You need JavaScript to view this

Sulpiride and the role of dopaminergic receptor blockade in the antipsychotic activity of neuroleptics

Journal Article:

Abstract

It is now generally recognized that dopamine receptors excist in the CNS as different subtypes: D/sub 1/ receptors, associated with adenylyl cyclase activity, and D/sub 2/ receptor, uncoupled to a cyclic AMP generating system. In order to understand the role of D/sub 1/ and D/sub 2/ receptors in the antipsychotic action of neuroleptics, we have performed subchronic treatment with haloperidol, a drug which acts on D/sub 1/ receptors, and sulpiride, a selective antagonist to D/sub 2/ receptors. Long-term treatment with haloperidol does not induce significant supersensitivity of the D/sub 2/ receptors. In fact under these conditions /sup 3/H-(-)-sulpiride binding, which is a marker of D/sub 2/ receptor function, does not increase in rat striatum, while the long-term administration of sulpiride, itself produces supersensitivity of D/sub 2/ receptors. Moreover, sulpiride does not induce supersensitivity of the D/sub 1/ receptors, characterized by /sup 3/H-spiroperidol binding. These data suggest that both types of dopamine receptors may be involved in the clinical antipsychotic effects of neuroleptics. Unilateral leison of the nigrostriatal dopaminergic pathway produces an increase of striatal dopaminergic receptors, measured either by /sup 3/H-spiroperidol and /sup 3/H-(-)-sulpiride binding. These findings suggest that D/sub 1/ and D/sub 2/ receptors are present in postsynaptic membranes  More>>
Authors:
Memo, M; Battaini, F; Spano, P F; Trabucchi, M [1] 
  1. University of Brescia, (Italy). Dept. of Pharmacology
Publication Date:
Jan 01, 1981
Product Type:
Journal Article
Reference Number:
AIX-12-621951; EDB-82-005088
Resource Relation:
Journal Name: Acta Psychiat. Scand.; (Denmark); Journal Volume: 63:4
Subject:
59 BASIC BIOLOGICAL SCIENCES; PSYCHOTROPIC DRUGS; BIOCHEMICAL REACTION KINETICS; ADENYLIC ACID; AMP; MENTAL DISORDERS; TRITIUM COMPOUNDS; CENTRAL NERVOUS SYSTEM AGENTS; DRUGS; KINETICS; LABELLED COMPOUNDS; NUCLEOTIDES; ORGANIC COMPOUNDS; REACTION KINETICS; 551001* - Physiological Systems- Tracer Techniques
OSTI ID:
6119750
Country of Origin:
Denmark
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: APYSA
Submitting Site:
INIS
Size:
Pages: 314-324
Announcement Date:

Journal Article:

Citation Formats

Memo, M, Battaini, F, Spano, P F, and Trabucchi, M. Sulpiride and the role of dopaminergic receptor blockade in the antipsychotic activity of neuroleptics. Denmark: N. p., 1981. Web.
Memo, M, Battaini, F, Spano, P F, & Trabucchi, M. Sulpiride and the role of dopaminergic receptor blockade in the antipsychotic activity of neuroleptics. Denmark.
Memo, M, Battaini, F, Spano, P F, and Trabucchi, M. 1981. "Sulpiride and the role of dopaminergic receptor blockade in the antipsychotic activity of neuroleptics." Denmark.
@misc{etde_6119750,
title = {Sulpiride and the role of dopaminergic receptor blockade in the antipsychotic activity of neuroleptics}
author = {Memo, M, Battaini, F, Spano, P F, and Trabucchi, M}
abstractNote = {It is now generally recognized that dopamine receptors excist in the CNS as different subtypes: D/sub 1/ receptors, associated with adenylyl cyclase activity, and D/sub 2/ receptor, uncoupled to a cyclic AMP generating system. In order to understand the role of D/sub 1/ and D/sub 2/ receptors in the antipsychotic action of neuroleptics, we have performed subchronic treatment with haloperidol, a drug which acts on D/sub 1/ receptors, and sulpiride, a selective antagonist to D/sub 2/ receptors. Long-term treatment with haloperidol does not induce significant supersensitivity of the D/sub 2/ receptors. In fact under these conditions /sup 3/H-(-)-sulpiride binding, which is a marker of D/sub 2/ receptor function, does not increase in rat striatum, while the long-term administration of sulpiride, itself produces supersensitivity of D/sub 2/ receptors. Moreover, sulpiride does not induce supersensitivity of the D/sub 1/ receptors, characterized by /sup 3/H-spiroperidol binding. These data suggest that both types of dopamine receptors may be involved in the clinical antipsychotic effects of neuroleptics. Unilateral leison of the nigrostriatal dopaminergic pathway produces an increase of striatal dopaminergic receptors, measured either by /sup 3/H-spiroperidol and /sup 3/H-(-)-sulpiride binding. These findings suggest that D/sub 1/ and D/sub 2/ receptors are present in postsynaptic membranes while it is still not known whether they exist in the same cellular elements.}
journal = {Acta Psychiat. Scand.; (Denmark)}
volume = {63:4}
journal type = {AC}
place = {Denmark}
year = {1981}
month = {Jan}
}