DAMGO, a mu-opioid receptor selective agonist, distinguishes between mu- and delta-opioid receptors around their first extracellular loops.
FEBS Lett
; 357(1): 93-7, 1995 Jan 02.
Article
em En
| MEDLINE
| ID: mdl-8001688
ABSTRACT
The structural basis of mu-opioid receptor (OPR) for the specificity in its ligand binding was investigated using chimeric mu/delta-OPRs. Replacement of the region around the first extracellular loop of delta-OPR with the corresponding region of mu-OPR gave the resultant chimeric receptor the similar affinity to DAMGO compared with the native mu-OPR. The reciprocal replacement deprived the high affinity to DAMGO from mu-OPR. These results indicate that the difference(s) in the structure around the first extracellular loop is critical for DAMGO to distinguish between mu- and delta-OPRs. Furthermore, displacement studies revealed that this region is partly involved in the discrimination between mu- and delta-OPRs by other peptidic mu-selective ligands, such as dermorphin, morphiceptin and CTOP, but not by non-peptidic ligands, such as morphine and naloxone.
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Base de dados:
MEDLINE
Assunto principal:
Encefalinas
/
Receptores Opioides delta
/
Receptores Opioides mu
Limite:
Animals
Idioma:
En
Ano de publicação:
1995
Tipo de documento:
Article