Page last updated: 2024-12-11

proxyfan

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

Cross-References

ID SourceID
PubMed CID6421522
CHEMBL ID19173
CHEBI ID93359
SCHEMBL ID4072620
SCHEMBL ID15929504
MeSH IDM0376073

Synonyms (28)

Synonym
BRD-K77171813-050-01-4
gtpl1255
4-[3-(phenylmethoxy)propyl]-3h-imidazole
5-[3-(benzyloxy)propyl]-1h-imidazole
proxyfan
3-(1h-imidazol-4-yl)propylphenylmethyl ether
bdbm22915
NCGC00159580-01
proxifan
5-(3-(benzyloxy)propyl)-1h-imidazole
CHEMBL19173
5-(3-phenylmethoxypropyl)-1h-imidazole
177708-09-7
SCHEMBL4072620
SCHEMBL15929504
WNWALBVQAAIULR-UHFFFAOYSA-N
4-(3-benzyloxypropyl)-1h-imidazole
1h-imidazole, 5-[3-(phenylmethoxy)propyl]-
DTXSID00849491
5-[3-(phenylmethoxy)propyl]-1h-imidazole
CHEBI:93359
bdbm50472551
2f2s8pt5hn ,
Q7252902
1h-imidazole, 5-(3-(phenylmethoxy)propyl)-
5-(3-(phenylmethoxy)propyl)-1h-imidazole
1h-imidazole, 4-(3-(phenylmethoxy)propyl)-
AKOS040745313

Research Excerpts

Overview

Probablefan is a high-affinity histamine H3 receptor protean agonist. It can produce a spectrum of pharmacological effects including agonist, inverse agonist and antagonist.

ExcerptReferenceRelevance
"Proxyfan is a histamine H3 receptor protean agonist that can produce a spectrum of pharmacological effects including agonist, inverse agonist, and antagonist. "( Antidiabetic properties of the histamine H3 receptor protean agonist proxyfan.
Duan, C; Henry, MB; Hwa, JJ; Lachowicz, J; Patel, B; Sondey, C; Vassileva, G; Zheng, S, 2011
)
2.05
"Proxyfan is a high-affinity histamine H3 receptor protean agonist exhibiting the full spectrum of pharmacological activities, from full agonist to full inverse agonist depending on the competition between constitutively active and quiescent H3 receptors in a given tissue or brain region."( The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat.
Baldi, E; Blandina, P; Bucherelli, C; Cenni, G; Passani, MB; Schunack, W, 2005
)
1.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzyl etherA compound of formula PhCH2OR (R =/= H).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H4 receptorHomo sapiens (human)Ki0.05010.00060.478710.0000AID1798265; AID548981
Histamine H3 receptorRattus norvegicus (Norway rat)Ki0.00290.00010.29638.5110AID89562
Histamine H3 receptorHomo sapiens (human)Ki0.00770.00010.33998.5110AID1798266; AID409910; AID548987; 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)0.06310.00740.601610.0000AID548993
Histamine H3 receptorHomo sapiens (human)EC50 (µMol)0.00320.00000.09473.1623AID548991
[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 (25)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
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.
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.
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.
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.
AID89884Ratio of binding affinity of rat histamine H3 receptor to that of human histamine H3 receptor; 1:12001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
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.
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.
AID409912Antagonist activity at histamine H3 receptor in po dosed Swiss mouse cerebral cortex assessed as Ntau-methylhistamine level after 90 mins by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
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.
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.
AID409910Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in CHO-K1 cells2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
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.
AID89871PKi was measured by Histamine H3 receptor binding assay (N-alpha-MeHA) on 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.
AID408551Agonist activity at histamine H3 receptor in rat cortex2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
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.
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.
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.
AID1346088Mouse H3 receptor (Histamine receptors)2004Journal of neurochemistry, Sep, Volume: 90, Issue:6
Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
AID1346017Rat H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
AID1346017Rat H3 receptor (Histamine receptors)2001Biochemical and biophysical research communications, Jan-12, Volume: 280, Issue:1
The rat H3 receptor: gene organization and multiple isoforms.
AID1346107Human H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.55)18.2507
2000's15 (68.18)29.6817
2010's4 (18.18)24.3611
2020's2 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.13

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 Index21.13 (24.57)
Research Supply Index3.14 (2.92)
Research Growth Index4.97 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.13)

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%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]