title: Arylacetamides as peripherally restricted kappa opioid receptor agonists.
abstract: Analogues of the kappa (kappa) opioid receptor agonist, ICI 199441, were prepared. Ki values for these analogues at the cloned human kappa opioid receptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherally restricted than the parent compound, ICI 199441.
authors.affiliation: Adolor Corporation, Malvern, PA 19355, USA. vkumar@adolor.com
authors.forename: V
authors.initials: V
authors.lastname: Kumar
authors.forename: M A
authors.initials: MA
authors.lastname: Marella
authors.forename: L
authors.initials: L
authors.lastname: Cortes-Burgos
authors.forename: A C
authors.initials: AC
authors.lastname: Chang
authors.forename: J A
authors.initials: JA
authors.lastname: Cassel
authors.forename: J D
authors.initials: JD
authors.lastname: Daubert
authors.forename: R N
authors.initials: RN
authors.lastname: DeHaven
authors.forename: D L
authors.initials: DL
authors.lastname: DeHaven-Hudkins
authors.forename: S L
authors.initials: SL
authors.lastname: Gottshall
authors.forename: E
authors.initials: E
authors.lastname: Mansson
authors.forename: A L
authors.initials: AL
authors.lastname: Maycock
mesh_terms: D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D015394:Molecular Structure; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017473:Receptors, Opioid, kappa / Q000819:agonists*
chemical_list: D000081:Acetamides; D000701:Analgesics, Opioid; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; C058468:ICI 199441