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EN
It is generally accepted that classical opioids exert their antinociceptive effect mainly when binding to opioid receptors located in the central nervous system. However, a growing body of evidence points to the relevance of peripheral opioid receptors in periphery pathology, including cancer. A cancer is very often the cause of pain resulting from peripheral metastasis. The peripheral component of antinociception induced by a dimeric enkephalin analog – biphalin showing limited blood-brainbarrier permeability may prove important in cancer pain therapy. An additional advantage of biphalin is a possibility to treat pain symptoms with reduction of side-effects – a result of the central action of some other opioid analgesics, e.g. morphine. We examined the peripheral and central analgesic effect of biphalin in a murine skin cancer pain model developed by an intraplantar inoculation of B16T0 melanoma cells. Animals developed robust thermal hypersensitivity in the tumor-bearing paw compared to PBS-injected individuals. Biphalin produced stronger analgesia in the tumor-bearing paw than morphine upon a comparable central effect. Our results suggest that biphalin analgesia manifested in the periphery is linked to a less effective transport through the bloodbrain barrier. We speculate that the centrally effective dose of biphalin equipotent to morphine simultaneously produces analgesia via peripheral opioid receptors. Thus, biphalin may become useful in cancer pain treatment as an alternative drug executing a local as well as a central analgesic response with limited undesirable side-effects.
8
Content available remote Antinociceptive effect in rats is induced by the cooling of their whole body
63%
EN
The effect of rats' whole-body cooling on their reactivity to the thermal nociceptive stimulus was determined by means of a hot-plate test. It has been found that a single exposure and a four time daily exposure to a cold temperature (-90° C) induced a significant antinociceptive effect. A possible mechanism of this effect was discussed.
PL
Określano wpływ schładzania ciała szczurów na termiczny bodziec bólowy w teście gorącej płytki. Wykazano, że zarówno jednorazowa, jak i powtarzana codziennie przez cztery dni ekspozycja na niską temperaturę (-90°C) wywoływała znamienny efekt przeciwbólowy. Przedyskutowano prawdopodobne mechanizmy tego zjawiska.
10
Content available Antinociceptive effect of MAS MT in rats
51%
EN
MAS MT is a myotropic decapeptide isolated from Manduca sexta. This peptide exerts stimulatory effect on insects heart-beat frequency. The present study was undertaken in order to determine a probable antinociceptive effect in rats of native synthetic decapeptide, MAS MT-I and its two analogs, heptapeptides MAS MT-II and MAS MT-III. All these peptides were applied directly into the lateral brain ventricle (icv) at three doses: 10, 25 and 50 nmol. The analgesic (antinociceptive) effect was evaluated by a tail immersion test. It was found that two doses of MAS MT-I: 25 and 50 nmol induced significant antinociceptive effect, while MAS MT-II and MAS MT-III exert a less antinociceptive effect in comparison with native MAS MT-I. Prior icv administration of naloxone, an opioid antagonist weakly blocked MAS MT-I effect. We conclude that antinociceptive effect of MAS MT-I in rats is not mediated by central opioid system.
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