Page last updated: 2024-11-12

histaprodifen

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Cross-References

ID SourceID
PubMed CID10447834
CHEMBL ID275507
SCHEMBL ID3019488
MeSH IDM0304784

Synonyms (10)

Synonym
bdbm22864
2-[2-(3,3-diphenylpropyl)-1h-imidazol-4-yl]ethan-1-amine
histaprodifen
CHEMBL275507
gtpl4026
2-[2-[3,3-di(phenyl)propyl]-3h-imidazol-4-yl]ethanamine
SCHEMBL3019488
2-[2-(3,3-diphenylpropyl)-1h-imidazol-4-yl]ethanamine
2-[2-(3,3-diphenylpropyl)-1h-imidazol-5-yl]ethanamine
Q27077985
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H1 receptorRattus norvegicus (Norway rat)IC50 (µMol)0.79430.00000.32271.2589AID87362
Histamine H1 receptorRattus norvegicus (Norway rat)Ki501,186,985,984.00000.00071.54406.5000AID87372
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)0.79430.00000.44365.1768AID87362
Histamine H1 receptorHomo sapiens (human)Ki501,186,985,984.00000.00000.511010.0000AID87372
Histamine H4 receptorHomo sapiens (human)Ki10.00000.00060.478710.0000AID1798265
[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)Kd1.99530.00000.02840.1060AID5965
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Kd45.70880.00000.53588.3176AID42212
5-hydroxytryptamine receptor 3BHomo sapiens (human)Kd1.99530.00000.01370.1060AID5965
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd6.45650.00012.62198.5114AID5600
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd45.70880.00012.29338.5114AID42212
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd3.54810.00020.89627.5858AID35610
5-hydroxytryptamine receptor 1BHomo sapiens (human)Kd14.12540.07944.10398.1283AID4489
Histamine H1 receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.15850.00260.53341.2020AID86921
Histamine H1 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.85110.15851.82554.4668AID87543
5-hydroxytryptamine receptor 3AHomo sapiens (human)Kd1.99530.00000.00980.1060AID5965
Histamine H2 receptorCavia porcellus (domestic guinea pig)Kd34.67370.01170.15720.9550AID88149
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd3.16230.02342.74218.5114AID6248
5-hydroxytryptamine receptor 3DHomo sapiens (human)Kd1.99530.00000.02840.1060AID5965
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kd2.81840.00090.92823.5481AID141205
5-hydroxytryptamine receptor 3CHomo sapiens (human)Kd1.99530.00000.02840.1060AID5965
[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)Concentration0.03000.03002.67675.0000AID86273
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

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)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo 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)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

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)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo 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)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

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)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo 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)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
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.
AID86268Antagonist effects was studied on contraction of guinea-pig ileum preparation; value ranges from 3 to 30; f means observed by Kaumann-Marano plot2000Journal 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.
AID86580The compound was evaluated for intrinsic activity i.e. maximum histamine controls relative to contraction evoked by 10 uM PGF2-alpha; termed: intrinsic activity2000Journal 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.
AID86433Intrinsic activity 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.
AID87387Maximum response (E max) 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.
AID86575Maximum 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.
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.
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.
AID87386Intrinsic activity of the histamine as reported 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.
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.
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.
AID87083Relative potency in guinea pig ileum whole segment; value ranges from 99 to 1242000Journal 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.
AID86269Concentration 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.
AID87540Maximum 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.
AID86579The compound was evaluated for intrinsic activity i.e. maximum histamine controls relative to contraction evoked by 10 uM PGF2-alpha2000Journal 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.
AID86763Relative potency determined 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.
AID28754concentration was determined; value ranges from 3 to 30.2000Journal 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.
AID87393maximum relaxation evoked by carbachol 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.
AID87212Relative potency was recorded in Endothelium-Denuded guinea pig aortic segment; value ranges from 81 to 1262000Journal 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.
AID87549Relative potency was recorded in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619; value ranges from 330 to 8472000Journal 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.
AID87536Relative 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.
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.
AID87372Inhibitory activity against human Histamine H1 receptor2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
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.
AID87362Inhibitory activity against human Histamine H1 receptor2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
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.
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.
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.
AID87227Intrinsic activity was determined2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
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.
AID79479Apparent pA2 value of compound at 10 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.
AID87074Negative logarithm of receptor dissociation constant Kp was reported guinea pig ileal 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.
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.
AID87381Compound was evaluated for mepyramine antagonism effects in rat 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.
AID86762Relative 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.
AID87217Relative potency was recorded in endothelium-denuded guinea pig aortic segment; value ranges from 105 to 126 at 10 uM2000Journal 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.
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.
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.
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.
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.
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.
AID86273concentration of mepyramine was determined; value ranges from 1 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.
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.
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.
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1346037Human H1 receptor (Histamine receptors)2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
[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's15 (83.33)29.6817
2010's2 (11.11)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: 23.53

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 Index23.53 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.53)

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]