Reaxys
PubChem
eMolecules
LabNetwork
Bioactivities (22)
SigmaAldrich
Reactions (0)
Substances (1)
Structure
Targets (5)
Citations (15)
N° of preparations All Preps | All Reactions
Structure/Compound Data Chemical Name: Amfonelic acid
no reactions.
Reaxys Registry Number: 6871759
Type of Substance: heterocyclic Molecular Formula: C18H16N2O3
Linear Structure Formula: C18H16N2O3
Molecular Weight: 308.337 InChI Key: WHHHJDGNBVQNAU-UHFFFAOYSA-N 1
Available Data
Target
N° of ref.
Druglikeness
Bioactivity
Identification Other Data (3)
Show Targets
15
Highest Clinical Phase: Marketed
Synthesize | Hide Details Find similar Chemical Names and Synonyms Amfonelic acid, amfonelic acid, oxaprozin Druglikeness Bioactivity In vitro: Efficacy (20) Quantitative Results pX
Parameter
7.35
IC50
Value (qual)
Value (quant)
Unit
45
nM
Action on Target
Target
Tissue/Organ
Cell
Bioassay
Sodium-dependent dopamine transporter [Rattus
corpus striatum
cells
Binding
Dose
Effect
Reference (expand all/collapse all) Brain research, 2003 , ...
Title/Abstract Full Text Show Details
norvegicus]:Wild Rao, Tadimeti S; Adams, Pamala B; Correa, Lucia D; Santori, Emily M; Sacaan, Aida I; Reid, Richard T; Suto, Carla M; Vernier, Jean Michel
Brain research, 2003 , vol. 981, # 1-2 p. 85 - 98 Title/Abstract Full Text Show Details
8.14
Ki
7.2
nM
Inhibitor
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
corpus striatum
Flux uptake
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
hypothalamus
Flux uptake
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
brain cortex
Flux uptake
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
corpus striatum
Binding
1.00000E-11 M
European Journal of Phar...
Title/Abstract Full Text Show Details
corpus striatum
Binding
1.00000E-11 M
European Journal of Phar...
Title/Abstract Full Text Show Details
brain
Binding
Maryanoff; McComsey; Gardocki; Shank; Costanzo; Nortey; Schneider; Setler
Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1433 - 1454 Title/Abstract Full Text View citing articles Show Details
7.39
Ki
41.1
nM
Inhibitor
sodium-dependent dopamine transporter [rattus norvegicus]:Wild
Maryanoff; McComsey; Gardocki; Shank; Costanzo; Nortey; Schneider; Setler
Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1433 - 1454 Title/Abstract Full Text View citing articles Show Details
6.06
Ki
879
nM
Inhibitor
Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild
Maryanoff; McComsey; Gardocki; Shank; Costanzo; Nortey; Schneider; Setler
Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1433 - 1454 Title/Abstract Full Text View citing articles Show Details
6.73
IC50
187
nM
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi
European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 195 - 203 Title/Abstract Full Text Show Details
nH
0.6
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi
European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 195 - 203 Title/Abstract Full Text Show Details
4.6
Ki
25.2
µM
Adenosine receptor A1 [Rattus norvegicus]:Wild
Nucleosides and Nucleoti...
Title/Abstract Full Text View citing articles Show Details
Siddiqi, Suhaib M.; Ji, Xiao-Duo; Melman, Neli; Olah, Mark E.; Jain, Rahul; Evans, Patricia; Glashofer, Marc; Padgett, William L.; Cohen, Louis A.; Daly, John W.; Stiles, Gary L.; Jacobson, Kenneth A. Nucleosides and Nucleotides, 1996 , vol. 15, # 1-3 p. 693 - 717 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
<=
10
%
Adenosine receptor A2a [Rattus norvegicus]:Wild
Binding
corpus striatum
0.000100000 M
Nucleosides and Nucleoti...
Title/Abstract Full Text View citing articles Show Details
Siddiqi, Suhaib M.; Ji, Xiao-Duo; Melman, Neli; Olah, Mark E.; Jain, Rahul; Evans, Patricia; Glashofer, Marc; Padgett, William L.; Cohen, Louis A.; Daly, John W.; Stiles, Gary L.; Jacobson, Kenneth A. Nucleosides and Nucleotides, 1996 , vol. 15, # 1-3 p. 693 - 717 Title/Abstract Full Text View citing articles Show Details
3.8
Ki
157
µM
Adenosine receptor A3 [Rattus norvegicus]:Wild
CHO cell line
Binding
Nucleosides and Nucleoti...
Title/Abstract Full Text View citing articles Show Details
Siddiqi, Suhaib M.; Ji, Xiao-Duo; Melman, Neli; Olah, Mark E.; Jain, Rahul; Evans, Patricia; Glashofer, Marc; Padgett, William L.; Cohen, Louis A.; Daly, John W.; Stiles, Gary L.; Jacobson, Kenneth A. Nucleosides and Nucleotides, 1996 , vol. 15, # 1-3 p. 693 - 717 Title/Abstract Full Text View citing articles Show Details
3.22
Kb
600
µM
Antagonist
Adenosine receptor A1 [Rattus norvegicus]:Wild
adipose tissue
Adenylate cyclase activity
Nucleosides and Nucleoti...
Title/Abstract Full Text View citing articles Show Details
Siddiqi, Suhaib M.; Ji, Xiao-Duo; Melman, Neli; Olah, Mark E.; Jain, Rahul; Evans, Patricia; Glashofer, Marc; Padgett, William L.; Cohen, Louis A.; Daly, John W.; Stiles, Gary L.; Jacobson, Kenneth A. Nucleosides and Nucleotides, 1996 , vol. 15, # 1-3 p. 693 - 717 Title/Abstract Full Text View citing articles Show Details
8
IC50
10.1
nM
Inhibitor
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
corpus striatum
Flux uptake
Journal of Neurochemistr...
Title/Abstract Full Text Show Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
corpus striatum
Binding
Journal of Neurochemistr...
Title/Abstract Full Text Show Details
telencephalon
Binding
The Journal of pharmacol...
Title/Abstract Full Text Show Details
Andersen
Journal of Neurochemistry, 1987 , vol. 48, # 6 p. 1887 - 1896 Title/Abstract Full Text Show Details
7.4
IC50
40
nM
Andersen
Journal of Neurochemistry, 1987 , vol. 48, # 6 p. 1887 - 1896 Title/Abstract Full Text Show Details
3.29
IC50
507
µM
Zaczek; Culp; Goldberg; Mccann; De Souza
The Journal of pharmacology and experimental therapeutics, 1991 , vol. 257, # 2 p. 820 - 829 Title/Abstract Full Text Show Details
7
IC50
<
0.1
µM
Inhibitor
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Radioligand (/ligand)
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild +
Patent: WO2002/64128 A...
Title/Abstract Full Text Show Details
NEUROSEARCH A/S
Patent: WO2002/64128 A1, 2002 ; Title/Abstract Full Text Show Details
1
Ki
>
10000
nM
brain
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild + sodium-dependent dopamine transporter [rattus norvegicus]:Wild Davids, Eugen; Zhang, Kehong; Kula, Nora S.; Tarazi, Frank I.; Baldessarini, Ross J.
Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 3 p. 1097 - 1102 Title/Abstract Full Text View citing articles Show Details
7.73
Ki
=
18.7
nM
Radioligand (/ligand)
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild +
brain
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild + sodium-dependent dopamine transporter [rattus norvegicus]:Wild Davids, Eugen; Zhang, Kehong; Kula, Nora S.; Tarazi, Frank I.; Baldessarini, Ross J.
Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 3 p. 1097 - 1102 Title/Abstract Full Text View citing articles Show Details
Activity
@
M. A. Davis Annual reports in medicinal chemistry, 1967 , vol. 3, p. 14 - 27 Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
6.8
IC50
=
160.08
nM
Inhibitor
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
neostriatum
inhibitory activity
Patent: US5413779 A, 1...
Title/Abstract Full Text Show Details
inhibitory activity
Patent: WO1992/2260 A1...
Title/Abstract Full Text Show Details
Research Triangle Institute; The United States of America represented by the Secretary of Health and Human Services
Patent: US5413779 A, 1995 ; Title/Abstract Full Text Show Details
6.8
IC50
=
160.08
nM
Inhibitor
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
neostriatum
KUHAR Michael J; CARROLL Frank Ivy; BOJA John W; LEWIN Antia H; ABRAHAM Philip
Patent: WO1992/2260 A1, 1992 ; Title/Abstract Full Text Show Details
Qualitative Information 1 of 1
Results
Prevention of the reduction of the striatal 5-hydroxytryptamine concentration (rat p.o.)
Citation
Waldmeier
Journal of Pharmacy and Pharmacology, 1985 , vol. 37, # 1 p. 58 - 60 Title/Abstract Full Text View citing articles Show Details
In vivo: Animal Model (2) Quantitative Results pX
Parameter Tmax
Value (qual)
Value (quant)
Unit
40
minute
Action on Target
Animal Model
Biological Species
Route of administration
Dose
Rattus norvegicus
intraperitoneal administration
0.100000 mmol/kg
intraperitoneal administration
0 mg/kg
Dosing regimen
Effect
Single
Reference (expand all/collapse all) European Journal of Phar...
Title/Abstract Full Text Show Details
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi
European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 195 - 203 Title/Abstract Full Text Show Details
ED50
1.25
mg/kg
Tirelli; Witkin
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 7 - 16 Title/Abstract Full Text View citing articles Show Details
Identification Other Data
Behavioural Symptoms
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details