Differential blockade by (?)mianserin of the alpha2-adrenoceptors mediating inhibition of noradrenaline and serotonin release from rat brain synaptosomes

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Abstract
Mianserin and its two enantiomers were studied as antagonists of the alpha2-adrenoceptors mediating inhibition of noradrenaline and 5-hydroxytryptamine release in rat brain cortex. The inhibitory effect of exogenous noradrenaline on the release of 3H-noradrenaline evoked by 15 mM KCl from superfused cortical synaptosomes was antagonized by racemic mianserin and by (+)mianserin; the (−)enatiomer was ineffective. In contrast, both (+)mianserin and (−)mianserin antagonized the inhibitory effect of noradrenaline on the release of 3H-5-hydroxytryptamine. The results suggest that the alpha2-autoreceptors on noradrenergic nerve endings differ from the alpha2-adrenoceptors located on serotoninergic terminals.

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