Page last updated: 2024-12-05

piperoxan

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Description

Piperoxan: A benzodioxane alpha-adrenergic blocking agent with considerable stimulatory action. It has been used to diagnose PHEOCHROMOCYTOMA and as an antihypertensive agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6040
CHEMBL ID31836
SCHEMBL ID83631
MeSH IDM0016888

Synonyms (57)

Synonym
piperoxan
1,4-benzodioxane, 2-(piperidinomethyl)-
piperoxane
piperoxan [inn:ban]
piperidine, 1-((2,3-dihydro-1,4-benzodioxin-2-yl)methyl)-
piperoxano [inn-spanish]
2-piperidinomethyl-1,4-benzodioxan
f933
piperoxane [inn-french]
1,4-benzodioxan, 2-(piperidinomethyl)-
fourneau 933
brn 0222516
benodaine
piperoxanum [inn-latin]
933f
piperidine, 1-(1,4-benzodioxan-2-ylmethyl)-
PDSP2_001085
PDSP1_001101
NCGC00160643-01
f-933
(rs)-piperoxane
CHEMBL31836 ,
fourneau-933
L001002
1-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)piperidine
1-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidine(piperoxan)
piperoxan1-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidine
1-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-piperidine
bdbm50017720
59-39-2
piperoxanum
unii-9zcs27634y
piperoxano
9zcs27634y ,
5-20-03-00452 (beilstein handbook reference)
dtxsid1046269 ,
cas-59-39-2
dtxcid9026269
tox21_111950
4(5)-amino-5(4)-imidazolecarboxamide hydrochloride
piperoxan [inn]
piperoxan [mi]
(+/-)-piperoxane
165963-28-0
piperidine,1-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]-
SCHEMBL83631
1-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]piperidine
piperidinomethylbenzodioxan
1-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)piperidine #
2-piperidinomethyl-1,4-benzodioxane
LYKMMUBOEFYJQG-UHFFFAOYSA-N
1-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)piperidine
AKOS030227988
AS-70066
1-((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)piperidine
BCP19333
Q3389064

Research Excerpts

Overview

Piperoxane is an alpha 2-noradrenergic antagonist with demonstrated excitatory effects on neurons in the locus coeruleus. Piperoxane causes a corresponding increase in norepinephrine in many forebrain areas.

ExcerptReferenceRelevance
"Piperoxane is an alpha 2-noradrenergic antagonist with demonstrated excitatory effects on neurons in the locus coeruleus, causing a corresponding increase in norepinephrine in many forebrain areas. "( Influence of the alpha 2 noradrenergic antagonist piperoxane on longevity in the Fischer-344 rat: a preliminary report.
Compton, DM; Dietrich, KL; Smith, JS, 1995
)
1.99

Treatment

The piperoxane-treated rats lived an average of 127.1 days longer than the saline- treated rats. Pretreatment with phentolamine (10 mg/kg) did not antagonize this effect.

ExcerptReferenceRelevance
"The piperoxane-treated rats lived an average of 127.1 days longer than the saline-treated rats."( Influence of the alpha 2 noradrenergic antagonist piperoxane on longevity in the Fischer-344 rat: a preliminary report.
Compton, DM; Dietrich, KL; Smith, JS, 1995
)
1.03
"Pretreatment with piperoxane (10 mg/kg) antagonized this effect but pretreatment with phentolamine (10 mg/kg) did not."( Effects of clonidine on habituation and sensitization of acoustic startle in normal, decerebrate and locus coeruleus lesioned rats.
Aghajanian, GK; Cedarbaum, JM; Davis, M; Gendelman, DS, 1977
)
0.58

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"4 X 10(-6) M) produced parallel shifts to the right of the dose-response curves to noradrenaline and oxymetazoline in isolated strips of cat splenic capsule."( The effects of labetalol (AH 5158) on adrenergic transmission in the cat spleen.
Blakeley, AG; Summers, RJ, 1977
)
0.26
" 6 In isolated strips of cat splenic capsule, piperoxan produced a shift to the right of the dose-response curve to noradrenaline with no change of the maximum response."( The effects of piperoxan on uptake of noradrenaline and overflow of transmitter in the isolated blood perfused spleen of the cat.
Blakeley, AG; Summers, RJ, 1978
)
0.87
" A dose-response curve of the lowering effect on intraocular pressure (IOP) has been made and compared with the dose-response cure obtained after intravenous administration."( The central ocular hypotensive effect of clonidine.
Innemee, HC; van Zwieten, PA, 1979
)
0.26
" Routine enantiomeric analyses were successfully carried out on samples taken from animals dosed orally with the racemic drugs, providing important data on the possible levels of exposure to individual enantiomers during toxicity testing."( Advantages of achiral h.p.l.c. as a preparative step for chiral analysis in biological samples and its use in toxicokinetic studies.
Beresford, AP; Caswell, K; Chambers, R; Kirk, IP, 1992
)
0.28
" (+/-)-Propranolol caused rightward shifts, usually parallel, of the dose-response curves for (-)-isoprenaline."( The antinociceptive action of some beta-adrenoceptor agonists in mice.
Bentley, GA; Starr, J, 1986
)
0.27
" The dose-response relationships for the effects of alpha 2-adrenoceptor antagonists on retinal TH activity were similar to those for the effects on brain noradrenergic neurons, where alpha 2-adrenoceptors have been shown to be involved in the autoregulation of neuronal activity."( Alpha 2-adrenergic receptors influence tyrosine hydroxylase activity in retinal dopamine neurons.
Iuvone, PM; Rauch, AL, 1983
)
0.27
" The corresponding dose-response curves, determined in control- and RU24722-treated rats, were expressed as a function of the quantity of TH contained either in the whole recorded LC or in the 100 microns-wide coronal interval surrounding the recording site."( Relationship between tyrosine hydroxylase content and noradrenergic cell reactivity to piperoxane: an in vivo voltammetric approach in the rat locus coeruleus.
Debure, L; Pujol, JF; Renaud, B; Rousset, C; Vachette, C, 1994
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency0.08490.000221.22318,912.5098AID743036
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.72000.00021.874210.0000AID167198
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.14000.00031.09147.7625AID167200
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.09500.00000.929610.0000AID35187
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.14000.00031.09147.7625AID167200
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.09500.00000.970810.0000AID35187
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.14000.00031.06917.7625AID167200
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.09500.00000.937510.0000AID35187
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.72000.00021.270410.0000AID167198
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.14000.00100.39573.3000AID167200
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.72000.00001.819410.0000AID167198
[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-2A adrenergic receptorHomo sapiens (human)Kd0.31620.00370.16750.5754AID33125
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd1.09770.00020.52667.5858AID196984; AID35643
Alpha-2B adrenergic receptorHomo sapiens (human)Kd0.31620.00370.16750.5754AID33125
Alpha-2C adrenergic receptorHomo sapiens (human)Kd0.31620.00370.16750.5754AID33125
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd0.58880.00020.62779.3325AID196987
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd0.58880.00020.62779.3325AID196987
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd0.58880.00020.62779.3325AID196987
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd1.09770.00020.89627.5858AID196984; AID35643
Alpha-1D adrenergic receptorHomo sapiens (human)Kd0.31620.00000.19451.2882AID33125
Alpha-1A adrenergic receptorHomo sapiens (human)Kd0.31620.00000.20481.2882AID33125
Alpha-1B adrenergic receptorHomo sapiens (human)Kd0.31620.00000.11991.2882AID33125
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd1.09770.00020.51397.5858AID196984; AID35643
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (80)

Processvia Protein(s)Taxonomy
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)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
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)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
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)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID33125In vitro relative blocking action (pA2) of the post-synaptic Alpha adrenergic receptor from rat and rabbit aorta.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID35860Antagonistic activity against Alpha-1 adrenergic receptor in the epidermal portion of the rat vas deferens1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID36504Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes Alpha-2 adrenergic receptor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID235866Index of alpha1/alpha2 adrenoceptor binding selectivity.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID233434Selectivity ratio is the ratio between pA2 values of alfa2 and alfa1 adrenoceptors1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID35359Antagonistic activity against Alpha-2 adrenergic receptor in the prostatic portion of the rat vas deferens1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID35858Antagonist potency towards alpha-1 adrenergic receptor in the rat electrically stimulated vas deferens with reference to phenylephrine1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID196984Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats. 1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID35642Alpha-2 adrenergic receptor pA2 value against clonidine in vitro experiment in rat vas deferens1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID167200Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes alpha2 adrenoceptor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID235864Index of alpha1/alpha2 adrenoceptor antagonist selectivity at post junctional vascular sites in vivo.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID167198Inhibition of specific [3H]-prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36059In vitro for relative blocking action (pA2) of Presynaptic Alpha-2 adrenergic receptor from guinea pig ileum.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID35563Agonist potency towards alpha-1 adrenergic receptor in the rat isolated electrically stimulated vas deferens with reference to phenylephrine (postjunctional)1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID235865Index of alpha1/alpha2 adrenoceptor antagonist selectivity at pre and postsynaptic sites in vitro.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36489Agonist potency towards alpha-2 adrenergic receptor in the mouse isolated electrically stimulated vas deferens with reference to clonidine (prejunctional)1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID36426Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID35357Antagonist potency towards alpha-2 adrenergic receptor in the rat electrically stimulated vas deferens with reference to P-aminoclonidine1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID35187Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
AID36491Antagonist potency towards alpha-2 adrenergic receptor in the mouse isolated electrically stimulated vas deferens with reference to idazoxan (prejunctional)1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID35643Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID35565Antagonist potency towards alpha-1 adrenergic receptor in the rat isolated electrically stimulated vas deferens with reference to pA2 idazoxan (postjunctional)1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
AID233641Ratio of pA2 value against alpha2 to alpha-1 adrenoceptor1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID196987Antagonist activity against B-HT 933-induced alpha-2-adrenoceptor-mediated vasoconstriction in pithed normotensive rats1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (175)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990140 (80.00)18.7374
1990's27 (15.43)18.2507
2000's4 (2.29)29.6817
2010's3 (1.71)24.3611
2020's1 (0.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.91

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.91 (24.57)
Research Supply Index5.24 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (1.08%)5.53%
Reviews6 (3.24%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other177 (95.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]