Dépression - page 3 - Publications Scientifiques

Dernière publication 01/09/2014

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,...

Array
(
    [id_prestablog_news] => 641
    [id_shop] => 1
    [date] => 2014-09-01 00:00:00
    [date_modification] => 2024-02-09 14:15:11
    [langues] => ["1","2"]
    [actif] => 1
    [slide] => 0
    [url_redirect] => 
    [average_rating] => 
    [number_rating] => 
    [author_id] => 1
    [featured] => 0
    [prim_key] => 1254
    [id_lang] => 2
    [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
    [content] => 
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)
    [meta_description] => 
    [meta_keywords] => http://www.ncbi.nlm.nih.gov/pubmed/25047937
    [meta_title] => 
    [link_rewrite] => antinociceptive-and-antidepressant-like-action-of-endomorphin-2-analogs-with-proline-surrogates-in-position-2
    [actif_langue] => 1
    [read] => 1003
    [count_comments] => 0
    [id] => 641
    [categories] => Array
        (
            [57] => Array
                (
                    [id_prestablog_categorie] => 57
                    [title] => Dépression
                    [link_rewrite] => Depression
                )

            [10] => Array
                (
                    [id_prestablog_categorie] => 10
                    [title] => Douleur
                    [link_rewrite] => Douleur
                )

            [27] => Array
                (
                    [id_prestablog_categorie] => 27
                    [title] => Douleurs générales
                    [link_rewrite] => Douleurs-generales
                )

            [2] => Array
                (
                    [id_prestablog_categorie] => 2
                    [title] => Publications
                    [link_rewrite] => publications
                )

            [15] => Array
                (
                    [id_prestablog_categorie] => 15
                    [title] => Troubles de l'humeur
                    [link_rewrite] => Troubles-de-l-humeur
                )

        )

    [authors] => 
    [paragraph_crop] => Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline [...]
    [link_for_unique] => 1
    [products_liaison] => Array
        (
            [2] => Array
                (
                    [name] => Test de suspension caudale automatique- Sans-fil
                    [description_short] => 
La version 5 du Test de Suspension Caudale de Bioseb, basée sur des capteurs de force ainsi que sur de l'acquisition vidéo, est la seule et unique solution totalement automatisée au monde pour effectuer un test de désespoir comportemental simple et objectif sur souris. Il s'agit d'une méthode rapide, fiable et sans douleur pour tester les effets psychotropes de drogues et substances comme les antidépresseurs et les sédatifs. Ce test classique et indolore pour la recherche sur l'anxiété et la dépression est désormais présenté avec un nouveau logiciel puissant et moderne, dans une version sans-fil BlueTooth.

                    [thumb] => 
                    [img_empty] => /var/www/vhosts/de3310.ispfr.net/bioseb2024/modules/prestablog/views/img/product_link_white.jpg
                    [image_presente] => 1
                    [link] => https://bioseb.com/fr/anxiete-depression/2-tail-suspension-test-wireless.html
                )

            [973] => Array
                (
                    [name] => Test de Nage Forcée: Nouveau FST DUAL SENSOR
                    [description_short] => 
Le nouveau Test de Nage Forcée Bioseb DUAL SENSOR à été développé selon une double approche:
En combinant une double acquisition, vibrations et trace vidéo,
 l'algorithme TYC (Train-Your-Computer) compare les deux sources capteur pour déterminer en temps réel le comportement de l'animal, rendant les résultats complètement indépendants de l'opérateur.

Le gestionnaire d'expériences, le module d'analyse, les possibilités de relecture et l'algorithme TYC sont parmi les fonctionnalités qui font du FST DUAL SENSOR un instrument très innovant et facile d'utilisation pour les études sur rats et souris (jusqu'à 4 animaux à la fois) pour automatiser le test de Porsolt, ou test de désespoir comportemental.

                    [thumb] => 
                    [img_empty] => /var/www/vhosts/de3310.ispfr.net/bioseb2024/modules/prestablog/views/img/product_link_white.jpg
                    [image_presente] => 1
                    [link] => https://bioseb.com/fr/anxiete-depression/973-forced-swimming-test-new-fst-dual-sensor.html
                )

        )

)
1