Abstract
A novel series of indoles and 1H-pyrrolo[2,3-b]pyridines having a piperidine ring at the 3-position were synthesized and found to bind with high affinity to the ORL-1 receptor. Structure-activity relationships at the piperidine nitrogen were investigated in each series. Substitution on the phenyl ring and nitrogen atom of the indole and 1H-pyrrolo[2,3-b]pyridine cores generated several selective high-affinity ligands that were agonists of the ORL-1 receptor.
MeSH terms
-
Binding Sites
-
Indoles / chemical synthesis
-
Indoles / chemistry
-
Indoles / pharmacology*
-
Ligands
-
Molecular Structure
-
Nociceptin Receptor
-
Piperidines / chemical synthesis
-
Piperidines / chemistry
-
Piperidines / pharmacology*
-
Pyridines / chemistry
-
Pyridines / pharmacology*
-
Pyrroles / chemical synthesis
-
Pyrroles / chemistry
-
Pyrroles / pharmacology*
-
Receptors, Opioid / agonists*
-
Structure-Activity Relationship
Substances
-
Indoles
-
Ligands
-
Piperidines
-
Pyridines
-
Pyrroles
-
Receptors, Opioid
-
Nociceptin Receptor