Page last updated: 2024-12-07

iodoproxyfan

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

Description

iodoproxyfan: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132937
CHEMBL ID19010
SCHEMBL ID3089477
MeSH IDM0238162

Synonyms (18)

Synonym
(125i)iodoproxyfan
1h-imidazole, 4-(3-((4-iodophenyl)methoxy)propyl)-
3-(1h-imidazol-4-yl)propyl-(4-iodophenyl)methyl ether
152028-96-1
4-[3-[(4-iodophenyl)methoxy]propyl]-3h-imidazole
gtpl1253
chembl19010 ,
5-{3-[(4-iodophenyl)methoxy]propyl}-1h-imidazole
bdbm22916
PDSP2_000542
PDSP1_000544
iodoproxyfan
L010934
5-[3-[(4-iodophenyl)methoxy]propyl]-1h-imidazole
SCHEMBL3089477
DTXSID30164942
bdbm50472544
Q27078083

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
", led to an oral bioavailability ratio of 62%."( Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Elz, S; Ganellin, CR; Jouvet, M; Ligneau, X; Lin, J; Muir, JL; Schunack, W; Schwartz, J; Stark, H; Vanni-Mercier, G, 1998
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H4 receptorHomo sapiens (human)Ki0.01270.00060.478710.0000AID1798265; AID548981; AID632452
Histamine H3 receptorRattus norvegicus (Norway rat)Ki0.07100.00010.29638.5110AID89562
Histamine H3 receptorHomo sapiens (human)Ki0.01070.00010.33998.5110AID1798266; AID548987; AID632451; AID86458
[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)
Histamine H4 receptorHomo sapiens (human)EC50 (µMol)0.01260.00740.601610.0000AID548993
Histamine H3 receptorHomo sapiens (human)EC50 (µMol)0.00010.00000.09473.1623AID548991
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
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)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
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)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID548993Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID86644In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID548981Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma22010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID89877Agonistic activity against histamine H3 receptor; Partial agonist2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
AID548994Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay relative to histamine2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID86774Tested for inhibition of forskolin-stimulated adenylate cyclase in SK-N-MC neuroblastoma cells expressing the rat Histamine H3 receptor; Full agonist2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
AID86247Agonistic activity tested against histamine H1 receptor on guinea pig ileum1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID86635In vivo antagonistic activity was tested against histamine H3 receptor after oral administration to mouse1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID87701Agonistic activity tested against histamine H2 receptor on guinea pig atrium1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID89872Affinity for histamine H3 receptor in rat cerebral cortex.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.
AID86640Binding affinity towards Histamine H3 receptor on synaptosomes from rat cerebral cortex1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID89889Ratio of binding affinity of rat histamine H3 receptor to that of human histamine H3 receptor; 2:12001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID549000Selectivity ratio of EC50 for human histamine H3 receptor to EC50 for human histamine H4 receptor2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID89562Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID548987Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID86458Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID632452Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID548992Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay relative to histamine2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID86283Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
AID89713In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
AID548991Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Histamine H4 receptor agonists.
AID632451Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID1346107Human H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1346017Rat H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1798266H3R 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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (32.00)18.2507
2000's13 (52.00)29.6817
2010's4 (16.00)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: 11.07

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 Index11.07 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]