Depression - page 3 Scientific Publications

Latest publication 09/01/2014

Antinociceptive and antidepressant-like action of endomorphin-2 analogs with pro

In our efforts to develop new candidate drugs with antinociceptive and/or antidepressant-like activity, two novel endomorphin-2 (EM-2,...

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    [title] => Antinociceptive and antidepressant-like action of endomorphin-2 analogs with pro
    [paragraph] => Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2
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Authors
Perlikowska R, Piekielna J, Mazur M, Koralewski R, Olczak J, do Rego JC, Fichna J, Modranka J, Janecki T, Janecka A

 Lab
Medical University of Lodz, Lodz, Poland
Journal
Bioorg Med Chem.
Abstract
In our efforts to develop new candidate drugs with antinociceptive and/or antidepressant-like activity, two novel endomorphin-2 (EM-2, Tyr-Pro-Phe-Phe-NH2) analogs, containing proline surrogates in position 2 were synthesized using commercially available racemic trans-4-phenylpyrrolidine-3-carboxylic acid (4-Ph-?-Pro). The obtained mixture of two diastereoisomeric peptides (2a and 2b) was separated by HPLC and both enantiopure analogs were used in the in vitro and in vivo studies. To assign the absolute configuration to the 4-Ph-?-Pro residues in both peptides, the stereoselective synthesis of (3R,4S)-4-phenylpyrrolidine-3-carboxylic acid was performed and this enantiomer was introduced into position 2 of EM-2 sequence. Based on the HPLC retention times we were able to assign the absolute configuration of 4-Ph-?-Pro residues in both peptide analogs. Analog 2a incorporating (3R,4S)-4-Ph-?-Pro residue produced strong analgesia in mice after intracerebroventricular (icv) administration which was antagonized by the ?-opioid receptor (MOR) antagonist, ?-funaltrexamine (?-FNA). This analog also influenced an emotion-related behavior of mice, decreasing immobility time in the forced swimming and tail suspension tests, without affecting locomotor activity. The antidepressant-like effect was reversed by the ?-selective antagonist, naltrindole (NLT) and ?-selective nor-binaltorphimine (nor-BNI). Thus, the experiments with selective opioid receptor antagonists revealed that analgesic action of analog 2a was mediated through the MOR, while the ?- and ?-receptors (DOR and KOR, respectively) were engaged in the antidepressant-like activity. Analog 2b with (3S,4R)-4-Ph-?-Pro in position 2 showed no antinociceptive or antidepressant-like activity in animal studies.
BIOSEB Instruments Used
Tail Suspension Test - Wireless (BIO-TST5),Forced Swimming Test: New FST DUAL SENSOR (BIO-FST-DSM)
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Bioseb's version 5 of the Tail Suspension Test system, based on both strain sensors and video acquisition, is the only fully automatic solution in the world for running a simple and objective despair test on mice. It is a fast, painless, and reliable way for testing psychotropic effects from stimulant doses of drugs such as anti-depressants and sedatives. This classic and painless research test for anxiety and depression is now offered with a new, powerful and modern software, in a wireless, bluetooth-based version.

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 the TYC (Train-Your-Computer) algorithm compares both inputs to determine the animal's behavior in real time, making results completely operator-independent.

Experiment manager, analysis module, replay possibilities and the TYC algorithm are some of the features that make FST DUAL SENSOR a very innovative and easy to use instrument for both mice or rats studies (up to 4 animals can be tested at a time), based on the famous Porsolt Test, or "behavioral despair" test

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