title: Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives.
abstract: Novel benzo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1.
authors.affiliation: Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, 532-8514, Osaka, Japan.
authors.forename: Hiromichi
authors.initials: H
authors.lastname: Itani
authors.forename: Harunobu
authors.initials: H
authors.lastname: Ito
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Sakata
authors.forename: Yoshifumi
authors.initials: Y
authors.lastname: Hatakeyama
authors.forename: Hiroko
authors.initials: H
authors.lastname: Oohashi
authors.forename: Yoshinari
authors.initials: Y
authors.lastname: Satoh
mesh_terms: D019817:Benzoic Acid / Q000737:chemistry*; D003508:Cycloheptanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D003508:Cycloheptanes; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; D019817:Benzoic Acid