1.
Bioorg Med Chem Lett
; 11(13): 1717-21, 2001 Jul 09.
Article
in English
| MEDLINE
| ID: mdl-11425545
ABSTRACT
In response to the unexpectedly high affinity for opioid receptors observed in a novel series of cyclazocine analogues where the prototypic 8-OH was replaced by a carboxamido group, we have prepared the corresponding 3-CONH(2) analogues of morphine and naltrexone. High affinity (K(i)=34 and 1.7nM) for mu opioid receptors was seen, however, the new targets were 39- and 11-fold less potent than morphine and naltrexone, respectively.