Compounds > bencycloquidium bromide
Page last updated: 2024-11-12

bencycloquidium bromide

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

Description

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

Cross-References

ID SourceID
PubMed CID11531643
CHEMBL ID4560341
MeSH IDM0508230

Synonyms (8)

Synonym
860804-18-8
bencycloquidium bromide
3-(2-cyclopentyl-2-hydroxy-2-phenylethoxy)-1-methylquinuclidin-1-ium bromide
CHEMBL4560341 ,
bdbm50528213
1-cyclopentyl-2-[(1-methyl-1-azoniabicyclo[2.2.2]octan-3-yl)oxy]-1-phenylethanol;bromide
1-azoniabicyclo[2.2.2]octane, 3-(2-cyclopentyl-2-hydroxy-2-phenylethoxy)-1-methyl-, bromide (1:1)
AKOS040747943

Research Excerpts

Overview

Bencycloquidium bromide is a novel inhaled anticholinergic bronchodilator with high selectivity for muscarinic M3 receptor. It is under development for the treatment of rhinorrhea in rhinitis.

ExcerptReferenceRelevance
"Bencycloquidium bromide (BCQB) is a novel inhaled anticholinergic bronchodilator with high selectivity for muscarinic M3 receptor. "( Safety, Tolerability and Pharmacokinetics of Bencycloquidium Bromide, a Novel Inhaled Anticholinergic Bronchodilator, in Healthy Subjects: Results from Phase I Studies.
Ding, L; Hu, C; Liang, M; Luo, Z; Miao, J; Pan, Y; Wang, Y, 2021)		2.32
"Bencycloquidium bromide (BCQB) is a novel selective muscarinic M1/M3 receptor antagonist with potent therapeutic effects on rhinitis and chronic obstructive pulmonary disease. "( In vitro metabolism of bencycloquidium bromide and its inhibitory effects on human P450 isoenzymes: implication of CYP2D6, CYP2C19 and CYP3A4/5.
Agbokponto, JE; Ding, L; Feng, H; Hu, L; Zhang, L, 2016)		2.19
"Bencycloquidium bromide (BCQB) is a novel, potent and selective muscarinic M1/M3 receptor antagonist under development for the treatment of rhinorrhea in rhinitis. "( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		2.08

Toxicity

ExcerptReferenceRelevance
" Safety and tolerability of BCQB were evaluated by monitoring adverse events (AEs), ECG recordings, vital signs and clinical laboratory parameters."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" There was no serious adverse event, death or withdrawal."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
"BCQB was safe and well tolerated in healthy Chinese subjects when administered intranasally with single and multiple doses across the doses studied."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" Adverse events were recorded in detail."( Bencycloquidium bromide nasal spray is effective and safe for persistent allergic rhinitis: a phase III, multicenter, randomized, double-blinded, placebo-controlled clinical trial.
Chen, J; Dong, P; Guo, M; He, G; He, J; Hu, G; Huang, Y; Jiang, Z; Lian, Z; Liang, J; Lin, C; Liu, S; Meng, J; Pan, Y; Tan, G; Xiao, H; Xiao, X; Xue, W; Zhang, Q; Zhang, X, 2020)		2
" The incidence of adverse reaction was similar between the two groups."( Bencycloquidium bromide nasal spray is effective and safe for persistent allergic rhinitis: a phase III, multicenter, randomized, double-blinded, placebo-controlled clinical trial.
Chen, J; Dong, P; Guo, M; He, G; He, J; Hu, G; Huang, Y; Jiang, Z; Lian, Z; Liang, J; Lin, C; Liu, S; Meng, J; Pan, Y; Tan, G; Xiao, H; Xiao, X; Xue, W; Zhang, Q; Zhang, X, 2020)		2
"90 μg BCQB per nostril four times daily is effective and safe in the treatment of rhinorrhea as well as sneezing, nasal congestion and itching for patients with PAR."( Bencycloquidium bromide nasal spray is effective and safe for persistent allergic rhinitis: a phase III, multicenter, randomized, double-blinded, placebo-controlled clinical trial.
Chen, J; Dong, P; Guo, M; He, G; He, J; Hu, G; Huang, Y; Jiang, Z; Lian, Z; Liang, J; Lin, C; Liu, S; Meng, J; Pan, Y; Tan, G; Xiao, H; Xiao, X; Xue, W; Zhang, Q; Zhang, X, 2020)		2

Pharmacokinetics

ExcerptReferenceRelevance
" However, no clinical pharmacokinetic data are available for BCQB in humans."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" The pharmacokinetic parameters for BCQB were calculated by software using non-compartmental methods."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" Blood samples were collected for pharmacokinetic analysis."( Study of pharmacokinetic interaction of paroxetine and roxithromycin on bencycloquidium bromide in healthy subjects.
Agbokponto, JE; Ding, L; Liang, M; Liu, R; Liu, Z; Luo, Z, 2015)		0.65
" Geometric mean Cmax were 187."( Study of pharmacokinetic interaction of paroxetine and roxithromycin on bencycloquidium bromide in healthy subjects.
Agbokponto, JE; Ding, L; Liang, M; Liu, R; Liu, Z; Luo, Z, 2015)		0.65
"This study consisted of single-ascending-dose (SAD), multiple-ascending-dose (MAD) tolerability study periods, and single- plus multiple-dose pharmacokinetic study periods."( Safety, Tolerability and Pharmacokinetics of Bencycloquidium Bromide, a Novel Inhaled Anticholinergic Bronchodilator, in Healthy Subjects: Results from Phase I Studies.
Ding, L; Hu, C; Liang, M; Luo, Z; Miao, J; Pan, Y; Wang, Y, 2021)		0.88
"The results of our study provided the initial safety, tolerability and pharmacokinetic profiles of BCQB inhalation, and could enable further clinical development in COPD patients."( Safety, Tolerability and Pharmacokinetics of Bencycloquidium Bromide, a Novel Inhaled Anticholinergic Bronchodilator, in Healthy Subjects: Results from Phase I Studies.
Ding, L; Hu, C; Liang, M; Luo, Z; Miao, J; Pan, Y; Wang, Y, 2021)		0.88

Dosage Studied

ExcerptRelevanceReference
"The clinical trial was comprised of the following four studies: (i) an open-label, single-dose escalation study to evaluate the safety and tolerability in healthy subjects after intranasal doses of BCQB ranging from 45 to 450 μg (total of six doses); (ii) an open-label, multiple-dose escalation study to assess the safety and tolerability in healthy subjects after intranasal administration with 120 and 150 μg doses of BCQB (360 and 450 μg/day) administered three times daily for 15 days; (iii) a randomized, open-label and parallel-group design to evaluate the single-dose pharmacokinetics of BCQB after intranasal dosing (45, 90, and 180 μg); and (iv) ten subjects received 120 μg of BCQB by intranasal administration, three times daily for 5 days with a final single dose on day 7 to assess its multiple-dose pharmacokinetics."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" During the multiple dosing, the steady state was achieved within 3 days of 120 μg three times daily dosing of BCQB."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
" A slight accumulation of BCQB following multiple dosing was observed."( Pharmacokinetics, safety and tolerability of Bencycloquidium bromide, a novel selective muscarinic M1/M3 receptor antagonist, after single and multiple intranasal doses in healthy chinese subjects: an open-label, single-center, first-in-human study.
Chen, X; Ding, L; Ou, N; Sun, L; Sun, W; Wang, Y; Yan, Z; Zhang, H; Zhou, W, 2012)		0.64
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.00620.00000.690210.0000AID1607601
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1607601Inhibition of M2 receptor (unknown origin)2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).
[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's0 (0.00)18.2507
2000's5 (27.78)29.6817
2010's10 (55.56)24.3611
2020's3 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.59

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 Index11.59 (24.57)
Research Supply Index3.14 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (22.22%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (72.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
histamine
[no description available]		2.1110aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0610ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
methacholine chloride
Methacholine Chloride: A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)		2.4720quaternary ammonium salt
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		8.511aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		2.1110
imd 0354
N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first source		3.3110benzamides
mcc-950
[no description available]		3.3110
batefenterol
batefenterol: a bronchodilator		3.3110
ConditionIndicatedRelationship StrengthStudiesTrials
Airflow Obstruction, Chronic
[description not available]		03.1210
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		03.1210
Allergic Rhinitis
[description not available]		04.331
Rhinorrhea
Excess nasal drainage.		07.610
Hay Fever
[description not available]		02.610
Rhinitis, Allergic, Seasonal
Allergic rhinitis that occurs at the same time every year. It is characterized by acute CONJUNCTIVITIS with lacrimation and ITCHING, and regarded as an allergic condition triggered by specific ALLERGENS.		02.610
Rhinitis, Allergic
An inflammation of the NASAL MUCOSA triggered by ALLERGENS.		04.331
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5220
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.4920
Pneumonia
Infection of the lung often accompanied by inflammation.		02.4920
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.7330
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.0610
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.0610
Airway Remodeling
The structural changes in the number, mass, size and/or composition of the airway tissues.		02.0610
Eosinophilia, Tropical
[description not available]		02.0610
Allergic Reaction
[description not available]		02.0610
Innate Inflammatory Response
[description not available]		02.0610
Eosinophilia
Abnormal increase of EOSINOPHILS in the blood, tissues or organs.		02.0610
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		02.0610
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		07.0610