- Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
-
Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.
- Le Bourdonnec, Bertrand,Ajello, Christopher W.,Seida, Pamela R.,Susnow, Roberta G.,Cassel, Joel A.,Belanger, Serge,Stabley, Gabriel J.,DeHaven, Robert N.,DeHaven-Hudkins, Diane L.,Dolle, Roland E.
-
p. 2647 - 2652
(2007/10/03)
-
- Certain benzofuranyl-N-[pyrrolidin-1-YL]-N-methyl-acetamide derivatives useful as opioid agonists
-
PCT No. PCT/US98/07832 Sec. 371 Date Jun. 30, 1999 Sec. 102(e) Date Jun. 30, 1999 PCT Filed Apr. 17, 1998 PCT Pub. No. WO98/49141 PCT Pub. Date Nov. 5, 1998The novel compounds of formula (I) of the instant invention are selective kappa opioid agonists use
- -
-
-
- Isothiocyanate-Substituted κ-Selective Opioid Receptor Ligands Derived from N-Methyl-N-phenylacetamide
-
The synthesis of isothiocyanate-substituted κ-selective opioid ligands derived from N-methyl-N-ethyl>phenylacetamide (8) and their effects in radioligand displacement assays are reported.Ligands 3-5 with the S-absolu
- Weerawarna, A. Ananda,Davis, Ronda D.,Nelson, Wendel L.
-
p. 2856 - 2864
(2007/10/02)
-