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Table 4 pKD values for clobenproprit and thioperamide

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

 

pKD

 

pKD

 

agonist

clobenpropit

n

thioperamide

n

histamine

9.38 ± 0.12

5

7.38 ± 0.04

4

N-α-methylhistamine

9.43 ± 0.14

5

7.28 ± 0.06

3

R-α-methylhistamine

9.36 ± 0.08

4

7.42 ± 0.09

3

S-α-methylhistamine

9.46 ± 0.08

4

7.45 ± 0.09

3

imetit

9.28 ± 0.07

5

7.48 ± 0.13

4

immepip

9.34 ± 0.15

5

7.46 ± 0.14

4

immethridine

9.32 ± 0.14

5

7.46 ± 0.13

4

proxyfan

9.32 ± 0.03

5

7.33 ± 0.09

4

VUF 8430

9.42 ± 0.10

5

7.43 ± 0.09

4

impentamine

9.46 ± 0.11

4

7.54 ± 0.09

4

burimamide

9.25 ± 0.14

4

7.39 ± 0.12

4

VUF 5681

9.20 ± 0.09

4

7.45 ± 0.10

4

  1. pKD values for clobenpropit and thioperamide as determined from 3H-cAMP accumulation measurements made in the presence of the 12 different agonists. Values represent mean ± s.e.mean of n separate experiments.