A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃ receptor stably expressed in CHO-K1 cells.

ABSTRACT:

Background and purpose

An alanine to valine exchange at amino acid position 280 (A280V) in the third intracellular loop of the human histamine H₃ receptor was first identified in a patient suffering from Shy-Drager syndrome and later reported as a risk factor for migraine. Here, we have compared the pharmacological and signalling properties of wild-type (hH₃ R(WT)) and A280V mutant (hH₃ R(A280V)) receptors stably expressed in CHO-K1 cells.

Experimental approach

The hH₃ R(A280V) cDNA was created by overlapping extension PCR amplification. Receptor expression and affinity were assessed by radioligand (N-α-[methyl-³H]-histamine) binding to cell membranes, and receptor function by the inhibition of forskolin-induced cAMP accumulation and stimulation of ERK1/2 phosphorylation in

SUBMITTER: Flores-Clemente C 

PROVIDER: S-EPMC3764854 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature