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• W1504294313 abstract "Background and Purpose An alanine to valine exchange at amino acid position 280 ( A280V ) in the third intracellular loop of the human histamine H 3 receptor was first identified in a patient suffering from S hy– D rager syndrome and later reported as a risk factor for migraine. Here, we have compared the pharmacological and signalling properties of wild‐type ( hH 3 R WT ) and A280V mutant ( hH 3 R A280V ) receptors stably expressed in CHO‐K1 cells. Experimental Approach The hH 3 R A280V cDNA was created by overlapping extension PCR amplification. Receptor expression and affinity were assessed by radioligand ( N ‐α‐[methyl‐ 3 H ]‐histamine) binding to cell membranes, and receptor function by the inhibition of forskolin‐induced cAMP accumulation and stimulation of ERK1 /2 phosphorylation in intact cells, as well as stimulation of [ 35 S ]‐ GTP γ S binding to cell membranes. Key Results Both receptors were expressed at similar levels with no significant differences in their affinities for H 3 receptor ligands. Upon activation the hH 3 R WT was significantly more efficacious to inhibit forskolin‐induced cAMP accumulation and to stimulate [ 35 S ]‐ GTP γ S binding, with no difference in pEC 50 estimates. The hH 3 R WT was also more efficacious to stimulate ERK1 /2 phosphorylation, but this difference was not significant. The inverse agonist ciproxifan was more efficacious at hH 3 R WT to reduce [ 35 S ]‐ GTP γ S binding but, for both receptors, failed to enhance forskolin‐induced cAMP accumulation. Conclusions and Implications The A280V mutation reduces the signalling efficacy of the human H 3 receptor. This effect may be relevant to the pathophysiology of disorders associated with the mutation. Linked Articles This article is part of a themed issue on Histamine Pharmacology Update. To view the other articles in this issue visit http://dx.doi.org/ 10.1111/bph.2013.170.issue‐1" @default.
• W1504294313 created "2016-06-24" @default.
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• W1504294313 date "2013-08-15" @default.
• W1504294313 modified "2023-09-30" @default.
• W1504294313 title "A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃receptor stably expressed in CHO-K1 cells" @default.
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• W1504294313 doi "https://doi.org/10.1111/bph.12257" @default.
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