Regulation of heterologously expressed 5-HT_1B receptors coupling to potassium channels in AtT-20 cells.

ABSTRACT:

Background and purpose

5-HT_1B receptors are widely expressed GPCRs and a target of triptans, the most commonly prescribed anti-migraine drugs. There is very limited information about the acute, agonist-induced regulation of 5-HT_1B receptor signalling and so we sought to characterize this in a neuron-like system.

Experimental approach

Epitope-tagged human 5-HT_1B receptors were expressed in mouse AtT20 cells. 5-HT_1B receptor signalling was assessed using whole-cell patch-clamp recordings of endogenous G protein-gated inwardly rectified potassium (GIRK) channels, and receptor localization measured using immunofluorescence.

Key results

5-HT (EC₅₀ 65 nM) and sumatriptan (EC₅₀ 165 nM) activated GIRK channels

SUBMITTER: Heblinski M 

PROVIDER: S-EPMC6329624 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature