title: [Comparative study of the interaction of purine antagonists with adenosine receptors of bone marrow lymphocytes and lymphoblasts].
abstract: In this study we used the radiolabeled selective ligand (3H-NECA) of A2-types purine receptors in order to investigate specific NECA binding with human blood lymphocytes and bone marrow lymphoblasts. Relative affinity of 6-mercaptopurine and azathioprine for purine receptors was determined. One type of high affinity NECA binding sites have been shown on the lymphocytes (Kd = 0.57 mkM, Bmax = 0.63 pmol/10(6) cells), which selectively interacted with AZT, but not 6-MP. Relative potencies of substance in competitive radioassay: adenosine > AZT > 6-MP. Two classes NECA binding sites on the lymphoblasts have been identified. One of them corresponds to lymphocyte receptors. The second type of NECA binding sites is characterised by following parameters: Kd = 6.5 mkM and Bmax = 1.5 pmole/10(6) cells. They are selective sensitized to 6-MP. Relative affinity changes in the line: 6-MP > adenosine > AZT.
authors.forename: P V
authors.initials: PV
authors.lastname: Sergeev
authors.forename: A S
authors.initials: AS
authors.lastname: Dukhanin
authors.forename: L I
authors.initials: LI
authors.lastname: Stankevich
authors.forename: T A
authors.initials: TA
authors.lastname: Erina
authors.forename: N N
authors.initials: NN
authors.lastname: Bulaeva
authors.forename: A V
authors.initials: AV
authors.lastname: Semeĭkin
mesh_terms: D001379:Azathioprine / Q000378:metabolism*; D001853:Bone Marrow / Q000378:metabolism*; D001854:Bone Marrow Cells; D006801:Humans; D008214:Lymphocytes / Q000378:metabolism*; D015122:Mercaptopurine / Q000378:metabolism*; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000378:metabolism; D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D013234:Stem Cells / Q000378:metabolism*
chemical_list: D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D015122:Mercaptopurine; D001379:Azathioprine
vernacular_title: Sravnitel'noe issledovanie vzaimodeĭstviia antagonistov purina s adenozinovymi retseptorami limfotsitov i limfoblastov kostnogo mozga.