Regulation of noradrenaline release in human cerebral arteries via presynaptic alpha 2-adrenoceptors.

1. Electrical stimulation induced tritium release from branches of human middle cerebral arteries preincubated with [3H]noradrenaline (NA), which was reduced by the alpha 2-adrenoceptor agonists, clonidine and B-HT 920, and not affected by the alpha 1-agonist, methoxamine. 2. The stimulated tritium release was inhibited by yohimbine (alpha 2-antagonist), and increased by phentolamine (alpha-antagonist) and prazosin (alpha 1-antagonist). 3. The inhibitory effect of clonidine was antagonized by yohimbine. 4. NA uptake was markedly reduced when the interval between the death and the autopsy was greater than 5 hr. 5. These data indicates the existence of presynaptic inhibitory alpha 2-adrenoceptors, but not alpha 1, in human cerebral arteries, and that the adrenergic nerve endings start to degenerate from 5 hr after death.