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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