Page last updated: 2024-12-07

zamifenacin

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

Description

zamifenacin: zamifenacin is the (R)-isomer; RN given for (+-)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3086618
CHEMBL ID27507
CHEBI ID93417
SCHEMBL ID311829
MeSH IDM0257340

Synonyms (32)

Synonym
BRD-K80451230-051-01-8
zamifenacin
uk-76654-2 [as fumarate]
CHEMBL27507
NCGC00247932-01
(3r)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine
tox21_300210
dtxsid9047257 ,
dtxcid7027257
NCGC00254011-01
cas-127308-82-1
(r)-3-(diphenylmethoxy)-1-(3,4-(methylenedioxy)phenetyl)piperidene
127308-82-1
y88q418y7m ,
zamifenacin [inn]
unii-y88q418y7m
(r)-3-(diphenylmethoxy)-1-(3,4-(methylenedioxy)phenethyl)piperidine
piperidine, 1-(2-(1,3-benzodioxol-5-yl)ethyl)-3-(diphenylmethoxy)-, (r)-
SCHEMBL311829
AKOS022182209
zamifenacin [mart.]
uk-76654-2 free base
CHEBI:93417
(r)-3-(benzhydryloxy)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)piperidine
Q27165120
HY-123337
uk-76654
(+/-)-1-(2-(1,3-benzodioxol-5-yl)ethyl)-3-(diphenylmethoxy)piperidine
BCP28100
CS-0082527
MS-27221
piperidine, 1-[2-(1,3-benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)-, (3r)-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Because the catechol was generally less toxic than the O-methylated product, species that eliminate zamifenacin primarily as the catechol or its conjugate may be less affected by the potential hepatotoxicity of the methylated product."( In vitro toxicity of zamifenacin (UK-76,654) and metabolites in primary hepatocyte cultures.
Amacher, DE; Beaumont, K; Charuel, C; Comby, P; Fasulo, LM, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
" Following oral administration to animals, metabolic clearance resulted in decreased bioavailability due to first-pass metabolism in rat and mouse."( Pharmacokinetics and metabolism of zamifenacin in mouse, rat, dog and man.
Beaumont, KC; Causey, AG; Coates, PE; Smith, DA, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny 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 Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency35.57420.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency61.13060.006038.004119,952.5996AID1159521; AID1159523
GLI family zinc finger 3Homo sapiens (human)Potency54.48270.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency57.78560.000221.22318,912.5098AID743035; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency48.55770.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency9.68850.001022.650876.6163AID1224838
progesterone receptorHomo sapiens (human)Potency27.30600.000417.946075.1148AID1346795
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency62.32630.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.05020.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency55.63820.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency21.87240.375827.485161.6524AID743217
estrogen nuclear receptor alphaHomo sapiens (human)Potency69.58240.000229.305416,493.5996AID1259244; AID1259248; AID743075; AID743079; AID743080; AID743091
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency48.96620.001019.414170.9645AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency8.84510.023723.228263.5986AID743222; AID743241
aryl hydrocarbon receptorHomo sapiens (human)Potency38.08630.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency68.58960.001723.839378.1014AID743083
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency13.57200.057821.109761.2679AID1159526; AID1159528
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency34.60440.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency34.66540.042027.378961.6448AID743210
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency61.13060.000627.21521,122.0200AID743202; AID743219
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency68.58960.001557.789015,848.9004AID1259244
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency68.58960.001551.739315,848.9004AID1259244
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (75.00)18.2507
2000's3 (18.75)29.6817
2010's0 (0.00)24.3611
2020's1 (6.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (25.00%)5.53%
Reviews1 (6.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (68.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]