[beta-Glu(2)]TRH Is a Functional Antagonist of Thyrotropin-Releasing Hormone (TRH) in the Rodent Brain

Date

2021-06-09

Authors

Prokai-Tatrai, Katalin
Nguyen, Vien
Prokai, Laszlo

ORCID

0000-0001-5595-1346 (Prokai-Tatrai, Katalin)
0000-0002-4559-3458 (Prokai, Laszlo)

Journal Title

Journal ISSN

Volume Title

Publisher

MDPI

Abstract

Selective antagonists of thyrotropin-releasing hormone (TRH; pGlu-His-Pro-NH2), in order to enable a better understanding of this peptide's central functions, have not been identified. Using pGlu-Glu-Pro-NH2 ([Glu(2)]TRH) as a lead peptide and with modification at its central residue, our studies focused on some of its analogues synthesized as potential functional antagonists of TRH in the rodent brain. Among the peptides studied, the novel isomeric analogue [beta-Glu(2)]TRH was found to suppress the analeptic and antidepressant-like pharmacological activities of TRH without eliciting intrinsic effects in these paradigms. [beta-Glu(2)]TRH also completely reversed TRH's stimulation of acetylcholine turnover in the rat hippocampus without a cholinergic activity of its own, which was demonstrated through in vivo microdialysis experiments. Altogether, [beta-Glu(2)]TRH emerged as the first selective functional antagonist of TRH's prominent cholinergic actions, by which this endogenous peptide elicits a vast array of central effects.

Description

Citation

Prokai-Tatrai, K., Nguyen, V., & Prokai, L. (2021). [[beta]-Glu2]TRH Is a Functional Antagonist of Thyrotropin-Releasing Hormone (TRH) in the Rodent Brain. International journal of molecular sciences, 22(12), 6230. https://doi.org/10.3390/ijms22126230

Rights

© 2021 by the authors.

License

Attribution 4.0 International (CC BY 4.0)