Different effects of intracerebral and systemic administration of buspirone in the forced swimming test

Involvement of a metabolite

Luigi Cervo, Giuliano Grignaschi, Rosario Samanin

Research output: Contribution to journalArticle

54 Citations (Scopus)

Abstract

Buspirone, a drug with high affinity for serotonin1A receptors, was studied for its ability to reduce rats' immobility in the forced swimming test when injected systematically or into the nucleus raphe dorsalis (DR). Between 0.1 and 10 mg/kg buspirone had no effect on rats' immobility when injected systemically as a single dose or as a 3-injection course during 24 hours. Direct injection of 1 and 5 ug/0.5 μl buspirone in the DR significantly reduced the duration of immobility without changing rats' activity in an open field. The anti-immobility effect of 1 μg/0.5 μl buspirone in the DR was completely prevented by injecting 2.5 μg (-)-propranolol in the same area. Oral administration of 0.3-1.0 mg/kg 1-(2-pyrimidinyl)piperazine (1-PP), one of the main metabolites of buspirone, and 0.3-3.0 mg/kg s.c. idazoxan, two substances with alpha2 adrenergic blocking properties, completely antagonized the effect of 0.25 mg/kg s.c. 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), an agent with selective affinity for serotonin1A receptors. The anti-immobility effect of an infusion of 1 μg/0.5 μl buspirone or 8-OH-DPAT in the DR was also antagonized by 1 mg/kg p.o. 1-PP. The results suggest that buspirone possesses potential antidepressant properties but its effect may be masked in certain tests by its metabolite, 1PP, through its alpha2 adrenergic blocking activity.

Original languageEnglish
Pages (from-to)2095-2102
Number of pages8
JournalLife Sciences
Volume43
Issue number25
DOIs
Publication statusPublished - 1988

Fingerprint

Buspirone
Metabolites
8-Hydroxy-2-(di-n-propylamino)tetralin
Rats
Adrenergic Agents
Idazoxan
Injections
Direct injection
Swimming
Propranolol
Antidepressive Agents
Oral Administration
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology

Cite this

Different effects of intracerebral and systemic administration of buspirone in the forced swimming test : Involvement of a metabolite. / Cervo, Luigi; Grignaschi, Giuliano; Samanin, Rosario.

In: Life Sciences, Vol. 43, No. 25, 1988, p. 2095-2102.

Research output: Contribution to journalArticle

@article{c12061da5c1e48cdbb27f09d409c31c9,
title = "Different effects of intracerebral and systemic administration of buspirone in the forced swimming test: Involvement of a metabolite",
abstract = "Buspirone, a drug with high affinity for serotonin1A receptors, was studied for its ability to reduce rats' immobility in the forced swimming test when injected systematically or into the nucleus raphe dorsalis (DR). Between 0.1 and 10 mg/kg buspirone had no effect on rats' immobility when injected systemically as a single dose or as a 3-injection course during 24 hours. Direct injection of 1 and 5 ug/0.5 μl buspirone in the DR significantly reduced the duration of immobility without changing rats' activity in an open field. The anti-immobility effect of 1 μg/0.5 μl buspirone in the DR was completely prevented by injecting 2.5 μg (-)-propranolol in the same area. Oral administration of 0.3-1.0 mg/kg 1-(2-pyrimidinyl)piperazine (1-PP), one of the main metabolites of buspirone, and 0.3-3.0 mg/kg s.c. idazoxan, two substances with alpha2 adrenergic blocking properties, completely antagonized the effect of 0.25 mg/kg s.c. 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), an agent with selective affinity for serotonin1A receptors. The anti-immobility effect of an infusion of 1 μg/0.5 μl buspirone or 8-OH-DPAT in the DR was also antagonized by 1 mg/kg p.o. 1-PP. The results suggest that buspirone possesses potential antidepressant properties but its effect may be masked in certain tests by its metabolite, 1PP, through its alpha2 adrenergic blocking activity.",
author = "Luigi Cervo and Giuliano Grignaschi and Rosario Samanin",
year = "1988",
doi = "10.1016/0024-3205(88)90359-1",
language = "English",
volume = "43",
pages = "2095--2102",
journal = "Life Sciences",
issn = "0024-3205",
publisher = "Elsevier Inc.",
number = "25",

}

TY - JOUR

T1 - Different effects of intracerebral and systemic administration of buspirone in the forced swimming test

T2 - Involvement of a metabolite

AU - Cervo, Luigi

AU - Grignaschi, Giuliano

AU - Samanin, Rosario

PY - 1988

Y1 - 1988

N2 - Buspirone, a drug with high affinity for serotonin1A receptors, was studied for its ability to reduce rats' immobility in the forced swimming test when injected systematically or into the nucleus raphe dorsalis (DR). Between 0.1 and 10 mg/kg buspirone had no effect on rats' immobility when injected systemically as a single dose or as a 3-injection course during 24 hours. Direct injection of 1 and 5 ug/0.5 μl buspirone in the DR significantly reduced the duration of immobility without changing rats' activity in an open field. The anti-immobility effect of 1 μg/0.5 μl buspirone in the DR was completely prevented by injecting 2.5 μg (-)-propranolol in the same area. Oral administration of 0.3-1.0 mg/kg 1-(2-pyrimidinyl)piperazine (1-PP), one of the main metabolites of buspirone, and 0.3-3.0 mg/kg s.c. idazoxan, two substances with alpha2 adrenergic blocking properties, completely antagonized the effect of 0.25 mg/kg s.c. 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), an agent with selective affinity for serotonin1A receptors. The anti-immobility effect of an infusion of 1 μg/0.5 μl buspirone or 8-OH-DPAT in the DR was also antagonized by 1 mg/kg p.o. 1-PP. The results suggest that buspirone possesses potential antidepressant properties but its effect may be masked in certain tests by its metabolite, 1PP, through its alpha2 adrenergic blocking activity.

AB - Buspirone, a drug with high affinity for serotonin1A receptors, was studied for its ability to reduce rats' immobility in the forced swimming test when injected systematically or into the nucleus raphe dorsalis (DR). Between 0.1 and 10 mg/kg buspirone had no effect on rats' immobility when injected systemically as a single dose or as a 3-injection course during 24 hours. Direct injection of 1 and 5 ug/0.5 μl buspirone in the DR significantly reduced the duration of immobility without changing rats' activity in an open field. The anti-immobility effect of 1 μg/0.5 μl buspirone in the DR was completely prevented by injecting 2.5 μg (-)-propranolol in the same area. Oral administration of 0.3-1.0 mg/kg 1-(2-pyrimidinyl)piperazine (1-PP), one of the main metabolites of buspirone, and 0.3-3.0 mg/kg s.c. idazoxan, two substances with alpha2 adrenergic blocking properties, completely antagonized the effect of 0.25 mg/kg s.c. 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), an agent with selective affinity for serotonin1A receptors. The anti-immobility effect of an infusion of 1 μg/0.5 μl buspirone or 8-OH-DPAT in the DR was also antagonized by 1 mg/kg p.o. 1-PP. The results suggest that buspirone possesses potential antidepressant properties but its effect may be masked in certain tests by its metabolite, 1PP, through its alpha2 adrenergic blocking activity.

UR - http://www.scopus.com/inward/record.url?scp=0024204356&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0024204356&partnerID=8YFLogxK

U2 - 10.1016/0024-3205(88)90359-1

DO - 10.1016/0024-3205(88)90359-1

M3 - Article

VL - 43

SP - 2095

EP - 2102

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

IS - 25

ER -