Author/Authors :
James B. Thomas، نويسنده , , S. Wayne Mascarella، نويسنده , , Jason P. Burgess، نويسنده , , Heng Xu، نويسنده , , Karen B. McCullough، نويسنده , , Richard B. Rothman، نويسنده , , Judith L. Flippen-Anderson، نويسنده , , Clifford F. George، نويسنده , , Buddy E. Cantrell، نويسنده , , Dennis M. Zimmerman، نويسنده , , F. Ivy Carroll، نويسنده ,
Abstract :
N-Methyl- and N-phenylethyl-(±)-1,2,3,4,4a,5,10,10a-octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines (4 and 5, respectively) were found to be pure opioid antagonists. These compounds were shown to share many of the characteristics identified with the N-methyl- and N-phenylethyl trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine (1 and 2, respectively) including N-substituent mediated potency and a lack of N-substituent mediated antagonism. These data suggest that compounds 4 and 5 and the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines (1 and 2) may interact with opioid receptors similarly.
