Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain

Marco Gobbi; Emanuela Frittoli; Tiziana Mennini

doi:10.1016/0014-2999(90)90608-9

Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain

Marco Gobbi, Emanuela Frittoli, Tiziana Mennini

Istituto di Ricerche Farmacologiche "Mario Negri"

Research output: Contribution to journal › Article › peer-review

Abstract

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 α₂-adrenoceptors located on noradrenergic and serotonergic nerve terminals, respectively.

Original language	English
Pages (from-to)	183-186
Number of pages	4
Journal	European Journal of Pharmacology
Volume	180
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(90)90608-9
Publication status	Published - May 3 1990

Keywords

PmP (1-(2-pyrimidinyl)piperazine)
Synaptosomes
[H]5-HT release
α-Adrenoceptors

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

Access to Document

10.1016/0014-2999(90)90608-9

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title = "Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain",

abstract = "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 α2-adrenoceptors located on noradrenergic and serotonergic nerve terminals, respectively.",

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