acetylcholine turnover
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2021 ◽  
Vol 22 (12) ◽  
pp. 6230
Author(s):  
Katalin Prokai-Tatrai ◽  
Vien Nguyen ◽  
Laszlo Prokai

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 ([Glu2]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 [β-Glu2]TRH was found to suppress the analeptic and antidepressant-like pharmacological activities of TRH without eliciting intrinsic effects in these paradigms. [β-Glu2]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, [β-Glu2]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.



2003 ◽  
Vol 88 (2) ◽  
pp. 502-512 ◽  
Author(s):  
James E. Smith ◽  
Tina C. Vaughn ◽  
Conchita Co


1989 ◽  
Vol 165 (2-3) ◽  
pp. 209-214 ◽  
Author(s):  
Cristina Cosi ◽  
Anthony C. Altar ◽  
Paul L. Wood


1988 ◽  
Vol 87 (3) ◽  
pp. 293-296 ◽  
Author(s):  
C. Cosi ◽  
P.L. Wood


1988 ◽  
Vol 445 (1) ◽  
pp. 160-164 ◽  
Author(s):  
Susan E. Robinson ◽  
Kristi L. Hambrecht ◽  
Bruce G. Lyeth


1987 ◽  
Vol 60 (2) ◽  
pp. 96-99 ◽  
Author(s):  
G. Lundgren ◽  
I. Nordgren ◽  
B. Karlén ◽  
G. Jacobsson


1986 ◽  
Vol 58 (3) ◽  
pp. 372-377 ◽  
Author(s):  
D D Lund ◽  
R P Oda ◽  
B J Pardini ◽  
P G Schmid


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