Neuropharmacological properties of V-9-M, a putative neuropeptide derived from procholecystokinin, in the rat

1989 ◽  
Vol 67 (3) ◽  
pp. 223-227 ◽  
Author(s):  
Akira Takashima ◽  
Shinji Itoh

It has been suggested that a nonapeptide called V-9-M (Val-Pro-Val-Glu-Ala-Val-Asp-Pro-Met) is produced by the processing of procholecystokinin. However, its physiological and pharmacological activities are not known. In the present study, synthetic V-9-M amide was injected into the lateral ventricle of the rat and its effects on general activities were observed. V-9-M caused a marked sedation; it suppressed spontaneous activity and hypermotility induced by thyrotropin-releasing hormone, methamphetamine, and apomorphine. Hypomotility induced by small doses of apomorphine was also decreased further. V-9-M caused hypothermia and prolonged the duration of pentobarbital-induced sleep, and it decreased locomotion in an open-field situation. However, V-9-M did not affect appetite in fasted rats.Key words: V-9-M, sedative action, hypothermia, sleep, appetite.

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.


1987 ◽  
Vol 116 (3_Suppl) ◽  
pp. S68-S69
Author(s):  
M. LOSA ◽  
J. ALBA-LOPEZ ◽  
S. SOBIESCZCZYK ◽  
A. KÖNIG ◽  
C. R. PICKARDT ◽  
...  

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