imidafenacin: structure in first source
ID Source | ID |
---|---|
PubMed CID | 6433090 |
CHEMBL ID | 53366 |
CHEBI ID | 134720 |
SCHEMBL ID | 929680 |
MeSH ID | M0331494 |
Synonym |
---|
imidafenacin |
uritos (tn) |
D06273 |
staybla (tn) |
170105-16-5 |
imidafenacin (jan/inn) |
CHEBI:134720 |
uritos |
ono-8025 |
CHEMBL53366 |
krp-197 |
staybla |
L001601 |
4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide |
4-(2-methylimidazol-1-yl)-2,2-diphenylbutanamide |
NCGC00183110-01 |
4-(2-methyl-1h-imidazol-1-yl)-2,2-diphenylbutanamide |
imidafenacin [inn] |
xjr8y07ljo , |
ono 8025 |
krp 197 |
unii-xjr8y07ljo |
1h-imidazole-1-butanamide, 2-methyl-alpha,alpha-diphenyl- |
FT-0670290 |
AM84591 |
imidafenacin [mart.] |
imidafenacin [who-dd] |
imidafenacin [mi] |
imidafenacin [jan] |
S5385 |
CS-3681 |
SQKXYSGRELMAAU-UHFFFAOYSA-N |
SCHEMBL929680 |
imidafenacin hydrochloride, >=95% (hplc) |
HY-B0662 |
DB09262 |
J-521484 |
AKOS030526649 |
4-(2-methyl-1h-imidazol-1-yl)-2,2-diphenylbutanamide, aldrichcpr |
mfcd09833703 |
4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide hydrochloride |
2-methyl-|a,|a-diphenyl-1h-imidazole-1-butanamide hydrochloride |
Q6003989 |
AS-47648 |
krp-197;ono-8025 |
BCP10054 |
HMS3886C04 |
CCG-267694 |
NCGC00183110-02 |
EX-A4417 |
F14841 |
A882053 |
DTXSID00870104 |
Imidafenacin is a potent and selective antagonist of M. It may improve the urodynamic parameters of patients with SCI, and it possibly alleviates bladder complications.
Excerpt | Reference | Relevance |
---|---|---|
"Treatment with imidafenacin significantly improved OAB symptoms. " | ( Effect of imidafenacin on nocturia and sleep disorder in patients with overactive bladder. Fujisawa, M; Hou, K; Iuchi, H; Kakizaki, H; Kita, M; Kunieda, M; Kura, T; Matsumoto, S; Nakata, Y; Niibori, D; Numata, A; Osanai, H; Saga, Y; Taniguchi, A; Wada, N; Watanabe, M; Yamaguchi, S, 2012) | 1.13 |
The overall incidence of adverse events and the incidence of dry mouth were significantly higher in the imidafenacin group than in the mirabegron group. The most common adverse event was a dry mouth (40%)
This study was designed to update the population pharmacokinetic model and investigate the exposure-response (efficacy and safety) and concentration-QT relationships for imidafenacin. Pharmacokinetic parameters were estimated from measurements of the concentration of imidahfenacin in serum, the bladder, and the submaxillary gland.
Excerpt | Reference | Relevance |
---|---|---|
"The objectives of this study were to develop a population pharmacokinetic model of imidafenacin and to explore the factors that affect the pharmacokinetics of imidafenecin." | ( Population pharmacokinetic analysis of a novel muscarinic receptor antagonist, imidafenacin, in healthy volunteers and overactive bladder patients. Kitagawa, J; Konomi, T; Miyabe, H; Miyata, Y; Nakade, S; Nakayama, K; Ohno, T, 2008) | 0.8 |
" Pharmacokinetic parameters were estimated from measurements of the concentration of imidafenacin in serum, the bladder, and the submaxillary gland by liquid chromatography-mass spectrometry/mass spectrometry." | ( Selective binding of bladder muscarinic receptors in relation to the pharmacokinetics of a novel antimuscarinic agent, imidafenacin, to treat overactive bladder. Fukata, A; Ito, Y; Nakamura, M; Ogoda, M; Seki, M; Yamada, S, 2011) | 0.8 |
"This study was designed to update the population pharmacokinetic model and investigate the exposure-response (efficacy and safety) and concentration-QT relationships for imidafenacin, a synthetic orally active muscarinic receptor antagonist." | ( Population pharmacokinetics and exposure-response relationship of a muscarinic receptor antagonist, imidafenacin. Hasegawa, C; Miyabe, H; Nakade, S; Ogawa, M; Ohno, T; Ouchi, T; Shibakawa, K, 2013) | 0.8 |
Imidafenacin is rapidly and well absorbed (at least 65% of dose recovered in urine) after oral administration. Circulates in human plasma as the unchanged form, its glucuronide, and other metabolites. Then excreted in urine and feces as the oxidized metabolites of 2-methylimidazole moiety.
The objective of this study was to formulate once-a-day extended-release (ER) pellet system of imidafenacin (IDN), a recently approved urinary antispasmodic agent.
Excerpt | Relevance | Reference |
---|---|---|
"To evaluate the efficacy, safety/tolerability, and dose-response relationship of imidafenacin in Japanese patients with overactive bladder." | ( A randomized, double-blind, placebo-controlled phase II dose-finding study of the novel anti-muscarinic agent imidafenacin in Japanese patients with overactive bladder. Homma, Y; Yamaguchi, O; Yamaguchi, T, 2008) | 0.78 |
"The objective of this study was to formulate once-a-day extended-release (ER) pellet system of imidafenacin (IDN), a recently approved urinary antispasmodic agent with twice-a-day dosing regimen." | ( Novel Extended-Release Multiple-Unit System of Imidafenacin Prepared by Fluid-Bed Coating Technique. Choi, YW; Goh, MS; Ho, MJ; Im, SH; Kang, MJ; Kim, CH; Lee, ES; Shin, TH, 2018) | 0.96 |
Class | Description |
---|---|
diarylmethane | Any compound containing two aryl groups connected by a single C atom. |
[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 (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Kb | 0.0041 | 0.0015 | 0.0594 | 0.4100 | AID142744; AID142745 |
Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Kb | 0.0041 | 0.0041 | 0.0063 | 0.0085 | AID142744 |
Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Kb | 0.0041 | 0.0041 | 0.0063 | 0.0085 | AID142744 |
Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Kb | 0.0041 | 0.0041 | 0.0063 | 0.0085 | AID142744 |
Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Kb | 0.0041 | 0.0041 | 0.0063 | 0.0085 | AID142744 |
Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Kb | 0.0041 | 0.0015 | 0.0054 | 0.0085 | AID142744 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
G protein-coupled acetylcholine receptor activity | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
arrestin family protein binding | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
G protein-coupled serotonin receptor activity | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID229681 | Selectivity ratio for Kb values at M1 and M3 receptors | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (1). |
AID140994 | Antimuscarinic activity against muscarinic acetylcholine M3-receptor in guinea pig ileum | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Design, synthesis and antimuscarinic activity of some imidazolium derivatives. |
AID229682 | Selectivity ratio for Kb values at M2 and M3 receptors | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (1). |
AID419509 | Volume of distribution at steady state in human at 0.1 mg/kg administered 15 mins infusion | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set. |
AID140996 | Antimuscarinic activity against M3 receptor of guinea pig ileum | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (2). |
AID142744 | Antimuscarinic activity against muscarinic acetylcholine M2-receptor in guinea pig atria | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Design, synthesis and antimuscarinic activity of some imidazolium derivatives. |
AID142610 | Antimuscarinic activity against muscarinic M1 receptor in rabbit vas deferens | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (1). |
AID419510 | Total clearance in human at 0.1 mg/kg administered 15 mins infusion | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set. |
AID142746 | Antimuscarinic activity against M2 receptor of guinea pig atrium | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (2). |
AID140995 | Antimuscarinic activity was evaluated against muscarinic M3 receptor in Guinea-Pig ileum | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (1). |
AID142745 | Antimuscarinic activity was evaluated against muscarinic M2 receptor in Guinea-Pig atria | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (1). |
AID232448 | Selectivity ratio between Kb values of M2-receptor (atria) and M3-receptor (ileum) | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Design, synthesis and antimuscarinic activity of some imidazolium derivatives. |
AID229680 | Selectivity ratio was calculated between Kb values at M2 and M3 muscarinic receptors | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | Novel imidazole derivatives with subtype-selective antimuscarinic activity (2). |
[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 | 4 (5.13) | 18.2507 |
2000's | 20 (25.64) | 29.6817 |
2010's | 50 (64.10) | 24.3611 |
2020's | 4 (5.13) | 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 (45.69) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 27 (34.62%) | 5.53% |
Reviews | 6 (7.69%) | 6.00% |
Case Studies | 1 (1.28%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 44 (56.41%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |