title: N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.
abstract: A series of N,N-dialkyl-4-(9-aryltropanylidenemethyl)benzamides was prepared. The lead compounds, 15a and 15c, exhibited extremely high affinity for the delta opioid receptor with excellent selectivity versus the micro opioid receptor. They were full agonists at the delta opioid receptor, as assessed by stimulation of GTPgammaS binding, and displayed antinociceptive activity.
authors.affiliation: Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, Welsh and McKean Roads, PO 776, Spring House, PA 19477-0776, USA. jcarson@prdus.jnj.com
authors.forename: John R
authors.initials: JR
authors.lastname: Carson
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Coats
authors.forename: Ellen E
authors.initials: EE
authors.lastname: Codd
authors.forename: Scott L
authors.initials: SL
authors.lastname: Dax
authors.forename: Jung
authors.initials: J
authors.lastname: Lee
authors.forename: Rebecca P
authors.initials: RP
authors.lastname: Martinez
authors.forename: Lou Anne
authors.initials: LA
authors.lastname: Neilson
authors.forename: Philip M
authors.initials: PM
authors.lastname: Pitis
authors.forename: Sui-Po
authors.initials: SP
authors.lastname: Zhang
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D017465:Receptors, Opioid, delta / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000701:Analgesics, Opioid; D001549:Benzamides; D017465:Receptors, Opioid, delta; D016244:Guanosine 5'-O-(3-Thiotriphosphate)