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
icon
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
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
Expert Solution
steps

Step by step

Solved in 2 steps

Blurred answer
Similar questions
  • SEE MORE QUESTIONS
Recommended textbooks for you
Biochemistry
Biochemistry
Biochemistry
ISBN:
9781305577206
Author:
Reginald H. Garrett, Charles M. Grisham
Publisher:
Cengage Learning
Biochemistry
Biochemistry
Biochemistry
ISBN:
9781305961135
Author:
Mary K. Campbell, Shawn O. Farrell, Owen M. McDougal
Publisher:
Cengage Learning
Human Heredity: Principles and Issues (MindTap Co…
Human Heredity: Principles and Issues (MindTap Co…
Biology
ISBN:
9781305251052
Author:
Michael Cummings
Publisher:
Cengage Learning
Biology 2e
Biology 2e
Biology
ISBN:
9781947172517
Author:
Matthew Douglas, Jung Choi, Mary Ann Clark
Publisher:
OpenStax
Anatomy & Physiology
Anatomy & Physiology
Biology
ISBN:
9781938168130
Author:
Kelly A. Young, James A. Wise, Peter DeSaix, Dean H. Kruse, Brandon Poe, Eddie Johnson, Jody E. Johnson, Oksana Korol, J. Gordon Betts, Mark Womble
Publisher:
OpenStax College
3-2-1 Code It
3-2-1 Code It
Biology
ISBN:
9781337660549
Author:
GREEN
Publisher:
Cengage