AI Article Synopsis
- The study investigated the cross-tolerance between two specific [D-Arg2]-dermorphin tetrapeptide analogs (TDAPG-NH2 and TDAPA) and morphine regarding their pain-relieving effects.
- Systemic administration of these compounds along with morphine over five days led to the development of tolerance, but when tested in morphine-tolerant mice, the analogs still exhibited strong antinociceptive effects.
- Notably, while morphine tolerance was evident with subcutaneous and intracerebroventricular administration, intrathecal morphine maintained its pain-relieving efficacy in mice previously tolerant to the dermorphin analogs.
Article Abstract
Cross-tolerance between [D-Arg2]-dermorphin tetrapeptide analogs and morphine with respect to antinociception was examined in the present set of experiments. Systemic administration of H-Tyr-D-Arg-Phe-Gly-NH2 (TDAPG-NH2), H-Tyr-D-Arg-Phe-beta-Ala-OH (TDAPA) or morphine over a period of 5 days produced the development of tolerance. In the cross-tolerance study, antinociception after subcutaneous (SC), intracerebroventricular (ICV) and intrathecal (IT) administrations of TDAPG-NH2 and TDAPA in morphine-tolerant mice was not significantly different from their respective effects in saline-pretreated control mice. A marked tolerance to SC- and ICV-administered morphine was seen in mice made tolerant to TDAPG-NH2 and TDAPA. However, IT administration of morphine produced no significant decrement in the antinociceptive activity in mice made tolerant to TDAPG-NH2 and TDAPA. These data indicate that [D-Arg2]-dermorphin tetrapeptide analogs can produce significant antinociception in morphine-tolerant mice.
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Article Synopsis
- The study investigated the cross-tolerance between two specific [D-Arg2]-dermorphin tetrapeptide analogs (TDAPG-NH2 and TDAPA) and morphine regarding their pain-relieving effects.
- Systemic administration of these compounds along with morphine over five days led to the development of tolerance, but when tested in morphine-tolerant mice, the analogs still exhibited strong antinociceptive effects.
- Notably, while morphine tolerance was evident with subcutaneous and intracerebroventricular administration, intrathecal morphine maintained its pain-relieving efficacy in mice previously tolerant to the dermorphin analogs.
Comparison of the antinociceptive effects of new [D-Arg2]-dermorphin tetrapeptide analogs and morphine in mice.
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October 1988
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