Title : Ligand-specific contribution of the N terminus and E2-loop to pharmacological properties of the histamine H1-receptor.

Pub. Date : 2008 Sep

PMID : 18577700






4 Functional Relationships(s)
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1 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine histamine receptor H1 Homo sapiens
2 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine histamine receptor H1 Homo sapiens
3 In the series hH(1)R > h(gpE2)H(1)R > h(gpNgpE2)H(1)R, we observed a significant decrease in potency of histamine 1 in the GTPase assay. Histamine histamine receptor H1 Homo sapiens
4 In conclusion, the differences in N terminus and E2-loop between hH(1)R and gpH(1)R exert an influence on affinity and/or potency for histamine and phenoprodifens 5, 6R, and 6S. Histamine histamine receptor H1 Homo sapiens