Page last updated: 2024-11-12

methylhistaprodifen

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Cross-References

ID SourceID
PubMed CID10403687
CHEMBL ID275035
MeSH IDM0304785

Synonyms (14)

Synonym
methylhistaprodifen
2-[2-[3,3-di(phenyl)propyl]-3h-imidazol-4-yl]-n-methylethanamine
n-methylhistaprodifen
gtpl1205
PDSP1_001310
PDSP2_001294
NCGC00186016-01
L000399
CHEMBL275035
bdbm86175
n-methyl-2-(3,3-diphenylpropyl)-1h-imidazole-4-(ethanamine)
2-[2-(3,3-diphenylpropyl)-1h-imidazol-5-yl]-n-methylethanamine
Q27085437
SDCCGSBI-0633735.P001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
regulator of G-protein signaling 4Homo sapiens (human)Potency0.47440.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency10.00000.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency12.58930.02245.944922.3872AID488981
chromobox protein homolog 1Homo sapiens (human)Potency44.66840.006026.168889.1251AID488953
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency23.28090.00669.809418.4927AID1347050
flap endonuclease 1Homo sapiens (human)Potency23.77810.133725.412989.1251AID588795
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency21.79800.00378.618923.2809AID2660; AID2666; AID2667; AID2668
D(1A) dopamine receptorSus scrofa (pig)Potency23.28090.00378.108123.2809AID2667
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[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)
5-hydroxytryptamine receptor 3EHomo sapiens (human)Kd1.58490.00000.02840.1060AID5965
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Kd14.45440.00000.53588.3176AID42212
5-hydroxytryptamine receptor 3BHomo sapiens (human)Kd1.58490.00000.01370.1060AID5965
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd4.07380.00012.62198.5114AID5600
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd14.45440.00012.29338.5114AID42212
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd5.75440.00020.89627.5858AID35610
5-hydroxytryptamine receptor 1BHomo sapiens (human)Kd8.12830.07944.10398.1283AID4489
Histamine H1 receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.03980.00260.53341.2020AID86921
Histamine H1 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.15850.15851.82554.4668AID87543
5-hydroxytryptamine receptor 3AHomo sapiens (human)Kd1.58490.00000.00980.1060AID5965
Histamine H2 receptorCavia porcellus (domestic guinea pig)Kd12.58920.01170.15720.9550AID88149
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd1.58490.02342.74218.5114AID6248
5-hydroxytryptamine receptor 3DHomo sapiens (human)Kd1.58490.00000.02840.1060AID5965
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kd3.54810.00090.92823.5481AID141205
5-hydroxytryptamine receptor 3CHomo sapiens (human)Kd1.58490.00000.02840.1060AID5965
[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)
Histamine H1 receptorCavia porcellus (domestic guinea pig)Concentration4.00000.03002.67675.0000AID86272
Histamine H3 receptorCavia porcellus (domestic guinea pig)Concentration4.00003.00004.00005.0000AID86272
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3EHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3BHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3BHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3DHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3DHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3CHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3CHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
cell surface5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3BHomo sapiens (human)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (63)

Assay IDTitleYearJournalArticle
AID86427Concentration required for agonistic activity against Histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID86924Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segment2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87535Relative potency against H1 receptor in rat aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID86895Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86921Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID86925Effective concentration for agonist activity in guinea pig ileum whole segment2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID28749Concentration of the compound2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID141205Compound was evaluated for its antagonist affinity towards Muscarinic acetylcholine receptor M3 of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87215Relative potency was recorded in endothelium-denuded guinea pig aortic segment; value ranges from 399 to 526, significantly more potent than histamine (P<0.01).2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87075Negative logarithm of receptor dissociation constant Kp was reported in guinea pig ileum whole segment2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID79480Apparent pA2 value of compound at 100 nM concentration of mepyramine in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID87210Relative potency was recorded in Endothelium-Denuded guinea pig aortic segment(pre contracted with PGF-2 alpha); value ranges from 296 to 569, significantly more potent than histamine2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86271Maximum response (E max) against Histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID87390The compound was evaluated for intrinsic activity i.e. maximum histamine controls relative to contraction evoked by 10 uM PGF2-alpha in in relaxed rat aortic rings2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID5600Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 2A receptor of rat2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86435Intrinsic activity was reported in guinea pig ileum whole segment; mean significantly different from 1002000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86430Intrinsic activity was reported in endothelium-denuded guinea pig aortic segment2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86922Effective concentration against histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID86272concentration of mepyramine was determined2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87071Equilibrium dissociation constant (pKp) against histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID87544Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,6192000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87546Relative potency was recorded in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619; value ranges from 1854 to 43052000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87080Relative potency in guinea pig ileum whole segment; value ranges from 308 to 3822000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86578The compound was evaluated for intrinsic activity i.e. maximum histamine controls relative to contraction evoked by 10 uM PGF2-alpha in Endothelium-Denuded guinea pig aortic segment(pre contracted with PGF-2 alpha)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86923Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID28748Mepyramine concentration required to antagonise histaprodifens compound induced effects in guinea pig or rat assays2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86761Relative potency against Histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID5965Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 3 receptor of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86758Maximum response (E max) against Histamine H1 receptor in rat aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID86898Antagonism of guinea pig ileum contraction at 100 nM mepyramine2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87539Maximum response (E max) against Histamine H1 receptor in guinea pig ileum2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID87389Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID35610Compound was evaluated for its antagonist affinity towards Alpha-1D adrenergic receptor of rat2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86285Compound was evaluated for its antagonist affinity towards Histamine H3 receptor of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86267Antagonist effects was studied on contraction of guinea-pig ileum preparation.2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87538Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID42212Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID88149Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87392The compound was evaluated for intrinsic activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,6192000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID87543Effective concentration against histamine H1 receptor in rat aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID4489Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID6248Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 4 receptor of rat2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID86576Relative potency against Histamine H1 receptor in rat aorta2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
AID28753concentration; value ranges from 3 to 302000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1346037Human H1 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (5.56)18.2507
2000's7 (38.89)29.6817
2010's5 (27.78)24.3611
2020's5 (27.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.95

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 Index11.95 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.89 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]