Index: Wichmann, Juergen; Adam, Geo; Roever, Stephan; Hennig, Michael; Scalone, Michelangelo; Cesura, Andrea M.; Dautzenberg, Frank M.; Jenck, Francois European Journal of Medicinal Chemistry, 2000 , vol. 35, # 9 p. 839 - 851
Novel hexahydrospiro [piperidine-4, 1'-pyrrolo [3, 4-c] pyrroles that act as potent and selective orphanin FQ/nociceptin (N/OFQ) receptor (NOP) agonists were identified. The best compound,(+)-5a, potently inhibited 3H-N/OFQ binding to the NOP receptor (K i= 0.49 nM) but was> 1000-fold less potent in binding to MOP, KOP, and DOP opiate receptors. Further,(+)-5a potently stimulated GTPγS binding to NOP membranes (EC50= 65 nM) and ...
