title: A SURVEY OF NONXANTHINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS.
abstract: The binding affinities at rat A1, A2a, and A3adenosine receptors of a wide range of heterocyclic derivatives have been determined. Mono-, bi-, tricyclic and macrocyclic compounds were screened in binding assays, using either [3H]PIA or [3H]CGS 21680 in rat brain membranes or [125I]AB-MECA in CHO cells stably transfected with rat A3receptors. Several new classes of adenosine antagonists (e.g.5-oxoimidazopyrimidines and a pyrazoloquinazoline) were identified. Various sulfonylpiperazines, 11-hydroxytetrahydrocarbazolenine, 4H-pyrido[1,2-a]pyrimidinone, folic acid, and cytochalasin H and J bound to A3receptors selectively. Moreover, cytochalasin A, which bound to A1adenosine receptors with Kivalue of 1.9 μM, inhibited adenylyl cyclase in rat adipocytes, but not via reversible A1receptor binding.
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Suhaib M
authors.initials: SM
authors.lastname: Siddiqi
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Xiao-Duo
authors.initials: XD
authors.lastname: Ji
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Neli
authors.initials: N
authors.lastname: Melman
authors.affiliation: Departments of Medicine and Pharmacology, Duke University Medical Center, Durham, NC 27710.
authors.forename: Mark E
authors.initials: ME
authors.lastname: Olah
authors.affiliation: Biochemical Mechanisms Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Rahul
authors.initials: R
authors.lastname: Jain
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Patricia
authors.initials: P
authors.lastname: Evans
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Marc
authors.initials: M
authors.lastname: Glashofer
authors.affiliation: Pharmacodynamics Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: William L
authors.initials: WL
authors.lastname: Padgett
authors.affiliation: Biochemical Mechanisms Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Louis A
authors.initials: LA
authors.lastname: Cohen
authors.affiliation: Pharmacodynamics Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: John W
authors.initials: JW
authors.lastname: Daly
authors.affiliation: Departments of Medicine and Pharmacology, Duke University Medical Center, Durham, NC 27710.
authors.forename: Gary L
authors.initials: GL
authors.lastname: Stiles
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson