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Table 3 Schild slopes for the H3-antagonists

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

agonist

iodophenpropit

n

clobenpropit

n

zolatidine

n

conessine

n

thioperamide

n

histamine

1.15 ± 0.04

5

0.98 ± 0.03

3

1.01 ± 0.04

4

1.07 ± 0.03

5

1.01 ± 0.03

4

N-α-methylhistamine

1.12 ± 0.04

5

1.08 ± 0.07

3

1.10 ± 0.12

4

0.98 ± 0.05

4

0.98 ± 0.07

5

R-α-methylhistamine

1.14 ± 0.05

5

1.10 ± 0.06

4

1.04 ± 0.04

3

1.00 ± 0.06

3

1.00 ± 0.05

5

S-α-methylhistamine

1.17 ± 0.04

4

1.09 ± 0.04

3

1.10 ± 0.07

4

1.08 ± 0.04

4

1.01 ± 0.08

6

Imetit

1.09 ± 0.04

5

1.02 ± 0.04

4

1.17 ± 0.05

4

1.18 ± 0.09

4

1.02 ± 0.07

3

immepip

1.13 ± 0.04

4

1.05 ± 0.02

4

1.18 ± 0.08

4

1.09 ± 0.05

4

1.06 ± 0.02

4

immethridine

1.28 ± 0.13

4

1.02 ± 0.04

4

0.96 ± 0.02

4

1.14 ± 0.08

3

1.08 ± 0.04

4

proxyfan

*

 

*

 

0.91 ± 0.11

3

*

 

1.02 ± 0.03

3

  1. Slope of the Schild plot from antagonism of those compounds where 3 different concentrations of antagonists were possible as determined from measurements of CRE-SPAP production from CHO-H3-SPAP cells. Values represent mean ± s.e.mean of n separate experiments.
  2. * Schild plots were not obtained. Schild plots were also not obtained when impentamine and VUF 8430 were agonists