Synthetic tetrapeptides related to dermorphin: potent long lasting analgesic action following subcutaneous administration

To examine the opioid properties of D-MetO2-dermorphin tetrapeptides, eight new analogues based on the following formula, X-Tyr-D-MetO-Phe-aa-Y, were prepared. All these peptides show dose-related naloxone-reversible opioid effects in vitro and in vivo. Substitution of Sar or Gly-ol for Gly4 were well tolerated by the isolated guinea pig-ileum preparation as well as in the tail-flick test, while alkyl-amidation of the C-terminal proved detrimental. The central activity of H-Tyr-D-MetO-Phe-Gly-NH2, the most potent compound in the series, was higher than that of dermorphin. Following intracerebroventricular or subcutaneous administrations in mice, H-Tyr-D-MetO-Phe-Gly-NH2 was about 1500 and 17 times as analgesic as morphine, respectively.

Trovami (UniCASearch)


Titolo: Synthetic tetrapeptides related to dermorphin: potent long lasting analgesic action following subcutaneous administration
Autori: 
BALBONI, GIANFRANCO
mostra contributor esterni 
Data di pubblicazione: 1985
Rivista: 
PEPTIDES  
Abstract: To examine the opioid properties of D-MetO2-dermorphin tetrapeptides, eight new analogues based on the following formula, X-Tyr-D-MetO-Phe-aa-Y, were prepared. All these peptides show dose-related naloxone-reversible opioid effects in vitro and in vivo. Substitution of Sar or Gly-ol for Gly4 were well tolerated by the isolated guinea pig-ileum preparation as well as in the tail-flick test, while alkyl-amidation of the C-terminal proved detrimental. The central activity of H-Tyr-D-MetO-Phe-Gly-NH2, the most potent compound in the series, was higher than that of dermorphin. Following intracerebroventricular or subcutaneous administrations in mice, H-Tyr-D-MetO-Phe-Gly-NH2 was about 1500 and 17 times as analgesic as morphine, respectively.
Handle: http://hdl.handle.net/11584/6788
Tipologia:1.1 Articolo in rivista

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