibitor, NG-nitro-L-arginine, attenuate analgesic tolerance to the mu-opioid morphine but not to kappa opioids.
Pain, Volume: 56, Issue: 1
1994
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]