The region in the mu opioid receptor conferring selectivity for sufentanil over the delta receptor is different from that over the kappa receptor.
FEBS Lett
; 384(2): 198-202, 1996 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-8612823
ABSTRACT
We determined the binding domains of sufentanil and lofentanil in the mu opioid receptor by comparing their binding affinities to seven mu/delta and six mu/kappa chimeric receptors with those to mu, delta and kappa opioid receptors. TMHs 6 and 7 and the e3 loop of the mu opioid receptor were important for selective binding of sufentanil and lofentanil to the mu over the kappa receptor. TMHs 1-3 and the e1 loop of the mu opioid receptor conferred binding selectivity for sufentanil over the delta receptor. Thus, the region that conferred binding selectivity for sufentanil differs, depending on chimeras used. In addition, the interaction TMHs 1-3 and TMHs 6-7 was crucial for the high affinity binding of these two ligands. These two regions are likely to contain sites of interaction with the ligands or to confer conformations specific to the mu receptor.
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Base de dados:
MEDLINE
Assunto principal:
Sufentanil
/
Receptores Opioides delta
/
Receptores Opioides kappa
/
Receptores Opioides mu
Limite:
Animals
Idioma:
En
Ano de publicação:
1996
Tipo de documento:
Article