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Table 2 pKD values for H3 antagonism

From: Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells

Agonist

pKD values

           
 

Iodophen-propit

n

Cloben-propit

n

zolatidine

n

conessine

n

thioperamide

n

cimetidine

n

histamine

8.65 ± 0.07

19

9.42 ± 0.04

9

6.51 ± 0.07

19

8.29 ± 0.05

15

7.22 ± 0.04

23

5.64 ± 0.11

11

N-α-methylhistamine

8.59 ± 0.10

16

9.42 ± 0.06

15

6.46 ± 0.07

17

8.27 ± 0.04

12

7.37 ± 0.06

18

5.57 ± 0.08

9

R-α-methylhistamine

8.57 ± 0.09

15

9.21 ± 0.08

15

6.52 ± 0.06

14

8.24 ± 0.06

9

7.33 ± 0.04

17

5.62 ± 0.12

8

S-α-methylhistamine

8.72 ± 0.05

14

9.25 ± 0.05

13

6.54 ± 0.07

18

8.28 ± 0.05

12

7.20 ± 0.05

17

5.64 ± 0.06

9

imetit

8.78 ± 0.06

16

9.20 ± 0.05

12

6.62 ± 0.08

17

8.24 ± 0.10

12

7.29 ± 0.06

13

5.64 ± 0.08

10

immepip

8.66 ± 0.07

14

9.36 ± 0.04

12

6.55 ± 0.07

17

8.09 ± 0.07

12

7.22 ± 0.09

15

5.70 ± 0.09

9

immethridine

8.81 ± 0.08

12

9.21 ± 0.06

12

6.66 ± 0.05

12

8.42 ± 0.10

11

7.31 ± 0.06

12

5.72 ± 0.09

4

proxyfan

8.82 ± 0.05

7

9.25 ± 0.08

7

6.78 ± 0.06

9

8.56 ± 0.08

5

7.59 ± 0.03

9

5.61 ± 0.11

6

VUF 8430

8.53 ± 0.08

6

9.11 ± 0.19

4

6.38 ± 0.10

4

8.15 ± 0.08

4

7.15 ± 0.27

4

5.53 ± 0.13

4

impentamine

8.60 ± 0.09

6

9.01 ± 0.10

4

6.52 ± 0.10

4

8.38 ± 0.11

4

7.47 ± 0.10

5

5.70 ± 0.01

5

agonist

Log KD values

           
 

Dimethin-dine

n

Chlorpheni-ramine

n

VUF 5681

n

ranitidine

n

triprolidine

n

clemastine

n

histamine

5.63 ± 0.07

7

5.32 ± 0.06

8

7.77 ± 0.08

5

5.05 ± 0.08

9

5.35 ± 0.05

7

5.73 ± 0.08

10

N-α-methylhistamine

5.67 ± 0.17

6

5.51 ± 0.07

3

7.95 ± 0.14

4

5.05 ± 0.08

9

5.34 ± 0.08

6

5.69 ± 0.13

7

R-α-methylhistamine

5.65 ± 0.04

5

5.44 ± 0.04

4

7.60 ± 0.07

4

5.18 ± 0.06

7

5.58 ± 0.05

5

5.79 ± 0.09

7

S-α-methylhistamine

5.67 ± 0.03

4

5.44 ± 0.08

3

7.75 ± 0.04

4

4.95 ± 0.10

7

5.47 ± 0.08

6

5.74 ± 0.11

8

imetit

5.60 ± 0.16

8

5.58 ± 0.08

4

7.85 ± 0.08

4

4.96 ± 0.09

7

5.43 ± 0.09

7

5.69 ± 0.15

6

immepip

5.72 ± 0.16

5

5.59 ± 0.12

4

7.72 ± 0.10

3

5.12 ± 0.06

6

5.61 ± 0.13

4

5.79 ± 0.15

6

immethridine

5.38 ± 0.05

9

5.53 ± 0.05

4

7.79 ± 0.12

4

5.19 ± 0.09

3

5.53 ± 0.13

3

5.50 ± 0.10

3

proxyfan

5.24 ± 0.14

3

5.39 ± 0.11

5

7.80 ± 0.03

3

4.97 ± 0.12

5

5.23 ± 0.07

5

5.60 ± 0.11

6

VUF 8430

5.11 ± 0.09

3

5.13 ± 0.15

4

7.71 ± 0.16

3

4.72 ± 0.01

3

5.26 ± 0.10

3

5.26 ± 0.06

4

impentamine

5.59 ± 0.24

3

5.21 ± 0.22

4

*

 

5.10 ± 0.09

5

5.65 ± 0.15

4

5.73 ± 0.09

5

  1. pKD values for 12 antagonists as determined from measurements of CRE-SPAP production from CHO-H3-cells made in the presence of the 12 different agonists. Values represent mean ± s.e.mean of n separate experiments. The pKD values quoted are for antagonism of the first component of the impentamine response.
  2. * it was not possible to determine a pKD value for VUF 5681 in the presence of impentamine due to the partial agonist nature of both responses.
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BMC Pharmacology

ISSN: 1471-2210