aclidinium bromide: a long-acting, inhaled antimuscarinic; in phase I trial 8/2008 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
aclidinium bromide : A quaternary ammonium salt that is the bromide salt of aclidinium. A muscarinic acetylcholine M3 receptor antagonist, for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD). [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]
| ID Source | ID |
|---|---|
| PubMed CID | 11519741 |
| CHEBI ID | 65344 |
| SCHEMBL ID | 72694 |
| MeSH ID | M0538292 |
| Synonym |
|---|
| HY-14144 |
| aclidinium (bromide) |
| krp-ab1102 |
| aclidinium bromide |
| las-w-330 |
| bretaris |
| eklira |
| las-34273 |
| eklira genuair (tn) |
| tudorza pressair (tn) |
| D08837 |
| aclidinium bromide (jan/usan/inn) |
| 320345-99-1 |
| las-34273 micronized |
| las 34273 |
| las w-330 |
| genuair |
| chebi:65344 , |
| las 34273 micronized |
| (3r)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide |
| aclidinium bromide [usan:inn] |
| unii-uqw7uf9n91 |
| uqw7uf9n91 , |
| tudorza pressair |
| las34273 |
| 1-azoniabicyclo(2.2.2)octane, 3-((hydroxydi-2-thienylacetyl)oxy)-1-(3-phenoxypropyl)-, bromide, (3r)- |
| (3r)-3-((hydroxydi(thiophen-2-yl)acetyl)oxy)-1-(3-phenoxypropyl)-1-azoniabicyclo(2.2.2)octane bromide |
| S4031 |
| AKOS016010522 |
| CS-0896 |
| (3r)-3-[2-hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide |
| 1-azoniabicyclo(2.2.2)octane, 3-((2-hydroxy-2,2-di-2-thienylacetyl)oxy)-1-(3-phenoxypropyl)-, bromide (1:1), (3r)- |
| aclidinium bromide [mart.] |
| duaklir pressair component aclidinium bromide |
| aclidinium bromide [usan] |
| aclidinium bromide [inn] |
| aclidinium bromide [vandf] |
| (3r)-3-((2-hydroxy-2,2-di-2-thienylacetyl)oxy)-1-(3-phenoxypropyl)-1-azoniabicyclo(2.2.2)octane bromide (1:1) |
| (3r)-3-{[hydroxydi(thiophen-2-yl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide |
| aclidinium bromide [jan] |
| aclidinium bromide [mi] |
| aclidinium bromide [orange book] |
| aclidinium bromide component of duaklir pressair |
| aclidinium bromide [who-dd] |
| SCHEMBL72694 |
| (3r)-3-((hydroxy(di-2-thienyl)acetyl)oxy)-1-(3-phenoxypropyl)-1-azoniabicyclo(2.2.2)octane bromide |
| XLAKJQPTOJHYDR-QTQXQZBYSA-M |
| 3(r)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide |
| (3r)-3-(2-hydroxy-2,2-di(thiophen-2-yl)acetoxy)-1-(3-phenoxypropyl)quinuclidin-1-ium bromide |
| AC-23963 |
| DTXSID30185854 , |
| las-w 330 |
| eklira genuair |
| (3r)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide |
| (r)-3-(2-hydroxy-2,2-di(thiophen-2-yl)acetoxy)-1-(3-phenoxypropyl)quinuclidin-1-ium bromide |
| J-018606 |
| SW219176-1 |
| Q27888207 |
| BS-16987 |
| HMS3885C20 |
| mfcd22683690 |
| CCG-270072 |
| [(3r)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-3-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate;bromide |
| D81774 |
| [(8r)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-8-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate bromide |
| r03bb05 |
| (3r)-3-(2-hydroxy(di-2-thienyl)acetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo(2.2.2)octane bromide |
| (3r)-3-(2-hydroxy-2,2-di(thiophen-2-yl)acetyloxy)-1-(3-phenyloxypropyl)-1-azoniabicyclo(2.2.2)octane bromide |
| aclidinium bromide (mart.) |
| bromure d'aclidinium |
| bromuro de aclidinio |
| dtxcid70108345 |
| aclidinii bromidum |
Aclidinium bromide is a new muscarinic antagonist that has been developed to relieve symptoms in patients with COPD. When administered at the FDA-approved dose, it safely produces clinically and statistically significant bronchodilation.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with aclidinium bromide significantly increased cell apoptosis rate, accompanied by the expression of anti-apoptotic protein Bcl-2 decreased, the expression of pro-apoptotic protein Active caspase-3 and Bax significantly increased in U2 OS cells treated with aclidinium bromide." | ( Aclidinium bromide inhibits proliferation of osteosarcoma cells through regulation of PI3K/Akt pathway. Ji, XF; Li, ZZ; Wang, YL; Xing, YL; Yu, YH, 2019) | 2.3 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " This study assessed the effect of aclidinium bromide combined with formoterol on COPD lung (n=20) and non-COPD lung (n=10) derived epithelial cells stimulated with TGF-β1+carbachol on: (i) the generation of mesenchymal cells in relation to epithelial cells, (II) extracellular matrix (ECM) deposition, and (iii) the interaction of ECM on the generation of epithelial and mesenchymal cells." | ( Aclidinium bromide combined with formoterol inhibits remodeling parameters in lung epithelial cells through cAMP. Costa, L; Dekan, G; Lambers, C; Lardinois, D; Roth, M; Schuller, E; Ying, Q; Zhong, J, 2015) | 2.14 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These data suggest a low systemic bioavailability and favorable safety profile for aclidinium bromide with repeated dosing for COPD." | ( Safety and pharmacokinetics of multiple doses of aclidinium bromide, a novel long-acting muscarinic antagonist for the treatment of chronic obstructive pulmonary disease, in healthy participants. de Miquel, G; Gurniak, M; Jansat, JM; Lamarca, R; Miletzki, B; Schrödter, A, 2009) | 0.83 |
| " This 2-part, phase I study evaluated the safety and tolerability of single ascending intravenous (IV) doses of aclidinium to determine its maximum tolerated dose (MTD; part I) and its absolute bioavailability (part II)." | ( Safety and tolerability of aclidinium administered intravenously and absolute bioavailability of inhaled aclidinium in healthy male participants. Caracta, C; Flach, S; Gil, EG; Jansat, JM; Ortiz, S, 2012) | 0.38 |
| " Pharmacological and preclinical studies demonstrated the low systemic bioavailability of aclidinium and the low propensity to induce cardiac arrhythmias." | ( Aclidinium bromide twice daily for the treatment of chronic obstructive pulmonary disease: a review. Jones, P, 2013) | 1.83 |
| " Preclinical and pharmacological studies demonstrating low systemic bioavailability and a low propensity to induce cardiac arrhythmias were translated into a favorable tolerability profile in the clinical trial program - the adverse event profile of aclidinium was similar to placebo, with a low incidence of anticholinergic and cardiac adverse events." | ( Clinical potential of aclidinium bromide in chronic obstructive pulmonary disease. Jones, PW, 2015) | 0.73 |
| " There were no major differences in relative bioavailability between the combination and monotherapies: the aclidinium Cmax and AUC0-t were 26% and 3% higher, respectively, with aclidinium/formoterol FDC compared with aclidinium alone, and 18% and 11% higher, respectively, compared with formoterol alone." | ( Pharmacokinetics of aclidinium bromide/formoterol fumarate fixed-dose combination compared with individual components: A phase 1, open-label, single-dose study. Aubets, J; Fuhr, R; Leselbaum, A, 2016) | 0.76 |
| " Moreover, the elevated plasma clearance of aclidinium has been related to low systemic bioavailability and low incidence of anticholinergic adverse events, whereas the reduced residence time at M2 receptors provides good cardiovascular safety." | ( Effects of aclidinium on determinants of COPD severity: symptoms and quality of life. Braido, F; Contoli, M; Corsico, A; Di Marco, F; Santus, P; Scichilone, N; Solidoro, P, 2016) | 0.43 |
This study was conducted to evaluate the pharmacokinetic (PK) parameters, safety, and tolerability of aclidinium bromide and its metabolites in patients with normal and impaired renal function. The aim was to determine whether dosing adjustments are required when renal dysfunction is present.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Discussions with the FDA concluded that more trials are needed to assess selected dosing regimens, including higher and/or more frequent doses." | ( Aclidinium bromide, a novel long-acting muscarinic M3 antagonist for the treatment of COPD. Cazzola, M, 2009) | 1.8 |
| " These data suggest a low systemic bioavailability and favorable safety profile for aclidinium bromide with repeated dosing for COPD." | ( Safety and pharmacokinetics of multiple doses of aclidinium bromide, a novel long-acting muscarinic antagonist for the treatment of chronic obstructive pulmonary disease, in healthy participants. de Miquel, G; Gurniak, M; Jansat, JM; Lamarca, R; Miletzki, B; Schrödter, A, 2009) | 0.83 |
| "This study was conducted to evaluate the pharmacokinetic (PK) parameters, safety, and tolerability of aclidinium bromide and its metabolites in patients with normal and impaired renal function to determine whether dosing adjustments are required when renal dysfunction is present." | ( Pharmacokinetics and safety of aclidinium bromide, a muscarinic antagonist, in adults with normal or impaired renal function: A phase I, open-label, single-dose clinical trial. Gil, EG; Jansat, JM; Ortiz, S; Pascual, S; Schmid, K, 2010) | 0.86 |
| " Blood and urine samples were obtained before dosing and at various time points up to 48 hours after dosing to analyze the PK parameters of aclidinium bromide and its metabolites." | ( Pharmacokinetics and safety of aclidinium bromide, a muscarinic antagonist, in adults with normal or impaired renal function: A phase I, open-label, single-dose clinical trial. Gil, EG; Jansat, JM; Ortiz, S; Pascual, S; Schmid, K, 2010) | 0.85 |
| " Aclidinium Cmax was observed in plasma by 5 minutes after dosing (ie, median Tmax) and did not differ significantly among the renal function groups." | ( Pharmacokinetics and safety of aclidinium bromide, a muscarinic antagonist, in adults with normal or impaired renal function: A phase I, open-label, single-dose clinical trial. Gil, EG; Jansat, JM; Ortiz, S; Pascual, S; Schmid, K, 2010) | 0.65 |
| " PK parameters on Day 7 following BID dosing of aclidinium showed that steady state was achieved for aclidinium and its metabolites." | ( Safety and pharmacokinetics of multiple doses of aclidinium bromide administered twice daily in healthy volunteers. Caracta, CF; Dilzer, S; Garcia Gil, E; Jansat, JM; Lasseter, K; Ortiz, S, 2012) | 0.63 |
| " This study also confirmed the use of an aclidinium BID dosing regimen and established aclidinium 200 μg and 400 μg as suitable doses for further investigation in Phase III trials." | ( A randomised, placebo- and active-controlled dose-finding study of aclidinium bromide administered twice a day in COPD patients. Caracta, C; Garcia Gil, E; Jarreta, D; Kirsten, A; Magnussen, H; Mindt, S; Seoane, B; Singh, D, 2012) | 0.62 |
| " Treatment with the approved dosage of aclidinium (400 μg twice daily) statistically significantly improved bronchodilation, disease-specific health status, dyspnoea, night-time COPD symptoms and use of rescue medication compared with placebo in pivotal studies of 12 (ACCORD COPD I) or 24 (ATTAIN) weeks duration in patients with moderate to severe COPD." | ( Aclidinium: in chronic obstructive pulmonary disease. Frampton, JE, 2012) | 0.38 |
| " Twice-daily dosing of aclidinium leads to clinically important improvements in forced expiratory volume in 1 second, health status, use of rescue medication, day-time dyspnoea and exercise tolerance." | ( [Aclidinium bromide improves the lung function and reduces dyspnoea in patients with COPD]. Ulrik, CS, 2014) | 1.31 |
| " Measurements of IOS, spirometry, 6-min walk test, St George's Respiratory Questionnaire (SGRQ) and Baseline/Transition Dyspnoea Index (TDI) were made at baseline and after chronic dosing at trough (12 h for ACL and 24 h for TIO), in addition to domiciliary diurnal spirometry." | ( Effects of Adding Tiotropium or Aclidinium as Triple Therapy Using Impulse Oscillometry in COPD. Lipworth, BJ; Manoharan, A; Morrison, AE, 2016) | 0.43 |
| " The total dosage employed for aclidinium and tiotropium was 4 mg and 200 μg, respectively." | ( Downregulation of the cough reflex by aclidinium and tiotropium in awake and anesthetized rabbits. Bongianni, F; Cinelli, E; Iovino, L; Mutolo, D; Pantaleo, T, 2016) | 0.43 |
| " Therapeutic adherence is known to be a multifactorial phenomenon that is frequently affected by other aspects than dosing frequency, including the technical features and ease of use of the inhalers." | ( Is aclidinium alone or combined with a LABA a rational choice for symptomatic COPD patients? Blasi, F; Canonica, GW; Miravitlles, M, 2017) | 0.46 |
| " Aclidinium/formoterol fixed combination differs from other dual bronchodilators by twice-daily dosing regimen, good safety profile and a specific delivery system." | ( New opportunities of dual bronchodilation therapy for patients with chronic obstructive pulmonary disease. Avdeev, SN; Trushenko, NV, 2019) | 0.51 |
| Role | Description |
|---|---|
| muscarinic antagonist | A drug that binds to but does not activate muscarinic cholinergic receptors, thereby blocking the actions of endogenous acetylcholine or exogenous agonists. |
| bronchodilator agent | An agent that causes an increase in the expansion of a bronchus or bronchial tubes. |
| [role 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] | |
| Class | Description |
|---|---|
| quaternary ammonium salt | Derivatives of ammonium compounds, (NH4(+))Y(-), in which all four of the hydrogens bonded to nitrogen have been replaced with univalent (usually organyl) groups. |
| organic bromide salt | |
| [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 | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Testosterone 17-beta-dehydrogenase 3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0001 | 0.0001 | 0.0015 | 0.0040 | AID1054736 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0000 | 1.2326 | 7.7930 | AID430617; AID539981; AID631742 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.0003 | 0.0000 | 0.6902 | 10.0000 | AID1591564; AID430623 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 (µMol) | 0.0002 | 0.0000 | 1.1546 | 7.5858 | AID539982 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 (µMol) | 0.0002 | 0.0001 | 0.9917 | 8.0000 | AID539983 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0000 | 1.4039 | 10.0000 | AID430616; AID539980 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 0.0001 | 0.0000 | 0.5972 | 9.1201 | AID430624 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0001 | 1.0104 | 9.9280 | AID1054736; AID430618; AID539979; AID631741 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.0003 | 0.0000 | 0.5405 | 7.7600 | AID1591563; AID430622 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID539981 | Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | The discovery of new spirocyclic muscarinic M3 antagonists. |
| AID430621 | Inhibition of acetylcholine-induced bronchoconstriction in Dunkin-Hartley guinea pig assessed as time taken to recover 50% of maximum inhibitory effect at 3 mg/mL administered as nebulized solution | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1591564 | Displacement of [3H]NMS from human M2R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID539979 | Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | The discovery of new spirocyclic muscarinic M3 antagonists. |
| AID1224077 | Effect on CCh-induced salivation in Sprague-Dawley rat after 24 hrs | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists. |
| AID631745 | Stability of the compound in human plasma | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | The discovery of AZD9164, a novel muscarinic M3 antagonist. |
| AID1224076 | Ratio of ID50 for effect on CCh-induced salivation in Sprague-Dawley rat to ID50 for inhibition of CCh-induced bronchoconstriction Sprague-Dawley rat | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists. |
| AID430624 | Binding affinity to muscarinic M1 receptor | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430612 | Chemical stability assessed as half life at pH 7.4 by UV-HPLC analysis | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430617 | Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHOK1 cells by microplate scintillation counting | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430614 | Metabolic stability in human plasma assessed as compound disappearance at pH 7.4 up to 15 mins by ultra-performance liquid chromatography | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1591576 | Bronchodilatory activity in tracheotomized ICR mouse at 5 ug/kg administered intratracheally measured after 72 hrs | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID430618 | Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430615 | Metabolic stability in human plasma assessed as elimination half life at pH 7.4 | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430611 | Metabolic stability in human plasma assessed as compound disappearance at pH 7.4 up to 60 mins by ultra-performance liquid chromatography | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID539983 | Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | The discovery of new spirocyclic muscarinic M3 antagonists. |
| AID430616 | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHOK1 cells by microplate scintillation counting | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430628 | Toxicity in Swiss mouse assessed as occurrence of mydriasis at 30 mg/kg, ip up to 24 hrs | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1591574 | Bronchodilatory activity in tracheotomized ICR mouse at 5 ug/kg administered intratracheally measured after 48 hrs | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID430613 | Metabolic stability in human plasma assessed as compound disappearance at pH 7.4 up to 5 mins by ultra-performance liquid chromatography | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID430625 | Inhibition of acetylcholine-induced bronchoconstriction in Dunkin-Hartley guinea pig administered as nebulized solution | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1054735 | Plasma protein binding in human | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD. |
| AID1054737 | Intrinsic clearance in human liver microsomes | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD. |
| AID430626 | Inhibition of acetylcholine-induced bronchoconstriction in Dunkin-Hartley guinea pig assessed as time taken to recover 50% of maximum inhibitory effect at 1 mg/mL administered as nebulized solution | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1591563 | Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID430629 | Toxicity in Swiss mouse assessed as neurobiological state and occurrence of xerostomia at 30 mg/kg, ip up to 24 hrs | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID1591578 | Bronchodilatory activity in tracheotomized ICR mouse at 5 ug/kg administered intratracheally measured after 96 hrs | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID1591569 | Bronchodilatory activity in tracheotomized ICR mouse assessed as suppression of methacholine-induced increase in airway resistance at 5 ug/kg administered intratracheally 1 hr before by methacholine challenge | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity. |
| AID1054736 | Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD. |
| AID539980 | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | The discovery of new spirocyclic muscarinic M3 antagonists. |
| AID631741 | Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | The discovery of AZD9164, a novel muscarinic M3 antagonist. |
| AID1224075 | Bronchodilatory effect in it dosed Sprague-Dawley rat assessed as inhibition of CCh-induced bronchoconstriction after 24 hrs | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists. |
| AID539982 | Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | The discovery of new spirocyclic muscarinic M3 antagonists. |
| AID631746 | Antagonist potency at M3 receptor in Dunkin Hartley guinea pig trachea assessed as inhibition of methacholine-induced airway smooth muscle contraction after 1 hr by organ-bath technique | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | The discovery of AZD9164, a novel muscarinic M3 antagonist. |
| AID430622 | Binding affinity to muscarinic M3 receptor | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID631742 | Displacement of [3H]NMS from recombinant human M2 receptor expressed in CHO-K1 cells after 16 hrs | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | The discovery of AZD9164, a novel muscarinic M3 antagonist. |
| AID430623 | Binding affinity to muscarinic M2 receptor | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace |
| AID631743 | Intrinsic clearance in human liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | The discovery of AZD9164, a novel muscarinic M3 antagonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 8 (5.93) | 29.6817 |
| 2010's | 119 (88.15) | 24.3611 |
| 2020's | 8 (5.93) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 strong demand-to-supply ratio for research on this compound.
| This Compound (45.22) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 46 (33.09%) | 5.53% |
| Reviews | 41 (29.50%) | 6.00% |
| Case Studies | 1 (0.72%) | 4.05% |
| Observational | 3 (2.16%) | 0.25% |
| Other | 48 (34.53%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||