[Comparative study of the interaction of purine antagonists with adenosine receptors of bone marrow lymphocytes and lymphoblasts].
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.
Sergeev
P V
PV
Dukhanin
A S
AS
Stankevich
L I
LI
Erina
T A
TA
Bulaeva
N N
NN
Semeĭkin
A V
AV
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*
D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D015122:Mercaptopurine; D001379:Azathioprine
Sravnitel'noe issledovanie vzaimodeĭstviia antagonistov purina s adenozinovymi retseptorami limfotsitov i limfoblastov kostnogo mozga.