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Biphalin preferentially recruits peripheral opioid receptors to facilitate analgesia in a mouse model of cancer pain - A comparison with morphine |
Tartalom: | http://real.mtak.hu/49743/ |
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Archívum: | MTA Könyvtár |
Gyűjtemény: |
Status = Published
Type = Article |
Cím: |
Biphalin preferentially recruits peripheral opioid receptors to facilitate analgesia in a mouse model of cancer pain - A comparison with morphine
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Létrehozó: |
Lesniak, Anna
Bochynska-Czyz, Marta
Sacharczuk, Mariusz
Benyhe, Sándor
Misicka, Aleksandra
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Kiadó: |
Elsevier
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Dátum: |
2016
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Téma: |
QH3011 Biochemistry / biokémia
RC0254 Neoplasms. Tumors. Oncology (including Cancer) / daganatok, tumorok, onkolĂłgia
RM Therapeutics. Pharmacology / terápia, gyógyszertan
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Tartalmi leírás: |
The search for new drugs for cancer pain management has been a long-standing goal in basic and clinical research. Classical opioid drugs exert their primary antinociceptive effect upon activating opioid receptors located in the central nervous system. A substantial body of evidence points to the relevance of peripheral opioid receptors as potential targets for cancer pain treatment. Peptides showing limited blood-brain-barrier permeability promote peripheral analgesia in many pain models. In the present study we examined the peripheral and central analgesic effect of intravenously administered biphalin - a dimeric opioid peptide in a mouse skin cancer pain model, developed by an intraplantar inoculation of B16F0 melanoma cells. The effect of biphalin was compared with morphine - a golden standard in cancer pain management. Biphalin produced profound, dose-dependent and naloxone sensitive spinal analgesia. Additionally, the effect in the tumor-bearing paw was largely mediated by peripheral opioid receptors, as it was readily attenuated by the blood-brain-barrier-restricted opioid receptor antagonist - naloxone methiodide. On the contrary, morphine facilitated its analgesic effect primarily by activating spinal opioid receptors. Both drugs induced tolerance in B16F0 - implanted paws after chronic treatment, however biphalin as opposed to morphine, showed little decrease in its activity at the spinal level. Our results indicate that biphalin may be considered a future alternative drug in cancer pain treatment due to an enhanced local analgesic activity as well as lower tolerance liability compared with morphine. (C) 2016 Elsevier B.V. All rights reserved.
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Nyelv: |
angol
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Típus: |
Article
PeerReviewed
info:eu-repo/semantics/article
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Formátum: |
text
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Azonosító: |
Lesniak, Anna and Bochynska-Czyz, Marta and Sacharczuk, Mariusz and Benyhe, Sándor and Misicka, Aleksandra (2016) Biphalin preferentially recruits peripheral opioid receptors to facilitate analgesia in a mouse model of cancer pain - A comparison with morphine. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 89. pp. 39-49. ISSN 0928-0987
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Kapcsolat: |
MTMT:3082860; doi:10.1016/j.ejps.2016.04.014
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