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

Salvadori, S; Marastoni, M; Balboni, Gianfranco; Degli Uberti, E; Tomatis, R.

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.

Scheda prodotto non validato

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Trovami (UniCASearch)

Titolo:	Synthetic tetrapeptides related to dermorphin: potent long lasting analgesic action following subcutaneous administration
Autori:	SALVADORI S MARASTONI M BALBONI, GIANFRANCO DEGLI UBERTI E TOMATIS R. mostra contributor esterni nascondi 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

File in questo prodotto:

Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

UNICA IRIS Institutional Research Information System

Scheda prodotto non validato

File in questo prodotto: