title: Piperazinyl oxime ethers as NK-1 receptor antagonists.
abstract: The synthesis and structure-activity relations for a new class of centrally active NK-1 receptor antagonists are described. The new compounds are based on piperazine 2 and contain an oxime ether functionality. Several new compounds have high affinity for the NK-1 receptor and show good antagonistic activity in the gerbil foot-tapping assay.
authors.affiliation: Solvay Pharmaceuticals, Research Laboratories, C.J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands.
authors.forename: Adri
authors.initials: A
authors.lastname: van den Hoogenband
authors.forename: Jan H
authors.initials: JH
authors.lastname: van Maarseveen
authors.forename: Andrew C
authors.initials: AC
authors.lastname: McCreary
authors.forename: Arie T
authors.initials: AT
authors.lastname: Mulder
authors.forename: Guus J M
authors.initials: GJ
authors.lastname: van Scharrenburg
authors.forename: Herman H
authors.initials: HH
authors.lastname: van Stuivenberg
authors.forename: Theo J J
authors.initials: TJ
authors.lastname: Zethof
authors.forename: Barbara
authors.initials: B
authors.lastname: Zijta
authors.forename: Wouter I
authors.initials: WI
authors.lastname: Iwema Bakker
mesh_terms: D000284:Administration, Oral; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D004353:Drug Evaluation, Preclinical; D004987:Ethers / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D005849:Gerbillinae; D006801:Humans; D008968:Molecular Conformation; D009043:Motor Activity / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists; D010091:Oximes / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010879:Piperazines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013373:Substance P / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology
chemical_list: D014151:Anti-Anxiety Agents; D004987:Ethers; D064729:Neurokinin-1 Receptor Antagonists; D010091:Oximes; D010446:Peptide Fragments; D010879:Piperazines; C068032:GR 73632; D013373:Substance P