Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
J Med Chem
; 44(15): 2387-90, 2001 Jul 19.
Article
en En
| MEDLINE
| ID: mdl-11448220
ABSTRACT
The design, synthesis and pharmacological evaluation of a novel class of Dmt-Tic dipeptide analogues are described. These resulting analogues bearing different C-terminal functionalities were found to bind to the human delta receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the delta receptor. Several dipeptides also showed good binding affinities with full activation of the human kappa receptor, a novel property for those ligands.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tirosina
/
Receptores Opioides delta
/
Receptores Opioides kappa
/
Receptores Opioides mu
/
Tetrahidroisoquinolinas
/
Dipéptidos
/
Isoquinolinas
Límite:
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2001
Tipo del documento:
Article