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

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dc.creatorProkai-Tatrai, Katalin
dc.creatorNguyen, Vien
dc.creatorProkai, Laszlo
dc.creator.orcid0000-0001-5595-1346 (Prokai-Tatrai, Katalin)
dc.creator.orcid0000-0002-4559-3458 (Prokai, Laszlo)
dc.date.accessioned2022-11-15T20:25:49Z
dc.date.available2022-11-15T20:25:49Z
dc.date.issued2021-06-09
dc.description.abstractSelective 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.
dc.description.sponsorshipThis research was funded by The Welch Foundation (endowment BK-0031) and the National Institutes of Health (grant number MH059360).
dc.identifier.citationProkai-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
dc.identifier.issn1422-0067
dc.identifier.issue12
dc.identifier.urihttps://hdl.handle.net/20.500.12503/31915
dc.identifier.volume22
dc.publisherMDPI
dc.relation.urihttps://doi.org/10.3390/ijms22126230
dc.rights.holder© 2021 by the authors.
dc.rights.licenseAttribution 4.0 International (CC BY 4.0)
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.sourceInternational Journal of Molecular Sciences
dc.subject[beta-Glu2]TRH
dc.subjectacetylcholine
dc.subjectanalepsia
dc.subjectantidepressant
dc.subjectfunctional antagonist
dc.subjectin vivo microdialysis
dc.subjectpeptide analogues
dc.subjectthyrotropin-releasing hormone (TRH)
dc.subject.meshAnimals
dc.subject.meshAntidepressive Agents / chemistry
dc.subject.meshAntidepressive Agents / pharmacology
dc.subject.meshCentral Nervous System Stimulants / chemistry
dc.subject.meshCentral Nervous System Stimulants / pharmacology
dc.subject.meshHippocampus / metabolism
dc.subject.meshHippocampus / pathology
dc.subject.meshMale
dc.subject.meshMice
dc.subject.meshPeptides / chemistry
dc.subject.meshPeptides / pharmacology
dc.subject.meshRats
dc.subject.meshRats, Sprague-Dawley
dc.subject.meshThyrotropin-Releasing Hormone / antagonists & inhibitors
dc.subject.meshThyrotropin-Releasing Hormone / metabolism
dc.title[beta-Glu(2)]TRH Is a Functional Antagonist of Thyrotropin-Releasing Hormone (TRH) in the Rodent Brain
dc.typeArticle
dc.type.materialtext

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