Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.
Bioorg Med Chem Lett
; 10(2): 167-70, 2000 Jan 17.
Article
en En
| MEDLINE
| ID: mdl-10673103
ABSTRACT
A series of Dmt-Tic analogues with substitution on the Tic aromatic ring has been synthesized and evaluated for opioid receptor affinity and activation. Incorporation of large hydrophobic groups at position 7 of Tic did not greatly alter the delta opioid receptor binding affinities of the dipeptides whereas substitution at position 6 substantially diminished their affinity. These modified Dmt-Tic peptides showed binding affinities as low as 2.5 nM with up to 500-fold selectivity for the delta versus mu opioid receptor and proved to be delta receptor antagonists.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tirosina
/
Receptores Opioides delta
/
Tetrahidroisoquinolinas
/
Dipéptidos
/
Isoquinolinas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2000
Tipo del documento:
Article
País de afiliación:
Canadá