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

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.

@article{ca4124bac7ed49808ed41964218bb0b4,

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.",

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

author = "Marco Gobbi and Emanuela Frittoli and Tiziana Mennini",

year = "1990",

month = "5",

day = "3",

doi = "10.1016/0014-2999(90)90608-9",

language = "English",

volume = "180",

pages = "183--186",

journal = "European Journal of Pharmacology",

issn = "0014-2999",

publisher = "Elsevier",

number = "1",

}

TY - JOUR

T1 - Antagonist properties of 1-(2-pyrimidinyl) piperazine at presynaptic α2-adrenoceptors in the rat brain

AU - Gobbi, Marco

AU - Frittoli, Emanuela

AU - Mennini, Tiziana

PY - 1990/5/3

Y1 - 1990/5/3

N2 - 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.

AB - 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.

KW - PmP (1-(2-pyrimidinyl)piperazine)

KW - Synaptosomes

KW - [H]5-HT release

KW - α-Adrenoceptors

UR - http://www.scopus.com/inward/record.url?scp=0025268302&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0025268302&partnerID=8YFLogxK

U2 - 10.1016/0014-2999(90)90608-9

DO - 10.1016/0014-2999(90)90608-9

M3 - Article

C2 - 1973112

AN - SCOPUS:0025268302

VL - 180

SP - 183

EP - 186

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 1

ER -

Access to Document

10.1016/0014-2999(90)90608-9