Table 1. Human D₁-Like Receptor Binding Data for Synthons" R. B C K₁ ± SEM (nM) compd R 11a H 11b H AHU B C D,R OMe а 619 ± 97.6 D,R 446 ± 25.2 DR D₁/D, D./D, D/D₂ 2300 ± 820 1.4 5.2 3.7 H H 13911.9 31.1 ± 0.462 316 ± 47.1 4.5 10 2.3 12a Me H OMe а 233±22.4 179 ± 18.1 400 ± 83.4 1.3 2.2 1.7 12b Me a H H 58.13.09 13.6±0.488 89.9 ± 6.81 4.3 6.6 1.5 13a -But H n-But Cl OMe H а H 29.8 ± 4.58 2.93 +0.316 13b "Binding inhibition values determined using HEK 293 cells transfected with hDR, hD,R, or hD and ['H]N-methylspiperone radioligand as described. 59 4.4 22.5 ± 4.86 0.363 + 0.052 322 ± 76.0 6.5.1+10.0 1.3 14 11 8.1 179 22
Table 1. Human D₁-Like Receptor Binding Data for Synthons" R. B C K₁ ± SEM (nM) compd R 11a H 11b H AHU B C D,R OMe а 619 ± 97.6 D,R 446 ± 25.2 DR D₁/D, D./D, D/D₂ 2300 ± 820 1.4 5.2 3.7 H H 13911.9 31.1 ± 0.462 316 ± 47.1 4.5 10 2.3 12a Me H OMe а 233±22.4 179 ± 18.1 400 ± 83.4 1.3 2.2 1.7 12b Me a H H 58.13.09 13.6±0.488 89.9 ± 6.81 4.3 6.6 1.5 13a -But H n-But Cl OMe H а H 29.8 ± 4.58 2.93 +0.316 13b "Binding inhibition values determined using HEK 293 cells transfected with hDR, hD,R, or hD and ['H]N-methylspiperone radioligand as described. 59 4.4 22.5 ± 4.86 0.363 + 0.052 322 ± 76.0 6.5.1+10.0 1.3 14 11 8.1 179 22
Biochemistry
6th Edition
ISBN:9781305577206
Author:Reginald H. Garrett, Charles M. Grisham
Publisher:Reginald H. Garrett, Charles M. Grisham
Chapter26: Synthesis And Degradation Of Nucleotides
Section: Chapter Questions
Problem 22P
Related questions
Question
The following table is from Kumar et. al. Highly Selective Dopamine D3 Receptor (DR) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment. J. Med Chem 2016.
![Table 1. Human D₁-Like Receptor Binding Data for Synthons"
R.
B
C
K₁ ± SEM (nM)
compd
R
11a
H
11b
H
AHU
B
C
D,R
OMe
а
619 ± 97.6
D,R
446 ± 25.2
DR
D₁/D,
D./D,
D/D₂
2300 ± 820
1.4
5.2
3.7
H
H
13911.9
31.1 ± 0.462
316 ± 47.1
4.5
10
2.3
12a
Me
H
OMe
а
233±22.4
179 ± 18.1
400 ± 83.4
1.3
2.2
1.7
12b
Me
a
H
H
58.13.09
13.6±0.488
89.9 ± 6.81
4.3
6.6
1.5
13a
-But
H
n-But
Cl
OMe
H
а
H
29.8 ± 4.58
2.93 +0.316
13b
"Binding inhibition values determined using HEK 293 cells transfected with hDR, hD,R, or hD and ['H]N-methylspiperone radioligand as
described. 59
4.4
22.5 ± 4.86
0.363 + 0.052
322 ± 76.0
6.5.1+10.0
1.3
14
11
8.1
179
22](/v2/_next/image?url=https%3A%2F%2Fcontent.bartleby.com%2Fqna-images%2Fquestion%2F4143f45a-5c96-4449-af2f-abda697f3e91%2F3372272e-1bc1-437c-80b9-79477780047b%2Fqym995t_processed.jpeg&w=3840&q=75)
Transcribed Image Text:Table 1. Human D₁-Like Receptor Binding Data for Synthons"
R.
B
C
K₁ ± SEM (nM)
compd
R
11a
H
11b
H
AHU
B
C
D,R
OMe
а
619 ± 97.6
D,R
446 ± 25.2
DR
D₁/D,
D./D,
D/D₂
2300 ± 820
1.4
5.2
3.7
H
H
13911.9
31.1 ± 0.462
316 ± 47.1
4.5
10
2.3
12a
Me
H
OMe
а
233±22.4
179 ± 18.1
400 ± 83.4
1.3
2.2
1.7
12b
Me
a
H
H
58.13.09
13.6±0.488
89.9 ± 6.81
4.3
6.6
1.5
13a
-But
H
n-But
Cl
OMe
H
а
H
29.8 ± 4.58
2.93 +0.316
13b
"Binding inhibition values determined using HEK 293 cells transfected with hDR, hD,R, or hD and ['H]N-methylspiperone radioligand as
described. 59
4.4
22.5 ± 4.86
0.363 + 0.052
322 ± 76.0
6.5.1+10.0
1.3
14
11
8.1
179
22
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