A simple novel approach for detecting blood-brain barrier permeability using GPCR internalization.

ABSTRACT:

Aims

Impairment of blood-brain barrier (BBB) is involved in numerous neurological diseases from developmental to aging stages. Reliable imaging of increased BBB permeability is therefore crucial for basic research and preclinical studies. Today, the analysis of extravasation of exogenous dyes is the principal method to study BBB leakage. However, these procedures are challenging to apply in pups and embryos and may appear difficult to interpret. Here we introduce a novel approach based on agonist-induced internalization of a neuronal G protein-coupled receptor widely distributed in the mammalian brain, the somatostatin receptor type 2 (SST2).

Methods

The clinically approved SST2 agonist octreotide (1 kDa), when injected intraperitoneally does not cross an intact BBB. At site

SUBMITTER: Csaba Z 

PROVIDER: S-EPMC7891648 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature