New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands

Ballet, S; Salvadori, S; Trapella, C; BRYANT S., D; Jinsmaa, Y; LAZARUS L., H; Negri, L; Giannini, E; Lattanzi, R; Tourwe', D; Balboni, Gianfranco

doi:10.1021/jm0603264

The Aba-Gly scaffold, incorporated into Dmt-Tic ligands (H-Dmt-Tic-Gly-NH-CH2-Ph, H-Dmt-Tic-Gly-NH-Ph, H-Dmt-Tic-NH-CH2-Bid), exhibited mixed micro/delta or delta opioid receptor activities with micro agonism. Substitution of Tic by Aba-Gly coupled to -NH-CH2-Ph (1), -NH-Ph (2), or -Bid (Bid=1H-benzimidazole-2-yl) (3) shifted affinity (Ki(micro)=0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to micro-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief.

Scheda prodotto non validato

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

Trovami (UniCASearch)

Titolo:	New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands
Autori:	BALLET S SALVADORI S TRAPELLA C BRYANT S. D JINSMAA Y LAZARUS L. H NEGRI L GIANNINI E LATTANZI R TOURWE' D BALBONI, GIANFRANCO mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2006
Rivista:	JOURNAL OF MEDICINAL CHEMISTRY
Citazione:	New 2',6'-Dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique mu-Opioid Ligands / BALLET S; SALVADORI S; TRAPELLA C; BRYANT S. D; JINSMAA Y; LAZARUS L. H; NEGRI L; GIANNINI E; LATTANZI R; TOURWE' D; BALBONI G. - 49(2006), pp. 3990-3993.
Abstract:	The Aba-Gly scaffold, incorporated into Dmt-Tic ligands (H-Dmt-Tic-Gly-NH-CH2-Ph, H-Dmt-Tic-Gly-NH-Ph, H-Dmt-Tic-NH-CH2-Bid), exhibited mixed micro/delta or delta opioid receptor activities with micro agonism. Substitution of Tic by Aba-Gly coupled to -NH-CH2-Ph (1), -NH-Ph (2), or -Bid (Bid=1H-benzimidazole-2-yl) (3) shifted affinity (Ki(micro)=0.46, 1.48, and 19.9 nM, respectively), selectivity, and bioactivity to micro-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief.
Handle:	http://hdl.handle.net/11584/17744
Tipologia:	1.1 Articolo in rivista

File in questo prodotto:

Non ci sono file associati a questo prodotto.

Utilizza questo identificativo per citare o creare un link a questo documento:
http://hdl.handle.net/11584/17744

Citazioni

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: