Inhibition of the development of morphine tolerance by a potent dual μ-/δ-opioid antagonist, H-Dmt-Tic-Lys-NH-CH2-Ph

@article{Jinsmaa2008InhibitionOT,
  title={Inhibition of the development of morphine tolerance by a potent dual $\mu$-/$\delta$-opioid antagonist, H-Dmt-Tic-Lys-NH-CH2-Ph},
  author={Y. Jinsmaa and E. Marczak and G. Balboni and S. Salvadori and L. Lazarus},
  journal={Pharmacology Biochemistry and Behavior},
  year={2008},
  volume={90},
  pages={651-657}
}
Three analogues of the dual mu-/delta-antagonist, H-Dmt-Tic-R-NH-CH2-Ph (R = 1, Lys-Z; 2, Lys-Ac; 3, Lys) were examined in vivo: 1 and 2 exhibited weak bioactivity, while 3 injected intracerebroventricularly was a potent dual antagonist for morphine- and deltorphin C-induced antinociception comparable to naltrindole (delta-antagonist), but 93% as effective as naloxone (nonspecific opioid receptor antagonist) and 4% as active as CTOP, a mu antagonist. Subcutaneous or oral administration of 3… Expand
Orally administered H-Dmt-Tic-Lys-NH-CH2-Ph (MZ-2), a potent mu/delta-opioid receptor antagonist, regulates obese-related factors in mice.
Endogenous opiates and behavior: 2008
Opioid peptides: potential for drug development.

References

SHOWING 1-10 OF 50 REFERENCES
Delta opioid receptor enhancement of mu opioid receptor-induced antinociception in spinal cord.
  • L. He, N. Lee
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1998
Morphine tolerance in spinal cord is due to interaction between mu- and delta-receptors.
Modulation of mu-mediated antinociception by delta agonists: characterization with antagonists.
Selective blockage of delta opioid receptors prevents the development of morphine tolerance and dependence in mice.
Differentiation of opioid receptor preference by [Dmt1]endomorphin-2-mediated antinociception in the mouse.
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
...
1
2
3
4
5
...