No abstract

Nucleoside transport inhibition is the major, if not the only, determinant for efficacy of R 75,231 and draflazine as cardioprotective agents. Taken together with the evidence for a role of endogenous adenosine, the benefit from nucleoside transport inhibition in this model may be the result of prolonged accumulation of endogenous adenosine.

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Two cellular model systems for the in vitro study of biochemical and pharmacological effects of new p-adrenergic compounds were compared: the human neutrophilic polymorphonuclear leukocyte and the hamster white fat tissue adipocyte. The adipocyte p-adrenoceptor governing the physiological response is atypical in nature, whereas neutrophils seem to have a homogeneous p2-adrenoceptor population. Both model systems have their own advantages, but as far as pharmacological characterisation is concerned, the &-adrenoceptor of neutrophils is far more sensitive and this model system is an obvious choice for the comparison of, for example, isomers. The differentiation between R 67 138 and R 67 145, optical isomers of the p-adrenoceptor antagonist nebivolol (R 67 555), is 20 times larger on neutrophils than on adipocytes. Some broader applications of both systems are discussed.

No abstract