Page last updated: 2024-11-12

cj 15,208

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

Cross-References

ID SourceID
PubMed CID44583372
CHEMBL ID506616
SCHEMBL ID12368055
MeSH IDM0536087

Synonyms (9)

Synonym
c[l-phe-d-pro-l-phe-l-trp]
bdbm50268462
cj-15208 ,
CHEMBL506616 ,
SCHEMBL12368055
(3s,6s,9s,12r)-3,9-dibenzyl-6-(1h-indol-3-ylmethyl)-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone
(3s,6s,9s,14ar)-6-((1h-indol-3-yl)methyl)-3,9-dibenzyldecahydropyrrolo[1,2-a][1,4,7,10]tetraazacyclododecine-1,4,7,10-tetraone
210236-47-8
AKOS040748141
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ki4.15000.00000.53939.4000AID1872117; AID727344
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.56300.00000.38458.6000AID1872116; AID1872119; AID727343
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki0.03270.00000.18683.9500AID1872118; AID1872121; AID727345
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.14250.00010.813310.0000AID1630474; AID375498
Mu-type opioid receptorHomo sapiens (human)Ki0.12850.00000.419710.0000AID1630477; AID375494
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)2.60000.00020.75218.0140AID1630475
Delta-type opioid receptorHomo sapiens (human)Ki51.00000.00000.59789.9300AID1630478; AID375495
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)0.24350.00001.201110.0000AID1630473; AID375497
Kappa-type opioid receptorHomo sapiens (human)Ki0.03050.00000.362410.0000AID1630479; AID375493
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)Kb0.01020.00000.03310.1792AID1872104
Kappa-type opioid receptorHomo sapiens (human)Kb0.06520.00030.05000.2640AID1872115
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID1401122Displacement of [3H]DAMGO from mu-opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method2017European journal of medicinal chemistry, Dec-01, Volume: 141Selective kappa opioid antagonists for treatment of addiction, are we there yet?
AID1872115Binding affinity to human KOP stably expressed in CHO cell membrane assessed as [35S]GTPgammaS binding incubated for 90 mins by liquid scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID757452Neurotoxicity in C57BL/6J mouse assessed as sedative effect at 10 to 60 mg/kg, po after 60 mins by rotarod test2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1630475Binding affinity to DOR (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID757459Antinociceptive activity in C57BL/6J mouse at 1 to 60 mg/kg, po after 60 mins by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1872121Displacement of [3H]diprenorphine from rat KOP stably expressed in CHO cell membrane2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID727343Displacement of [3H]DAMGO from rat cloned MOR expressed in CHO cells after 90 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID375494Displacement of [3H]diprenorphine from human cloned mu receptor by cell based assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID375495Displacement of [3H]diprenorphine from human cloned delta receptor by cell based assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID727471Displacement of DPDPE from DOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID1872119Displacement of [3H]DAMGO from rat MOP stably expressed in CHO cell membrane2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID727337Antinociceptive activity in icv dosed C57B1/6J mouse assessed as tail withdrawal latency measured in every 10 mins for 1 hr by warm water tail withdrawal assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID1872129Antinociceptive activity in icv dosed C57BL/6J mouse assessed as tail withdrawal latency from warm water2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872117Displacement of [3H]DPDPE from mouse DOP stably expressed in CHO cell membrane incubated for 90 mins by scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID375488Binding affinity to kappa opioid receptor in guinea pig brain membrane2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID1401123Displacement of [3H]DPDPE from delta-opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method2017European journal of medicinal chemistry, Dec-01, Volume: 141Selective kappa opioid antagonists for treatment of addiction, are we there yet?
AID757449Prevention of cocaine-induced reinstatement of extinguished cocaine seeking behavior in C57BL/6J mouse at 30 to 60 mg/kg, po qd for 2 days followed by additional cycle of cocaine place conditioning at 30 mins post last dose measured on day 32013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1630474Binding affinity to MOR (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID727345Displacement of [3H]diprenorphine from rat cloned KOR expressed in CHO cells after 90 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID757455Antinociceptive activity in C57BL/6J mouse at 60 mg/kg, po after 140 mins by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID757456Antagonist activity at kappa opioid receptor in po dosed C57BL/6J mouse assessed as inhibition of po dosed U50,488-induced antinociception effect incubated for 3 hrs prior to testing by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1630477Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID1630478Displacement of [3H]diprenorphine from human DOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID757458Antinociceptive activity in C57BL/6J mouse at 0.3 mg/kg, po after 60 mins by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID375493Displacement of [3H]diprenorphine from human cloned kappa opioid receptor by cell based assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID757460Antinociceptive activity in po dosed C57BL/6J mouse after 40 mins by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID727344Displacement of [3H]DPDPE from mouse cloned DOR expressed in CHO cells after 90 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID1872128Toxicity in icv dosed C57BL/6J mouse assessed as antinociceptive activity tolerance2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872116Displacement of [3H]DAMGO from rat MOP stably expressed in CHO cell membrane incubated for 90 mins by scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID375497Antagonist activity at human cloned kappa opioid receptor assessed as inhibition of 50 nM U50488H-stimulated GTPgammaS binding by cell based assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID727470Displacement of DAGO from MOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID375498Antagonist activity at human cloned mu opioid receptor assessed as inhibition of 100 nM loperamide-stimulated GTPgammaS binding by cell based assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID1872056Half life in mouse liver microsomes2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1401121Displacement of [3H]CI-977 from kappa opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method2017European journal of medicinal chemistry, Dec-01, Volume: 141Selective kappa opioid antagonists for treatment of addiction, are we there yet?
AID375496Ratio of Ki for human cloned mu opioid receptor to Ki for human cloned kappa opioid receptor2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID757457Antinociceptive activity in C57BL/6J mouse at 1 to 30 mg/kg, po after 120 mins by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1401124Antagonist activity at KOR in Japanese white rabbit vas deferens assessed as inhibition of asimadoline-induced suppression of electric field stimulated twitch response after 30 mins2017European journal of medicinal chemistry, Dec-01, Volume: 141Selective kappa opioid antagonists for treatment of addiction, are we there yet?
AID375492Antagonist activity at kappa opioid receptor in rabbit vas deferens assessed as reversal of asimadoline-suppressed electrically-stimulated twitch response2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID1872104Binding affinity to human MOP stably expressed in CHO cell membrane assessed as [35S]GTPgammaS binding incubated for 90 mins by liquid scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID757451Prevention of stress-induced reinstatement of extinguished cocaine seeking behavior in C57BL/6J mouse at 60 mg/kg, po qd for 2 days measured 3 hrs post last dose by forced swim test2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID1630476Antagonist activity against KOR in rabbit vas deferens smooth muscles assessed as inhibition of asimadoline-induced response2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID1872118Displacement of dynorphin A-(1-13) amide (Dyn A-(1-13) amide) from rat KOP stably expressed in CHO cell membrane incubated for 90 mins by scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID375491Ratio of IC50 for mu opioid receptor in guinea pig brain membrane to IC50 for kappa opioid receptor in guinea pig brain membrane2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID757450Prevention of stress-induced reinstatement of extinguished cocaine cocaine seeking behavior in C57BL/6J mouse at 30 mg/kg, po qd for 2 days measured 3 hrs post last dose by forced swim test2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID375489Binding affinity to mu opioid receptor in guinea pig brain membrane2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID1630479Displacement of [3H]U69,593 from human KOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID375490Binding affinity to delta opioid receptor in guinea pig brain membrane2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
AID757454Antagonist activity at kappa opioid receptor in po dosed C57BL/6J mouse assessed as inhibition of icv dosed U50,488-induced antinociception effect incubated for 3 hrs prior to testing by warm water tail withdrawal assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
AID727472Displacement of [3H]Cl-977 from KOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Development of κ opioid receptor antagonists.
AID1630473Binding affinity to KOR (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
AID1872127Antinociceptive activity in icv dosed C57BL/6J mouse assessed as tail withdrawal latency from warm water measured after 1 hr for every 10 mins2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's4 (66.67)24.3611
2020's1 (16.67)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 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]