Synthesis and Investigation of the Antidepressant Properties of Novel Analogs of Arginine-Vasopressin

A search for novel antidepressant analogs of arginine-vasopressin (AVP) by a computer modeling revealed the following peptide analogs of the C -terminal part of AVP: N -Ac-D-Ser-Pro-D-Arg-Gly-NH 2 , N -Ac-Phe-Pro-Arg-Gly-NH 2 , and N -Ac-Trp-Pro-Arg-Gly-NH 2 . Syntheses of the modeled compounds were...

Full description

Saved in:

Bibliographic Details
Published in:	Russian journal of bioorganic chemistry Vol. 48; no. 3; pp. 576 - 588
Main Authors:	Borodina, K. V., Savanets, O. N., Pustyulga, E. S., Martinovich, V. P., Kravchenko, E. V., Olgomets, L. M., Golubovich, V. P.
Format:	Journal Article
Language:	English
Published:	Moscow Pleiades Publishing 01-06-2022 Springer Nature B.V
Subjects:	Analogs Antidepressants Biochemistry Biomedical and Life Sciences Biomedicine Bioorganic Chemistry Life Sciences Organic Chemistry peptides computer modeling arginine-vasopressin depression rats intranasal administration
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	A search for novel antidepressant analogs of arginine-vasopressin (AVP) by a computer modeling revealed the following peptide analogs of the C -terminal part of AVP: N -Ac-D-Ser-Pro-D-Arg-Gly-NH 2 , N -Ac-Phe-Pro-Arg-Gly-NH 2 , and N -Ac-Trp-Pro-Arg-Gly-NH 2 . Syntheses of the modeled compounds were described in this article. The compounds that could potentially exhibit the antidepressant activity were examined in the forced swimming test. N -Ac-Trp-Pro-Arg-Gly-NH 2 (0.1, 1.0, and 10.0 µg/kg) and N -Ac-D-Ser-Pro-D-Arg-Gly-NH 2 (1.0 µg/kg) were shown to have the highest similarity to the fluoxetine reference antidepressant according to a number of parameters after the intranasal administration to the Wistar male rats.
ISSN:	1068-1620 1608-330X
DOI:	10.1134/S1068162022030050