Page last updated: 2024-12-06

besipirdine

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Description

Besipirdine is a novel, selective, and orally active inhibitor of the mitochondrial permeability transition pore (mPTP) that has shown promising therapeutic potential in preclinical models of neurodegenerative diseases. It is structurally distinct from cyclosporine A and its analogs, which are the only other known mPTP inhibitors. Besipirdine has been shown to protect against neuronal death in models of stroke, Alzheimer's disease, and Parkinson's disease, suggesting it may have broad neuroprotective effects. It is currently in clinical trials for the treatment of Alzheimer's disease.'

besipirdine: structure given in first source; a non-receptor-dependent cholinomimetic agent with noradrenergic activity with potential use for treating Alzheimer's disease [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60691
CHEMBL ID29835
SCHEMBL ID637011
MeSH IDM0201978

Synonyms (22)

Synonym
besipirdine
indol-1-yl-propyl-pyridin-4-yl-amine
bdbm50048580
indol-1-yl-propyl-pyridin-4-yl-amine(besipirdine)
CHEMBL29835 ,
n-propyl-n-pyridin-4-ylindol-1-amine
1-(propyl-4-pyridylamino)indole
95py16j933 ,
unii-95py16j933
119257-34-0
besipirdine [inn]
besipirdine [who-dd]
1h-indol-1-amine, n-propyl-n-4-pyridinyl-
besipirdine [mi]
SCHEMBL637011
DTXSID50152361
AKOS027326217
n-(n-propyl) -n-(4-pyridinyl) -1h-indol-1-amine
Q4896297
n-propyl-n-(pyridin-4-yl)-1h-indol-1-amine
HY-15376
CS-0006035

Research Excerpts

Overview

Besipirdine hydrochloride is a novel compound with cholinergic and adrenergic activity being investigated as a treatment for Alzheimer's disease.

ExcerptReferenceRelevance
"Besipirdine hydrochloride is a novel compound with cholinergic and adrenergic activity being investigated as a treatment for Alzheimer's disease (AD). "( A "bridging" (safety/tolerance) study of besipirdine hydrochloride in patients with Alzheimer's disease.
Cutler, NR; Hourani, J; Huff, FJ; Sramek, JJ; Stewart, JA; Viereck, C; Wardle, T, 1995
)
2
"1. Besipirdine (HP 749) is a compound undergoing clinical trials for efficacy in treating Alzheimer's disease. "( Effects of besipirdine at the voltage-dependent sodium channel.
Huger, FP; Kongsamut, S; Smith, CP; Tang, L, 1995
)
1.3

Actions

ExcerptReferenceRelevance
"Besipirdine displays potent adrenergic activity in a variety of pharmacological and behavioral tests. "( alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog.
Brooks, KM; Hubbard, JW; Laws-Ricker, L; Nordstrom, ST; Smith, CP; Vargas, HM; Zhou, L, 1997
)
1.99

Toxicity

ExcerptReferenceRelevance
" The most common adverse events were asymptomatic postural hypotension and asymptomatic bradycardia."( A "bridging" (safety/tolerance) study of besipirdine hydrochloride in patients with Alzheimer's disease.
Cutler, NR; Hourani, J; Huff, FJ; Sramek, JJ; Stewart, JA; Viereck, C; Wardle, T, 1995
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" The tmax was 2 to 4 hours after dosing, with nonlinear increases in Cmax and the AUC0-4th for HP 749."( The pharmacokinetics and cardiovascular pharmacodynamics of HP 749 (besipirdine HCl) and metabolite P86-7480 in the conscious monkey.
Dean, R; Dileo, EM; Griffiths, L; Hintze, TH; Hsu, RS; Hubbard, JW; Natarajan, C, 1995
)
0.53

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic studies in animals and humans showed that I was well absorbed and metabolized primarily to the N-despropyl metabolite (P7480, II) after oral administration."( Determination of HP 749, a potential therapeutic agent for Alzheimer's disease, in plasma by high-performance liquid chromatography.
Chesson, SM; DiLeo, EM; Effland, RC; Hsu, RS; Klein, JT, 1991
)
0.28

Dosage Studied

ExcerptRelevanceReference
" The results suggest a dose-response relationship, with greater efficacy after 3 months of treatment and longer persistence after treatment withdrawal for besipiridine 20 mg BID than for 5 mg BID."( Preliminary evaluation of besipirdine for the treatment of Alzheimer's disease. Besipirdine Study Group.
Huff, FJ, 1996
)
0.59
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (35)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tissue alpha-L-fucosidaseHomo sapiens (human)IC50 (µMol)0.25000.14000.23500.4100AID36800
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00300.77706.0000AID145671
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)2.16440.00052.773925.1700AID141456; AID141573; AID141667; AID141669; AID141675; AID141676
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)2.31330.00052.891925.1700AID141667; AID141669; AID141675; AID141676
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)2.31330.00052.747825.1700AID141667; AID141669; AID141675; AID141676
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00040.629810.0000AID4829
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)2.31330.00052.780225.1700AID141667; AID141669; AID141675; AID141676
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00030.30952.3000AID145671
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)2.31330.00053.314249.5000AID141667; AID141669; AID141675; AID141676
Neuronal acetylcholine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00300.03470.1000AID145671
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00030.32092.3000AID145671
Neuronal acetylcholine receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00200.02680.1000AID145671
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00300.88696.0000AID145671
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)20.00000.00040.908610.0000AID4829
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00021.874210.0000AID36732
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.29500.00031.09147.7625AID36799; AID36800; AID36928; AID36929; AID36930; AID36931
Neuronal acetylcholine receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00300.03470.1000AID145671
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00132.24956.9000AID217463
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.29500.00031.09147.7625AID36799; AID36800; AID36928; AID36929; AID36930; AID36931
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.29500.00031.06917.7625AID36799; AID36800; AID36928; AID36929; AID36930; AID36931
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00021.270410.0000AID36732
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00040.615610.0000AID4829
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.600310.0000AID144903; AID157451
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00020.52597.2000AID31960; AID32094
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00001.819410.0000AID36732
Neuronal acetylcholine receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00200.69046.0000AID145671
Neuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00240.03010.1000AID145671
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.630610.0000AID144903; AID157451
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00061.525710.0000AID144903; AID157451
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.747210.0000AID144903; AID157451
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00301.69437.0795AID145671
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.741110.0000AID144903; AID157451
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.741110.0000AID144903; AID157451
Neuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00300.03470.1000AID145671
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)20.00000.00071.741110.0000AID144903; AID157451
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
fucose metabolic processTissue alpha-L-fucosidaseHomo sapiens (human)
glycosaminoglycan catabolic processTissue alpha-L-fucosidaseHomo sapiens (human)
glycoside catabolic processTissue alpha-L-fucosidaseHomo sapiens (human)
glycolipid catabolic processTissue alpha-L-fucosidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
alpha-L-fucosidase activityTissue alpha-L-fucosidaseHomo sapiens (human)
protein bindingTissue alpha-L-fucosidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
extracellular regionTissue alpha-L-fucosidaseHomo sapiens (human)
cytoplasmTissue alpha-L-fucosidaseHomo sapiens (human)
azurophil granule lumenTissue alpha-L-fucosidaseHomo sapiens (human)
lysosomal lumenTissue alpha-L-fucosidaseHomo sapiens (human)
intracellular membrane-bounded organelleTissue alpha-L-fucosidaseHomo sapiens (human)
extracellular exosomeTissue alpha-L-fucosidaseHomo sapiens (human)
lysosomeTissue alpha-L-fucosidaseHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneNeuronal acetylcholine receptor subunit alpha-9Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneNeuronal acetylcholine receptor subunit alpha-10Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID197115Compound was tested for inhibition of [3H]5-HT against rat whole brain using in vitro biogenic amine uptake assay using rat brain synaptosomes.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID217926Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID61191Inhibitory activity against [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118332Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.16 mg/kg sc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118355Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration at a concentration of 0.16 mg/kg1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID142813Inhibitory activity against [3H]N-methyl-scopolamine binding to Muscarinic acetylcholine receptor M2 in rat cerebellum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID141456Compound was tested for inhibition of [3H]pirenzepine binding against Muscarinic acetylcholine receptor M1 from rat cortical membranes using in vitro cholinergic receptor binding assay.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID197117Inhibitory activity against [3H]5-HT uptake in rat whole brain1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID157451Inhibitory activity against [3H]TCP binding to Phencyclidine receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID151448Inhibitory activity against [3H]DHM binding to mu opioid receptor in rat whole brain1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID32095Inhibitory activity against Acetylcholinesterase in rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID145671Inhibitory activity against [3H]-NMCC binding to nicotinic receptors in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID4829Inhibitory activity against [3H]spiroperidol binding to 5-HT2 receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID141674Inhibitory activity against [3H]oxotremorine-M binding to muscarinic receptors in rat forebrain membrane1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID196772Inhibitory activity against [3H]dopamine uptake in rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID141675Inhibition of radioligand [3H]QNB binding (competitive inhibition) to muscarinic acetylcholine receptor in the rat forebrain in the absence of zinc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID141676Inhibition of radioligand [3H]QNB binding to muscarinic acetylcholine receptor in the rat forebrain in the presence of zinc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID148684Inhibitory activity against [3H]bremazocine binding to kappa opioid receptor in guinea pig cerebellum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID36732Compound was tested for inhibition of [3H]WB-4101 against Alpha-1 adrenergic receptor from rat whole brain membranes using in vitro adrenergic receptor binding assay.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID141667Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the absence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID3774Inhibitory activity against [3H]DPAT binding to 5-HT1A receptor in rat hippocampus1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID4681Inhibitory activity against [3H]5-HT binding to 5-HT1B receptor in rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118352Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration at a concentration of 0.02 mg/kg1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID36799Compound was tested for inhibition of [3H]clonidine against Alpha-2 adrenergic receptor from rat cortical membranes using in vitro adrenergic receptor binding assay.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID36931Inhibitory activity against [3H]yohimbine binding to Alpha-2 adrenergic receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID232627Ratio of inhibitory activity against [3H]quinuclidinyl benzilate (QNB) binding in the absence of Zn to in the presence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID141573Inhibitory activity against [3H]pirenzepine binding to muscarinic M1 receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID197116Inhibitory activity against [3H]norepinephrine (NE) uptake in rat whole brain1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID36929Inhibitory activity against [3H]-idazoxan binding to Alpha-2 adrenergic receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID32094Inhibitory activity against acetylcholinesterase in rat striatal preparation1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID36928Inhibitory activity against [3H]clonidine binding to Alpha-2 adrenergic receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID217463Inhibition of [3H]nitrendipine binding to [Ca2+] channel of rat heart1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118354Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration at a concentration of 0.08 mg/kg1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID114183Effective dose against administration in mice1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118329Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.04 mg/kg sc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID36800Compound was tested for inhibition of [3H]yohimbine against Alpha-2 adrenergic receptor from rat cortical membranes using in vitro adrenergic receptor binding assay.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID118351Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID36930Inhibitory activity against [3H]idazoxan binding to Alpha-2 adrenergic receptor in rat cortex, in the presence of GPP1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID196038Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID197114Compound was tested for inhibition of [3H]norepinephrine against rat whole brain using in vitro biogenic amine uptake assay using rat brain synaptosomes.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID64456Inhibitory activity against [3H]spiroperidol bingind to Dopamine receptor D2 in rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID36878Inhibitory activity against [3H]WB-4101 binding to Alpha-1 adrenergic receptor in rat whole brain membrane1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118358Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration at a concentration of 0.63 mg/kg1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID141669Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID144903Inhibitory activity against [3H]-CPP binding to NMDA receptor in rat cortex1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID217930Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release)2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID197418Inhibitory activity against [3H]norepinephrine (NE) uptake in rat hypothalamus1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID31960In vitro inhibition of Acetylcholinesterase from rat striatum1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID118339Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.63 mg/kg sc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118331Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.08 mg/kg sc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID118328Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.02 mg/kg sc1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID196413Compound was tested for inhibition of [3H]dopamine against rat striatum using in vitro biogenic amine uptake assay using rat brain synaptosomes.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID118353Antagonistic activity against scopolamine-induced behavioral deficits in mice by subcutaneous administration at a concentration of 0.04 mg/kg1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID112904Evaluated for the prevention of TBZ ptosis by intraperitoneal administration in mice1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
AID142814Inhibitory activity against [3H]N-methyl-scopolamine in rat Muscarinic acetylcholine receptor M2 cerebellum in the presence GPP(NH)P1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID112006Antagonistic activity against Scopolamine induced behavioral deficits in mice; 5/61996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's13 (86.67)18.2507
2000's1 (6.67)29.6817
2010's1 (6.67)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: 16.58

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 Index16.58 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (20.00%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (73.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]