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

31 Citations (Scopus)

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

Fingerprint

Adrenergic Receptors

Norepinephrine

Brain

Buspirone

Synaptosomes

Cerebral Cortex

Serotonin

1-(2-pyrimidinyl)piperazine

Keywords

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

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

Cite this

Gobbi, M., Frittoli, E., & Mennini, T. (1990). Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain. European Journal of Pharmacology, 180(1), 183-186. https://doi.org/10.1016/0014-2999(90)90608-9

Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain. / Gobbi, Marco; Frittoli, Emanuela; Mennini, Tiziana.

In: European Journal of Pharmacology, Vol. 180, No. 1, 03.05.1990, p. 183-186.

Research output: Contribution to journal › Article

Gobbi, M, Frittoli, E & Mennini, T 1990, 'Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain', European Journal of Pharmacology, vol. 180, no. 1, pp. 183-186. https://doi.org/10.1016/0014-2999(90)90608-9

Gobbi M, Frittoli E, Mennini T. Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain. European Journal of Pharmacology. 1990 May 3;180(1):183-186. https://doi.org/10.1016/0014-2999(90)90608-9

Gobbi, Marco ; Frittoli, Emanuela ; Mennini, Tiziana. / Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain. In: European Journal of Pharmacology. 1990 ; Vol. 180, No. 1. pp. 183-186.

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