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Table 1 pIC50 values for H3 agonism

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

 

3H-cAMP accumulation

 

CRE-SPAP

 

agonist

pIC50

n

pIC50

n

histamine

8.55 ± 0.05

12

7.89 ± 0.04

19

N-α-methylhistamine

9.45 ± 0.05

5

8.89 ± 0.04

17

R-α-methylhistamine

9.54 ± 0.06

4

8.94 ± 0.04

16

S-α-methylhistamine

8.31 ± 0.01

5

7.82 ± 0.06

17

imetit

9.91 ± 0.05

5

9.36 ± 0.04

16

immepip

10.30 ± 0.14

5

9.65 ± 0.03

15

immethridine

9.76 ± 0.08

5

9.41 ± 0.04

10

proxyfan

8.31 ± 0.11

5

7.79 ± 0.06

10

VUF 8430

6.38 ± 0.07

6

5.66 ± 0.08

8

Impentamine*

8.43 ± 0.08

5

Site 1 7.59 ± 0.05

8

   

Site 2 5.40 ± 0.05

8

burimamide

6.65 ± 0.10

5

6.37 ± 0.11

6

VUF 5681

8.41 ± 0.10

5

7.60 ± 0.13

5

  1. pIC50 values for 3H-cAMP accumulation and CRE-SPAP production for the ligands found to be agonists at the histamine H3 receptor in CHO-H3-SPAP cells. Values represent mean ± s.e.mean of n separate experiments. * the CRE-SPAP response to impentamine appeared to consist of 2 components (Figure 6a). Of this 50.2 ± 2.0% was occurring via site 1