gr 89696 profile

GR 89696: a potent & selective kappa opioid receptor agonist; RN given refers to (E)-2-butenedioate(1:1); RN for parent cpd not available 11/92; GR 103545 is the (R)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	3505
CHEMBL ID	603370
CHEBI ID	91965
SCHEMBL ID	4545382
MeSH ID	M0194417

Synonym
BRD-A93659613-051-03-6
gtpl1649
LOPAC0_000572
gr 89696
NCGC00025181-03
NCGC00025181-02
NCGC00015465-05
L003484
methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
gr-89696
bdbm50027433
chembl603370 ,
gr 85571
CCG-204661
NCGC00015465-03
NCGC00015465-04
SCHEMBL4545382
gr89696
J363.375F ,
CHEBI:91965
4-[(3,4-dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid methyl ester
DTXSID50875164
126766-31-2
methyl 4-[(3,4-dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylate
Q5514393
SDCCGSBI-0050554.P002
NCGC00015465-08
YXV3Q43RS9 ,
1-piperazinecarboxylic acid, 4-((3,4-dichlorophenyl)acetyl)-3-(1-pyrrolidinylmethyl)-, methyl ester
1-piperazinecarboxylic acid, 4-(2-(3,4-dichlorophenyl)acetyl)-3-(1-pyrrolidinylmethyl)-, methyl ester
(+/-)-methyl 4-((3,4-dichlorophenyl)acetyl)-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
4-((3,4-dichlorophenyl)acetyl)-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylic acid methyl ester
unii-yxv3q43rs9
CS-0653690
HY-107747A
gr 89696 (free base)

Class	Description
acetamides	Compounds with the general formula RNHC(=O)CH3.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	39.8107	0.1000	20.8793	79.4328	AID588453
TDP1 protein	Homo sapiens (human)	Potency	25.9290	0.0008	11.3822	44.6684	AID686978
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	23.7781	0.0355	20.9770	89.1251	AID504332
chromobox protein homolog 1	Homo sapiens (human)	Potency	25.1189	0.0060	26.1688	89.1251	AID488953
Ataxin-2	Homo sapiens (human)	Potency	28.1838	0.0119	12.2221	68.7989	AID588378
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	33.8078	0.0601	10.7453	37.9330	AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Mu-type opioid receptor	Homo sapiens (human)	Ki	0.0004	0.0000	0.4197	10.0000	AID481114
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0005	0.0000	0.2018	6.4240	AID1901076
Kappa-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0020	0.0000	1.2011	10.0000	AID148434
Kappa-type opioid receptor	Homo sapiens (human)	Ki	0.1802	0.0000	0.3624	10.0000	AID1255650; AID601794
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Mu-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
sensory perception	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Mu-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
behavioral response to ethanol	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of neurogenesis	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of Wnt protein secretion	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Mu-type opioid receptor	Homo sapiens (human)
calcium ion transmembrane transport	Mu-type opioid receptor	Homo sapiens (human)
cellular response to morphine	Mu-type opioid receptor	Homo sapiens (human)
regulation of cellular response to stress	Mu-type opioid receptor	Homo sapiens (human)
regulation of NMDA receptor activity	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
immune response	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
chemical synaptic transmission	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception	Kappa-type opioid receptor	Homo sapiens (human)
locomotory behavior	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
response to insulin	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of dopamine secretion	Kappa-type opioid receptor	Homo sapiens (human)
negative regulation of luteinizing hormone secretion	Kappa-type opioid receptor	Homo sapiens (human)
response to nicotine	Kappa-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
maternal behavior	Kappa-type opioid receptor	Homo sapiens (human)
eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
response to estrogen	Kappa-type opioid receptor	Homo sapiens (human)
estrous cycle	Kappa-type opioid receptor	Homo sapiens (human)
response to ethanol	Kappa-type opioid receptor	Homo sapiens (human)
regulation of saliva secretion	Kappa-type opioid receptor	Homo sapiens (human)
behavioral response to cocaine	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of temperature stimulus	Kappa-type opioid receptor	Homo sapiens (human)
defense response to virus	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to lipopolysaccharide	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to glucose stimulus	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of p38MAPK cascade	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Kappa-type opioid receptor	Homo sapiens (human)
response to acrylamide	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
conditioned place preference	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
negative regulation of receptor internalization	Ataxin-2	Homo sapiens (human)
regulation of translation	Ataxin-2	Homo sapiens (human)
RNA metabolic process	Ataxin-2	Homo sapiens (human)
P-body assembly	Ataxin-2	Homo sapiens (human)
stress granule assembly	Ataxin-2	Homo sapiens (human)
RNA transport	Ataxin-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G-protein alpha-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor activity	Mu-type opioid receptor	Homo sapiens (human)
beta-endorphin receptor activity	Mu-type opioid receptor	Homo sapiens (human)
voltage-gated calcium channel activity	Mu-type opioid receptor	Homo sapiens (human)
protein binding	Mu-type opioid receptor	Homo sapiens (human)
morphine receptor activity	Mu-type opioid receptor	Homo sapiens (human)
G-protein beta-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
protein binding	Kappa-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Kappa-type opioid receptor	Homo sapiens (human)
dynorphin receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Kappa-type opioid receptor	Homo sapiens (human)
RNA binding	Ataxin-2	Homo sapiens (human)
epidermal growth factor receptor binding	Ataxin-2	Homo sapiens (human)
protein binding	Ataxin-2	Homo sapiens (human)
mRNA binding	Ataxin-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endosome	Mu-type opioid receptor	Homo sapiens (human)
endoplasmic reticulum	Mu-type opioid receptor	Homo sapiens (human)
Golgi apparatus	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
axon	Mu-type opioid receptor	Homo sapiens (human)
dendrite	Mu-type opioid receptor	Homo sapiens (human)
perikaryon	Mu-type opioid receptor	Homo sapiens (human)
synapse	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
neuron projection	Mu-type opioid receptor	Homo sapiens (human)
nucleoplasm	Kappa-type opioid receptor	Homo sapiens (human)
mitochondrion	Kappa-type opioid receptor	Homo sapiens (human)
cytosol	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
membrane	Kappa-type opioid receptor	Homo sapiens (human)
sarcoplasmic reticulum	Kappa-type opioid receptor	Homo sapiens (human)
T-tubule	Kappa-type opioid receptor	Homo sapiens (human)
dendrite	Kappa-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Kappa-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
perikaryon	Kappa-type opioid receptor	Homo sapiens (human)
axon terminus	Kappa-type opioid receptor	Homo sapiens (human)
postsynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
neuron projection	Kappa-type opioid receptor	Homo sapiens (human)
cytoplasm	Ataxin-2	Homo sapiens (human)
Golgi apparatus	Ataxin-2	Homo sapiens (human)
trans-Golgi network	Ataxin-2	Homo sapiens (human)
cytosol	Ataxin-2	Homo sapiens (human)
cytoplasmic stress granule	Ataxin-2	Homo sapiens (human)
membrane	Ataxin-2	Homo sapiens (human)
perinuclear region of cytoplasm	Ataxin-2	Homo sapiens (human)
ribonucleoprotein complex	Ataxin-2	Homo sapiens (human)
cytoplasmic stress granule	Ataxin-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay ID	Title	Year	Journal	Article
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347410	qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library	2019	Cellular signalling, 08, Volume: 60	A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504836	Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation	2002	The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16	Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347057	CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378	qHTS for Inhibitors of ATXN expression: Validation
AID1347151	Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings 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.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058	CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050	Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347059	CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349	qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID601794	Displacement of [3H]U69593 from kappa opioid receptor	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
AID481114	Displacement of [(3)H]U69593 from mu opioid receptor	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
AID148434	In vitro agonist activity at kappa opioid receptor in rabbit vas deferens.	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1901076	Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay	2022	European journal of medicinal chemistry, Feb-15, Volume: 230	Synthesis of 8-aminomorphans with high KOR affinity.
AID132781	In vivo antinociceptive activity was determined using mouse acetylcholine induced abdominal constriction test following subcutaneous administration; range (0.00012-0.00045)	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1255653	Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1255652	Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1255660	Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID224585	In vitro inhibitory activity against mu specific tissue of rat vas deferens	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1255651	Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID147942	In vitro inhibitory activity against delta specific tissue of hamster vas deferens	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1255650	Binding affinity to kappa opioid receptor (unknown origin)	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID481113	Agonist activity at kappa opioid receptor in rabbit vas deferens	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
AID176998	In vivo antinociceptive activity was determined using rat paw pressure test following subcutaneous administration; range (0.00058-0.0014)	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID132778	In vivo antinociceptive activity was determined using mouse acetylcholine induced abdominal constriction test following oral administration; range (0.005-0.035)	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1255661	Intrinsic activity at kappa opioid receptor in human HEK293 cells at 1 uM after 30 mins by [35S]GTPgammaS binding assay relative to U-69593	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID148441	Binding constant in rabbit vas deferens (LVD) antagonized by naloxone	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID132782	In vivo antinociceptive activity was determined using mouse acetylcholine induced abdominal constriction test following subcutaneous administration; range (0.00027-0.00086)	1993	Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15	A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346329	Human kappa receptor (Opioid receptors)	2002	Nuclear medicine and biology, Jan, Volume: 29, Issue:1	[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	10 (19.61)	18.2507
2000's	11 (21.57)	29.6817
2010's	20 (39.22)	24.3611
2020's	10 (19.61)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	52 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Condition	Relationship Strength	Studies
Ache	low	2
Addiction, Opioid	low	1
Allodynia	low	2
Allodynia, Mechanical	low	2
Allodynia, Tactile	low	2
Allodynia, Thermal	low	2
Anemia, Fanconi	low	1
Arrhythmia	low	2
Arrhythmias, Cardiac	low	2
Arrythmia	low	2
Arterial Diseases, Carotid	low	1
Arterial Diseases, Common Carotid	low	1
Arterial Diseases, External Carotid	low	1
Arterial Diseases, Internal Carotid	low	1
Ataxia	low	1
Ataxia, Appendicular	low	1
Ataxia, Limb	low	1
Ataxia, Motor	low	1
Ataxia, Sensory	low	1
Ataxia, Truncal	low	1
Ataxy	low	1
Atherosclerotic Disease, Carotid	low	1
Body Weight	low	1
Bone Cancer	low	1
Bone Neoplasms	low	1
Brain Edema	low	1
Brain Ischemia	low	2
Brain Swelling	low	1
Breast Cancer	low	1
Breast Carcinoma	low	1
Breast Neoplasms	low	1
Breast Tumors	low	1
Cancer of Bone	low	1
Cancer of Breast	low	1
Cancer of the Bone	low	1
Cancer of the Breast	low	1
Cardiac Arrhythmia	low	2
Cardiac Arrhythmias	low	2
Cardiac Dysrhythmia	low	2
Cardiovascular Stroke	low	1
Carotid Artery Diseases	low	1
Carotid Artery Disorders	low	1
Carotid Atherosclerosis	low	1
Carotid Atherosclerotic Disease	low	1
Cerebral Edema	low	1
Cerebral Edema, Cytotoxic	low	1
Cerebral Edema, Vasogenic	low	1
Cerebral Ischemia	low	2
Cocaine Abuse	low	2
Cocaine Addiction	low	2
Cocaine Dependence	low	2
Cocaine-Related Disorders	low	2
Common Carotid Artery Diseases	low	1
Congenital Zika Syndrome	low	1
Congenital Zika Virus Infection	low	1
Contact Dermatitis	low	1
Coordination Impairment	low	1
Cytotoxic Brain Edema	low	1
Cytotoxic Cerebral Edema	low	1
Decerebrate Posturing	low	1
Decerebrate State	low	1
Decorticate Rigidity	low	1
Decorticate State	low	1
Degenerative Diseases, Central Nervous System	low	1
Degenerative Diseases, Nervous System	low	1
Degenerative Diseases, Neurologic	low	1
Degenerative Diseases, Spinal Cord	low	1
Degenerative Neurologic Diseases	low	1
Degenerative Neurologic Disorders	low	1
Dependence, Opioid	low	1
Depression	low	1
Depression, Involutional	low	1
Depressive Disorder, Major	low	1
Dermatitis Venenata	low	1
Dermatitis, Contact	low	1
Disease Models, Animal	low	5
Dyscoordination	low	1
Dyssynergia	low	1
Eczema, Contact	low	1
Encephalopathy, Ischemic	low	2
External Carotid Artery Diseases	low	1
Fanconi Anemia	low	1
Fanconi Hypoplastic Anemia	low	1
Fanconi Pancytopenia	low	1
Fanconi Panmyelopathy	low	1
Fanconi's Anemia	low	1
Fever, Zika	low	1
Heart Attack	low	1
Human Mammary Carcinoma	low	1
Hyperalgesia	low	2
Hyperalgesia, Mechanical	low	2
Hyperalgesia, Primary	low	2
Hyperalgesia, Secondary	low	2
Hyperalgesia, Tactile	low	2
Hyperalgesia, Thermal	low	2
Hyperalgesic Sensations	low	2
Hyperalgia	low	2
Hyperalgia, Mechanical	low	2
Hyperalgia, Primary	low	2
Hyperalgia, Secondary	low	2
Hypersensitivity, Contact	low	1
Incoordination	low	1
Injuries, Spinal Cord	low	2
Injury, Myocardial Reperfusion	low	3
Internal Carotid Artery Diseases	low	1
Intracranial Edema	low	1
Ischemia, Cerebral	low	2
Ischemic Encephalopathy	low	2
Itching	low	1
Lack of Coordination	low	1
Major Depressive Disorder	low	1
Malignant Neoplasm of Breast	low	1
Malignant Tumor of Breast	low	1
Mammary Cancer	low	1
Mammary Carcinoma, Human	low	1
Mammary Neoplasm, Human	low	1
Mammary Neoplasms, Human	low	1
Mechanical Allodynia	low	2
Mechanical Hyperalgesia	low	2
Melancholia, Involutional	low	1
Muscle Contraction	low	2
Muscle Relaxation	low	2
Myelopathy, Traumatic	low	2
Myocardial Infarct	low	1
Myocardial Infarction	low	1
Myocardial Ischemic Reperfusion Injury	low	3
Myocardial Reperfusion Injury	low	3
Neoplasms, Bone	low	1
Neoplasms, Breast	low	1
Nervous System Degenerative Diseases	low	1
Nervous System Diseases	low	1
Nervous System Disorders	low	1
Neuritis	low	1
Neuritis, Motor	low	1
Neuritis, Peripheral	low	1
Neuritis, Sensory	low	1
Neurodegenerative Diseases	low	1
Neurodegenerative Disorders	low	1
Neurologic Degenerative Conditions	low	1
Neurologic Degenerative Diseases	low	1
Neurologic Diseases, Degenerative	low	1
Neurologic Disorders	low	1
Neurological Disorders	low	1
Opiate Abuse	low	1
Opiate Addiction	low	1
Opiate Dependence	low	1
Opioid Abuse	low	1
Opioid Addiction	low	1
Opioid Dependence	low	1
Opioid Misuse	low	1
Opioid Use Disorder	low	1
Opioid-Related Disorders	low	1
Pain	low	2
Pain, Burning	low	2
Pain, Crushing	low	2
Pain, Migratory	low	2
Pain, Radiating	low	2
Pain, Splitting	low	2
Paraphrenia, Involutional	low	1
Peripheral Nerve Diseases	low	1
Peripheral Nervous System Disease	low	1
Peripheral Nervous System Diseases	low	1
Peripheral Nervous System Disorders	low	1
Peripheral Neuropathies	low	1
PNS (Peripheral Nervous System) Diseases	low	1
PNS Diseases	low	1
Polyneuritis	low	1
Post-Traumatic Myelopathy	low	2
Prescription Opioid Abuse	low	1
Prescription Opioid Misuse	low	1
Pruritis	low	1
Pruritus	low	1
Psychosis, Involutional	low	1
Reperfusion Injury, Myocardial	low	3
Rigidity, Decerebrate	low	1
Rigidity, Decorticate	low	1
Sensitivity, Contact	low	1
Spinal Cord Contusion	low	2
Spinal Cord Injuries	low	2
Spinal Cord Laceration	low	2
Spinal Cord Transection	low	2
Spinal Cord Trauma	low	2
Suffering, Physical	low	2
Tactile Allodynia	low	2
Thermal Allodynia	low	2
Tremor, Rubral	low	1
Tumors, Breast	low	1
Vasogenic Brain Edema	low	1
Vasogenic Cerebral Edema	low	1
Zika Fever	low	1
Zika Virus Disease	low	1
Zika Virus Infection	low	1
ZikV Infection	low	1

Article	Year
Myocardial resistance to ischemic and reperfusion injuries under conditions of chronic administration of opioid receptor agonists and antagonists. Bulletin of experimental biology and medicine, Volume: 145, Issue: 6	2008
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Article	Year
Evaluation of the effects of specific opioid receptor agonists in a rodent model of spinal cord injury. Spinal cord, Volume: 54, Issue: 10	2016
Neuroprotective actions of GR89696, a highly potent and selective kappa-opioid receptor agonist. British journal of pharmacology, Volume: 103, Issue: 3	1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

gr 89696

Description

Cross-References

Synonyms (36)

Drug Classes (1)

Protein Targets (9)

Potency Measurements

Inhibition Measurements

Biological Processes (47)

Molecular Functions (14)

Ceullar Components (24)

Bioassays (39)

Research

Studies (51)

Study Types

Research Highlights

Long-term Use (1)

Dosage (2)

Substance	Description	Relationhip Strength	Studies	Classes	Roles
u-50488	[no description available]	medium	10	dichlorobenzene; monocarboxylic acid amide; N-alkylpyrrolidine	analgesic; antitussive; calcium channel blocker; diuretic; kappa-opioid receptor agonist
morphine	[no description available]	medium	6	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
haloperidol	[no description available]	medium	2	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
1,3-ditolylguanidine	[no description available]	medium	2	toluenes
u 69593	[no description available]	medium	8	monocarboxylic acid amide; N-alkylpyrrolidine; organic heterobicyclic compound; oxaspiro compound	anti-inflammatory agent; diuretic; kappa-opioid receptor agonist
dizocilpine	[no description available]	medium	1	secondary amino compound; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
naloxone	[no description available]	medium	6	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
norbinaltorphimine	[no description available]	medium	4	isoquinolines
trk 820	[no description available]	medium	2	phenanthrenes
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer	[no description available]	medium	1	acetamides
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide	[no description available]	medium	1	diarylmethane
pentazocine	[no description available]	medium	1	benzazocine
brl 52537	[no description available]	medium	1	acetamides
cocaine	[no description available]	medium	2	benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid	adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic
piperidines	[no description available]	medium	2
dynorphins	[no description available]	medium	3
ici 199441	[no description available]	medium	1
naltrexone	[no description available]	medium	7	cyclopropanes; morphinane-like compound; organic heteropentacyclic compound	antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic
pf-04455242	[no description available]	medium	2
enkephalin, ala(2)-mephe(4)-gly(5)-	[no description available]	medium	4
salvinorin a	[no description available]	medium	1	organic heterotricyclic compound; organooxygen compound	metabolite; oneirogen
quinoxalines	[no description available]	medium	2	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
enkephalin, d-penicillamine (2,5)-	[no description available]	medium	3	heterodetic cyclic peptide	delta-opioid receptor agonist
bremazocine	[no description available]	medium	3
morphinans	[no description available]	medium	2	isoquinoline alkaloid fundamental parent; morphinane alkaloid
enkephalin-leu, ala(2)-arg(6)-	[no description available]	medium	1
enkephalin, leucine-2-alanine	[no description available]	medium	1
quadazocine	[no description available]	medium	1
carbamic acid	[no description available]	medium	1	carbon oxoacid; one-carbon compound; organonitrogen compound	Escherichia coli metabolite
carbamates	[no description available]	medium	1	amino-acid anion
1,8-diazabicyclo(5.4.0)undec-7-ene	[no description available]	medium	1
spiradoline	[no description available]	medium	1
n-methylnaloxone	[no description available]	medium	1
brimonidine tartrate	[no description available]	medium	1
substance p	[no description available]	medium	2	peptide	neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent
sumatriptan	[no description available]	medium	1	sulfonamide; tryptamines	serotonergic agonist; vasoconstrictor agent
histamine	[no description available]	medium	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
yohimbine	[no description available]	medium	1	methyl 17-hydroxy-20xi-yohimban-16-carboxylate	alpha-adrenergic antagonist; dopamine receptor D2 antagonist; serotonergic antagonist
pyrroles	[no description available]	medium	2	pyrrole; secondary amine
enadoline	[no description available]	medium	1

gr 89696

Description

Cross-References

Synonyms (36)

Drug Classes (1)

Protein Targets (9)

Potency Measurements

Inhibition Measurements

Biological Processes (47)

Molecular Functions (14)

Ceullar Components (24)

Bioassays (39)

Research

Studies (51)

Study Types

Related Drugs (203)

Related Conditions (193)

Research Highlights

Long-term Use (1)

Dosage (2)