Antagonist properties of 1-(2-pyrimidinyl)piperazine at presynaptic alpha 2-adrenoceptors in the rat brain.
The effect of 1-(2-pyrimidinyl)piperazine (PmP), the main metabolite of buspirone, was tested on K(+)-evoked [3H]noradrenaline and [3H]serotonin release from superfused synaptosomes obtained from rat cerebral cortex. PmP had no effects per se, but antagonized the effect of noradrenaline, producing a parallel shift to the right of the noradrenaline inhibition curves. From these data pA2 (apparent affinity) values of 6.8 and 7.3 were calculated for PmP on presynaptic alpha 2-adrenoceptors located on noradrenergic and serotonergic nerve terminals, respectively.
Gobbi
M
M
Istituto di Ricerche Farmacologiche, Mario Negri, Milano, Italy.
Frittoli
E
E
Mennini
T
T
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D002065:Buspirone / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009411:Nerve Endings / Q000187:drug effects; D009638:Norepinephrine / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology; D011188:Potassium / Q000494:pharmacology; D051381:Rats; D012701:Serotonin / Q000378:metabolism / Q000502:physiology; D013569:Synapses / Q000187:drug effects; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D012701:Serotonin; C037921:1-(2-pyrimidinyl)piperazine; D011188:Potassium; D002065:Buspirone; D009638:Norepinephrine