Query Query
N
Results
Date
1 substances in Reaxys
2018-04-03 15h:10m:33s (UTC)
N
1. Query OH
O
O
Search as: As drawn
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Reaxys ID 6871759 View in Reaxys
N
1/1 Chemical Name: Amfonelic acid; amfonelic acid; oxaprozin Linear Structure Formula: C18H16N2O3 Molecular Formula: C18H16N2O3 Molecular Weight: 308.337 Type of Substance: heterocyclic InChI Key: WHHHJDGNBVQNAU-UHFFFAOYSA-N Note:
N OH O
O
Substance Label (3) Label References 61
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; vol. 15; nb. 1-3; (1996); p. 693 - 717, View in Reaxys
Negwer 6240
Nakachi, Noriyuki; Kiuchi, Yuji; Inagaki, Masahiro; Inazu, Masato; Yamazaki, Yukako; Oguchi, Katsuji; European Journal of Pharmacology; vol. 281; nb. 2; (1995); p. 195 - 204, View in Reaxys
AFA
Waldmeier; Journal of Pharmacy and Pharmacology; vol. 37; nb. 1; (1985); p. 58 - 60, View in Reaxys
Druglikeness (1) 1 of 1
LogP
3.798
H Bond Donors
1
H Bond Acceptors
5
Rotatable Bonds
4
TPSA
70.5
Lipinski Number
4
Veber Number
2
Highest Clinical Phase (1) Highest Clinical Phase Marketed Use (3) Use Pattern
References
dopamine reuptake inhibitor
Patent; DESCARTES THERAPEUTICS, INC.; WO2005/107467; (2005); (A2) English, View in Reaxys
Dopaminergic agent for composition for treating pain
Patent; DESCARTES THERAPEUTICS, INC.; WO2005/107467; (2005); (A2) English, View in Reaxys
Dopaminergic Patent; DESCARTES THERAPEUTICS, INC.; WO2005/107467; (2005); (A2) English, View in Reaxys agent for composition for treating nociception Medchem (22) 1 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
amfonelic acid
Measurement Parameter
IC50
Unit
nM
Quantitative value
45
Deviation
5
Measurement pX
7.35
Concomitants: Compound RN
578614
Concomitants: Compound name
[3H]-GBR 12935
Concomitants: Compound role
RAD
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
corpus striatum
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
6871759View in Reaxys
Substance Name
amfonelic acid
Measurement Parameter
Ki
Unit
nM
Quantitative value
7.2
Measurement pX
8.14
Concomitants: Compound RN
11305494; 1072822
Concomitants: Compound name
[3H]-Dopamine; Dopamine
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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4 of 22
Concomitants: Compound role
MAR; SUB
Target Name
sodium-dependent dopamine transporter [rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
sodium-dependent dopamine transporter [rattus norvegicus]
Target Mutant/Chimera Details
sodium-dependent dopamine transporter [rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
hypothalamus
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
6871759View in Reaxys
Substance Name
amfonelic acid
Measurement Parameter
Ki
Unit
nM
Quantitative value
41.1
Measurement pX
7.39
Concomitants: Compound RN
2804840; 2804840
Concomitants: Compound name
Norepinephrine; [3H]-Norepinephrine
Concomitants: Compound role
SUB; MAR
Target Name
Sodium-dependent serotonin transporter [Rattus norvegicus]
Target Synonyms
5ht transporter; 5htt; slc6a4; sodium-dependent serotonin transporter; solute carrier family 6 member 4
Target Uniprot ID
p31652
Target, Subunit, Species
Sodium-dependent serotonin transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
Wistar rat
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Organs/Tissues
brain cortex
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
6871759View in Reaxys
Substance Name
amfonelic acid
Measurement Parameter
Ki
Unit
nM
Quantitative value
879
Measurement pX
6.06
Concomitants: Compound RN
8144579; 143524
Concomitants: Compound name
[3H]-5-HT; 5-HT
Concomitants: Compound role
MAR; SUB
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
6871759View in Reaxys
Substance Name
43254
Qualitative Results
Prevention of the reduction of the striatal 5-hydroxytryptamine concentration (rat p.o.)
Measurement Parameter
Qualitative
Waldmeier; Journal of Pharmacy and Pharmacology; vol. 37; nb. 1; (1985); p. 58 - 60, View in Reaxys 6 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Substance Dose
1.00000E-11 M
Measurement Parameter
IC50
Unit
nM
Quantitative value
187
Deviation
13
Measurement pX
6.73
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Concomitants: Compound RN
578614; 5696321
Concomitants: Compound name
[3H]-GBR 12935; Vanoxerine dihydrochloride
Concomitants: Compound role
RAD; NSB
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi; European Journal of Pharmacology; vol. 281; nb. 2; (1995); p. 195 203, View in Reaxys 7 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Substance Dose
1.00000E-11 M
Measurement Parameter
nH
Quantitative value
0.6
Concomitants: Compound RN
578614; 5696321
Concomitants: Compound name
[3H]-GBR 12935; Vanoxerine dihydrochloride
Concomitants: Compound role
RAD; NSB
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi; European Journal of Pharmacology; vol. 281; nb. 2; (1995); p. 195 203, View in Reaxys 8 of 22
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Brain biochemistry : Dopamine (DA, DOPAC, DOPA, HVA)
Biological Species/NCBI ID
Rattus norvegicus
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Substance Dose
0.100000 mmol/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
Tmax
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Unit
minute
Measurement Object
Dopamine
Quantitative value
40
Concomitants: Compound name
Ringer's buffer
Concomitants: Compound role
OCV
Nakachi; Kiuchi; Inagaki; Inazu; Yamazaki; Oguchi; European Journal of Pharmacology; vol. 281; nb. 2; (1995); p. 195 203, View in Reaxys 9 of 22
Target Name
Adenosine receptor A1 [Rattus norvegicus]
Target Synonyms
adenosine receptor a1; adora1
Target Uniprot ID
p25099
Target, Subunit, Species
Adenosine receptor A1 [Rattus norvegicus]
Target Mutant/Chimera Details
Adenosine receptor A1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
61
Measurement Parameter
Ki
Unit
µM
Quantitative value
25.2
Deviation
7.50000
Measurement pX
4.6
Concomitants: Compound RN
1181455; 1181455
Concomitants: Compound name
PIA; [3H]-PIA
Concomitants: Compound role
NSB; RAD
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; vol. 15; nb. 1-3; (1996); p. 693 - 717, View in Reaxys 10 of 22
Target Name
Adenosine receptor A2a [Rattus norvegicus]
Target Synonyms
adenosine receptor a2a; adora2a
Target Uniprot ID
p30543
Target, Subunit, Species
Adenosine receptor A2a [Rattus norvegicus]
Target Mutant/Chimera Details
Adenosine receptor A2a [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
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Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
61
Substance Dose
0.000100000 M
Measurement Parameter
% Inhibition
Unit
%
Qualitative value
<=
Quantitative value
10
Measurement pX
1
Concomitants: Compound RN
43957; 3641320
Concomitants: Compound name
2-Chloroadenosine; [3H]-CGS 21680
Concomitants: Compound role
NSB; RAD
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; vol. 15; nb. 1-3; (1996); p. 693 - 717, View in Reaxys 11 of 22
Target Name
Adenosine receptor A3 [Rattus norvegicus]
Target Synonyms
adenosine receptor a3; adora3; tgpcr1
Target Uniprot ID
p28647
Target, Subunit, Species
Adenosine receptor A3 [Rattus norvegicus]
Target Mutant/Chimera Details
Adenosine receptor A3 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Substance RN
6871759View in Reaxys
Substance Name
61
Measurement Parameter
Ki
Unit
µM
Quantitative value
157
Deviation
3
Measurement pX
3.8
Concomitants: Compound RN
4912716; 6832347
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Concomitants: Compound name
(-)-(R)-PIA; [125I]-I-AB-MECA
Concomitants: Compound role
NSB; RAD
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; vol. 15; nb. 1-3; (1996); p. 693 - 717, View in Reaxys 12 of 22
Target Name
Adenosine receptor A1 [Rattus norvegicus]
Target Synonyms
adenosine receptor a1; adora1
Target Uniprot ID
p25099
Target, Subunit, Species
Adenosine receptor A1 [Rattus norvegicus]
Target Mutant/Chimera Details
Adenosine receptor A1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Action on Target
Antagonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Adenylate cyclase activity
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
adipose tissue
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
61
Measurement Parameter
Kb
Unit
µM
Quantitative value
600
Measurement pX
3.22
Concomitants: Compound RN
9220381; 4912716; 73010; 2213857
Concomitants: Compound name
cAMP; (-)-(R)-PIA; [32P]-ATP; Isoproterenol
Concomitants: Compound role
COM; AGO; MAR; IND
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; vol. 15; nb. 1-3; (1996); p. 693 - 717, View in Reaxys 13 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
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Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cell Fraction
Membrane
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Measurement Parameter
IC50
Unit
nM
Quantitative value
10.1
Measurement pX
8
Concomitants: Compound RN
11305494; 1072822
Concomitants: Compound name
[3H]-Dopamine; Dopamine
Concomitants: Compound role
MAR; SUB
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
corpus striatum
Cell Fraction
Homogenate
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Measurement Parameter
IC50
Unit
nM
Quantitative value
40
Measurement pX
7.4
Concomitants: Compound RN
578614; 5696321
Concomitants: Compound name
[3H]-GBR 12935; Vanoxerine dihydrochloride
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15 of 22
Concomitants: Compound role
RAD; NSB
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
telencephalon
Substance RN
6871759View in Reaxys
Substance Name
Amfonelic acid
Measurement Parameter
IC50
Unit
µM
Quantitative value
507
Deviation
132
Measurement pX
3.29
Concomitants: Compound RN
2205872
Concomitants: Compound name
[3H]-d-Amphetamine
Concomitants: Compound role
RAD
Zaczek; Culp; Goldberg; Mccann; De Souza; The Journal of pharmacology and experimental therapeutics; vol. 257; nb. 2; (1991); p. 820 - 829, View in Reaxys 16 of 22
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : gnawing in 50 percent of miceTarget : C57BL/6J mouseBioassay : in vivo; 21-to 32-g mice housed in groups of 4 in dimly illuminated and quiet testing room with free access to food and water; gnawing upon corrugated packing paper was behavioral measure (8 mice per dose, 75 min after drug administration)
Substance RN
6871759View in Reaxys
Substance Name
43254
Substance Dose
0 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
1.25
Tirelli; Witkin; Journal of Pharmacology and Experimental Therapeutics; vol. 273; nb. 1; (1995); p. 7 - 16, View in Reaxys 17 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Inhibitor
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19 of 22
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro inhibitory activity of the compound against rat striatal synaptosomes Dopamine reuptake using 1 nM 3H-dopamine as radioligand upon incubation with krebs-ringer buffer, at pH 7.2 and 37 degree C for 25 min
Biological Species/NCBI ID
Rattus norvegicus
Substance RN
6871759View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
<
Quantitative value
0.1
Measurement pX
7
Concomitants: Compound name
[3H]Dopamine
Concomitants: Compound role
RAD
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]; Sodium-dependent serotonin transporter [Rattus norvegicus]; sodium-dependent dopamine transporter [rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3 + 5ht transporter; 5htt; slc6a4; sodium-dependent serotonin transporter; solute carrier family 6 member 4 + da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977 + p31652 + p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]; Sodium-dependent serotonin transporter [Rattus norvegicus]; sodium-dependent dopamine transporter [rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild; Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild; sodium-dependent dopamine transporter [rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus; Rattus norvegicus; Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the comoound towards rat forebriain Dopamine transporter using [3H]2--carbomethoxy-3--[4-iodophenyl]tropane as radioligand; 18.7 +/- 1.3
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
brain
Substance RN
6871759View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
>
Quantitative value
10000
Measurement pX
1
Concomitants: Compound name
[3H]2-carbomethoxy-3-[4-iodophenyl]tropane
Concomitants: Compound role
RAD
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]; Sodium-dependent serotonin transporter [Rattus norvegicus]; sodium-dependent dopamine transporter [rattus norvegicus]
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Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3 + 5ht transporter; 5htt; slc6a4; sodium-dependent serotonin transporter; solute carrier family 6 member 4 + da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977 + p31652 + p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]; Sodium-dependent serotonin transporter [Rattus norvegicus]; sodium-dependent dopamine transporter [rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild; Sodium-dependent serotonin transporter [Rattus norvegicus]:Wild; sodium-dependent dopamine transporter [rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus; Rattus norvegicus; Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the comoound towards rat forebriain Dopamine transporter using [3H]2--carbomethoxy-3--[4-iodophenyl]tropane as radioligand; 18.7 +/- 1.3
Biological Species/NCBI ID
Rattus norvegicus
Organs/Tissues
brain
Substance RN
6871759View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
18.7
Measurement pX
7.73
Concomitants: Compound name
[3H]2-carbomethoxy-3-[4-iodophenyl]tropane
Concomitants: Compound role
RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was tested for locomotor stimulant; Potent
Substance RN
6871759View in Reaxys
Qualitative Results
Potent
Measurement Parameter
Activity
Qualitative value
@
M. A. Davis; Annual reports in medicinal chemistry; vol. 3; (1967); p. 14 - 27, View in Reaxys 21 of 22
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Inhibitor
Substance Effect
inhibitory activity
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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2018-04-03 15:14:02
22 of 22
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition of 0.15 nM [125I]RTI-55 binding to Dopamine reuptake in rat striatum
Organs/Tissues
neostriatum
Substance RN
6871759View in Reaxys
Measurement Parameter
IC50
Unit
nM
Qualitative value
=
Quantitative value
160.08
Measurement pX
6.8
Target Name
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [Rattus norvegicus]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Inhibitor
Substance Effect
inhibitory activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Dopamine transporter activity was determined by inhibition of [125I]RTI-55 (0.15 nM) binding in rat striatum
Organs/Tissues
neostriatum
Substance RN
6871759View in Reaxys
Measurement Parameter
IC50
Unit
nM
Qualitative value
=
Quantitative value
160.08
Measurement pX
6.8
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
14/14
2018-04-03 15:14:02