New characterization of dihydroergotamine receptor pharmacology in the context of migraine: utilization of a β-arrestin recruitment assay.

ABSTRACT:

Introduction

Dihydroergotamine mesylate (DHE) is an established effective acute therapy for migraine and is often characterized by its broad receptor pharmacology. Knowledge of DHE pharmacology largely comes from studies employing older methodologies.

Objective

To assess DHE receptor activity using high-throughput methods to screen for functional ß-arrestin activity at G protein-coupled receptors (GPCRs).

Methods

Functional receptor activities of DHE and sumatriptan succinate (both 10 μM) were screened against 168 GPCRs using the gpcrMAX assay. Agonist and antagonist effects were considered significant if receptor activity was >30% or inhibited by >50%, respectively. Radiolabeled ligand binding assays were performed for DHE (0.01-300 nM for 5-HT₃ and ₄

SUBMITTER: McConnachie L 

PROVIDER: S-EPMC10703426 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature