Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine
The development of morphine-induced antinociceptive tolerance limits its therapeutic efficacy in pain management. Effects of non-benzodiazepine anxiolytics ladasten and GB-115 on the development of antinociceptive tolerance to morphine were studied in albino male rats. The tolerance was induced by d...
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2016-03-01
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| Series: | Фармакокинетика и Фармакодинамика |
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| Online Access: | https://www.pharmacokinetica.ru/jour/article/view/173 |
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| author | M. A. Konstantinopolsky I. V. Chernyakova L. G. Kolik |
| author_facet | M. A. Konstantinopolsky I. V. Chernyakova L. G. Kolik |
| author_sort | M. A. Konstantinopolsky |
| collection | DOAJ |
| description | The development of morphine-induced antinociceptive tolerance limits its therapeutic efficacy in pain management. Effects of non-benzodiazepine anxiolytics ladasten and GB-115 on the development of antinociceptive tolerance to morphine were studied in albino male rats. The tolerance was induced by daily sub-chronic administration of morphine (2,0 mg/kg, i.p., twice daily for 5 days) and assessed in immersion tail-flick test on days 1 and 5. Concomitant sub-chronic administration of dipeptide anxiolytic GB-115 (0,1 mg/kg/5 days, i.p.), developed on the base of endogenous tetrapeptide cholecystokinin (CCK), followed by morphine (2,0 mg/kg), reversed the antinociceptive tolerance to morphine on day 5. GB-115 per se at the same anxiolytic dose demonstrated a short-term analgesic activity on days 1 and 5. In contrast, 2-aminoadamantane derivative Ladasten (50,0 mg/kg/5 days, i.p.) with psychostimulant and anxiolytic activity, failed to do so. Ladasten at dose employed in the study, did not exert any effects on pain threshold on days 1 and 5. Our results suggest that in this well-characterized model of acute somatic pain, the development of tolerance to the antinociceptive effect of systemic morphine can be prevented by co-administration with GB-115. |
| format | Article |
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| institution | Kabale University |
| issn | 2587-7836 2686-8830 |
| language | Russian |
| publishDate | 2016-03-01 |
| publisher | LLC “Publisher OKI” |
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| series | Фармакокинетика и Фармакодинамика |
| spelling | doaj-art-cd1ff9a31f954d18ac8b950b42be9c3b2025-08-20T03:42:31ZrusLLC “Publisher OKI”Фармакокинетика и Фармакодинамика2587-78362686-88302016-03-01024045172Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphineM. A. Konstantinopolsky0I. V. Chernyakova1L. G. Kolik2FSBI «Zakusov Institute of Pharmacology»FSBI «Zakusov Institute of Pharmacology»FSBI «Zakusov Institute of Pharmacology»The development of morphine-induced antinociceptive tolerance limits its therapeutic efficacy in pain management. Effects of non-benzodiazepine anxiolytics ladasten and GB-115 on the development of antinociceptive tolerance to morphine were studied in albino male rats. The tolerance was induced by daily sub-chronic administration of morphine (2,0 mg/kg, i.p., twice daily for 5 days) and assessed in immersion tail-flick test on days 1 and 5. Concomitant sub-chronic administration of dipeptide anxiolytic GB-115 (0,1 mg/kg/5 days, i.p.), developed on the base of endogenous tetrapeptide cholecystokinin (CCK), followed by morphine (2,0 mg/kg), reversed the antinociceptive tolerance to morphine on day 5. GB-115 per se at the same anxiolytic dose demonstrated a short-term analgesic activity on days 1 and 5. In contrast, 2-aminoadamantane derivative Ladasten (50,0 mg/kg/5 days, i.p.) with psychostimulant and anxiolytic activity, failed to do so. Ladasten at dose employed in the study, did not exert any effects on pain threshold on days 1 and 5. Our results suggest that in this well-characterized model of acute somatic pain, the development of tolerance to the antinociceptive effect of systemic morphine can be prevented by co-administration with GB-115.https://www.pharmacokinetica.ru/jour/article/view/173ладастенгб-115толерантность к морфинуанальгезиякрысыladastengb-115tolerance to morphineantinociceptionrats |
| spellingShingle | M. A. Konstantinopolsky I. V. Chernyakova L. G. Kolik Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine Фармакокинетика и Фармакодинамика ладастен гб-115 толерантность к морфину анальгезия крысы ladasten gb-115 tolerance to morphine antinociception rats |
| title | Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine |
| title_full | Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine |
| title_fullStr | Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine |
| title_full_unstemmed | Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine |
| title_short | Experimental assessment of ladasten and GB-115 effects on the antinociceptive tolerance to morphine |
| title_sort | experimental assessment of ladasten and gb 115 effects on the antinociceptive tolerance to morphine |
| topic | ладастен гб-115 толерантность к морфину анальгезия крысы ladasten gb-115 tolerance to morphine antinociception rats |
| url | https://www.pharmacokinetica.ru/jour/article/view/173 |
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