Page last updated: 2024-11-13

2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1h-imidazole

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Description

2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1H-imidazole: an alpha2C agonist and alpha2A antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24906198
CHEMBL ID495095
MeSH IDM0552885

Synonyms (6)

Synonym
CHEMBL495095 ,
allyphenyline
bdbm50412245
2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1h-imidazole
1043533-91-0
2-[1-(2-prop-2-enylphenoxy)ethyl]-4,5-dihydro-1h-imidazole
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)Ki0.08510.00100.03000.0851AID536940
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.02820.00010.532610.0000AID682996; AID772375
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.05750.00010.807410.0000AID339888; AID536932; AID682997; AID772379
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.33880.00020.725710.0000AID339892; AID536936; AID683002; AID772378
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.08510.00030.483410.0000AID339896; AID536940; AID683157; AID772377
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)16.90000.00091.901410.0000AID683153
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2C adrenergic receptorHomo sapiens (human)EC50 (µMol)0.05010.00050.55416.7100AID339898; AID536941; AID683158; AID772380
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC50 (µMol)0.05010.00301.29038.3000AID339898
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)EC50 (µMol)0.05010.00301.02226.8600AID339898
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)EC50 (µMol)0.05010.00300.86696.8600AID339898
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)EC50 (µMol)0.05010.00301.11276.8600AID339898
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)EC50 (µMol)0.05010.00301.39378.3000AID339898
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)EC50 (µMol)0.05010.00300.90516.8600AID339898
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)EC50 (µMol)0.05010.00300.90516.8600AID339898
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (84)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID772374Agonist activity at human 5HT1A receptor relative to control2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID339892Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2B receptor expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID772382Antagonist activity at human alpha2A AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID772371Agonist activity at human alpha2C AR assessed as intrinsic activity2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID536954Reduction in morphine tolerance acquisition in CD1 mouse assessed as morphine analgesic effect incidence at 0.05 mg/kg, ip bid administered 15 mins before last morphine dosing by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID339889Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID536932Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID536956Reduction in morphine dependence expression in CD1 mouse assessed as decrease in somatic signs at 0.05 mg/kg, ip bid administered 15 mins before last morphine dosing by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID683158Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID772378Binding affinity at human alpha2B AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID536940Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID683000Agonist activity at human 5HT1A receptor expressed in HeLa cells assessed as [35S]GTPgammaS binding incubated for 20 mins prior to [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting relative to 8-OH-DPAT2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683002Displacement of [3H]RX821002 from human alpha2B adrenoceptor expressed in CHO cells after 30 mins by scintillation counting2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID772380Agonist activity at human alpha2C AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID772372Binding affinity to I2 imidazoline binding site in rat brain membrane2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID683023Antidepressant activity in CD1 mouse assessed as decrease in immobility time at 0.012 mg/kg, ip after 15 mins by forced swim test relative to vehicle-treated control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683153Inhibition of human ERG expressed in HEK293 cells after 240 secs by patch clamp assay2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683001Agonist activity at human 5HT1A receptor expressed in HeLa cells assessed as [35S]GTPgammaS binding incubated for 20 mins prior to [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID772381Agonist activity at human alpha2B AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID339894Agonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID339888Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID536942Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry relative to (-)noradrenaline2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID772377Binding affinity at human alpha2C AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID683022Antidepressant activity in CD1 mouse assessed as decrease in immobility time at 0.2 mg/kg, ip after 15 mins by forced swim test relative to vehicle-treated control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID536947Reduction in morphine tolerance acquisition in CD1 mouse assessed as morphine analgesic effect incidence at 0.05 mg/kg, ip administered as single dose 15 mins before last morphine dosing on test day post morphine challenge by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID339898Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID683021Antidepressant activity in CD1 mouse assessed as decrease in immobility time at 0.025 mg/kg, ip after 15 mins by forced swim test relative to vehicle-treated control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683160Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis relative to control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID682996Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID772379Binding affinity at human alpha2A AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID536957Reduction in morphine dependence expression in CD1 mouse assessed as decrease in frequency of jumping at 0.05 mg/kg, ip bid administered 15 mins before last morphine dosing by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID536936Displacement of [3H]RX821002 from human alpha2B adrenoceptor expressed in CHO cells2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID682997Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683004Antagonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as reduction in clonidine-induced extracellular acidification after 30 mins by cytosensor microphysiometric analysis2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683024Antidepressant activity in CD1 mouse assessed as decrease in immobility time at 0.5 mg/kg, ip after 15 mins by forced swim test relative to vehicle-treated control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID772370Antidepressant-like activity in mouse assessed as reduction in immobility time at 0.05 mg/kg, ip by forced swimming test2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID536941Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID339899Intrinsic activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification relative to (-)-noradrenaline2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID536935Antagonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as effect on agonist-induced extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID339896Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID772375Binding affinity at human 5HT1A receptor2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID683003Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID536937Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID536938Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry relative to (-)noradrenaline2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID536955Reduction in morphine dependence expression in CD1 mouse assessed as decrease in expression of naloxone-precipitated withdrawal syndrome at 0.05 mg/kg, ip bid administered 15 mins before last morphine dosing by radiant heat tail flick test2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
AID772376Agonist activity at human 5HT1A receptor2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID683159Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis relative to control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID339890Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
AID683019Antidepressant activity in CD1 mouse assessed as decrease in immobility time at 0.05 mg/kg, ip after 15 mins by forced swim test relative to vehicle-treated control2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
AID683157Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation counting2012ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's6 (85.71)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.75

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 Index12.75 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.75)

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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]