Dissociation of the locomotor and hypotensive effects of adenosine analogues in the rat.

Rats implanted with chronic indwelling cannulae were injected in the lateral cerebral ventricle with two adenosine analogues and the effects on spontaneous locomotor activity and blood pressure recorded. Both analogues produced dose-related decreases in locomotor activity, with 5'-N-ethylcarboxamidoadenosine (NECA) exhibiting slightly more potent depressant activity than (-)-N-(1-methyl-2-phenylethyl)adenosine (L-phenylisopropyladenosine) (L-PIA). NECA and L-PIA also produced dose-related reductions in blood pressure but the threshold dose for hypotensive activity was 10-100-fold higher than the dose required for depression of spontaneous locomotor activity. The depression of locomotor activity and the hypotensive effect of both analogues were antagonized by parenteral injections of caffeine. These results show that the hypoactive and hypotensive effects of adenosine analogues can be dissociated and that methylxanthines probably exert an antagonism of central adenosine receptors in the rat.