Author/Authors :
James B. Thomas، نويسنده , , Xavier M. Herault، نويسنده , , Richard B. Rothman، نويسنده , , Jason P. Burgess، نويسنده , , S. Wayne Mascarella، نويسنده , , Heng Xu، نويسنده , , Robert B. Horel، نويسنده , , Christina M. Dersch، نويسنده , , F. Ivy Carroll، نويسنده ,
Abstract :
Racemic 4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide (3a) was synthesized and found to have good affinity and selectivity for the δ receptor. these compounds can be viewed as an analog of BW373U86 and SNC-80 where an internal piperazine nitrogen has been transposed with a benzylic carbon. Functionally, 3a behaves as an agonist at the δ receptor with no measurable stimulation of either the μ ork receptor subtypes and was found to be devoid of any measurable amount of antagonist activity for any opioid receptor. A comparison of 3a to SNC-80 and DPDPE in the [35S]GTPγS functional assay suggests that 3a may be more like the peptide DPDPE.
