Aripiprazole acts as a selective dopamine D2 receptor partial agonist

被引：60

作者：

Wood, Martyn ^{[1
]}

Reavill, Charlie ^{[1
]}

机构：

[1] GlaxoSmithKline Schizophrenia & Bipolar Neurophys, Psychiat CEDD, Harlow CM19 5AW, Essex, England

来源：

EXPERT OPINION ON INVESTIGATIONAL DRUGS | 2007年 / 16卷 / 06期

关键词：

D O I：

10.1517/13543784.16.6.771

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Aripiprazole has made a significant contribution to the treatment of schizophrenia and related disorders with an improved safety and tolerability profile, which has been attributed to its unique pharmacological profile. It has been claimed that partial agonism of the dopamine D-2 and 5-HT1A receptors and antagonism of the 5-HT2 receptor contribute to the clinical profile of aripiprazole, a so-called dopamine- and 5-HT stabiliser. However, recent studies have questioned the role of the 5-HT-mediated systems in the mechanism of action of aripiprazole. This report reviews published and unpublished data that suggest that aripiprazole acts as a selective partial agonist at the dopamine D, receptor and does not affect 5-HT receptors at therapeutic doses.

引用

页码：771 / 775

页数：5

共 50 条

[31] Discovery of a true bivalent dopamine D2 receptor agonist
Qian, Mingcheng
Ricarte, Adrian
Wouters, Elise
Dalton, James A. R.
Risseeuw, Martijn D. P.
Giraldo, Jesus
Van Calenbergh, Serge
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 212
[32] VANADATE INHIBITS AGONIST BINDING TO D2 DOPAMINE RECEPTOR
ELAZAR, Z
FUCHS, S
[J]. JOURNAL OF MOLECULAR NEUROSCIENCE, 1991, 3 (01) : 1 - 6
[33] TERGURIDE, A DOPAMINE D2 PARTIAL AGONIST, AS A DISCRIMINATIVE STIMULUS IN RATS
YAMAGUCHI, M
KIMURAIWASAKI, K
AKAI, T
NAKADA, Y
NAKAGAWA, H
[J]. BEHAVIOURAL PHARMACOLOGY, 1991, 2 (03): : 233 - 240
[34] STATE-DEPENDENT EFFECTS OF D2 PARTIAL AGONIST ARIPIPRAZOLE ON DOPAMINE NEURON ACTIVITY IN THE MAM NEURODEVELOPMENTAL MODEL OF SCHIZOPHRENIA
Sonnenschein, Susan
Gill, Kathryn
Grace, Anthony
[J]. SCHIZOPHRENIA BULLETIN, 2018, 44 : S338 - S338
[35] State-dependent effects of the D2 partial agonist aripiprazole on dopamine neuron activity in the MAM neurodevelopmental model of schizophrenia
Sonnenschein, Susan F.
Gill, Kathryn M.
Grace, Anthony A.
[J]. NEUROPSYCHOPHARMACOLOGY, 2019, 44 (03) : 572 - 580
[36] State-dependent effects of the D2 partial agonist aripiprazole on dopamine neuron activity in the MAM neurodevelopmental model of schizophrenia
Susan F. Sonnenschein
Kathryn M. Gill
Anthony A. Grace
[J]. Neuropsychopharmacology, 2019, 44 : 572 - 580
[37] BREXPIPRAZOLE: A NEW DOPAMINE D2 RECEPTOR PARTIAL AGONIST FOR THE TREATMENT OF SCHIZOPHRENIA AND MAJOR DEPRESSIVE DISORDER
Citrome, L.
[J]. DRUGS OF TODAY, 2015, 51 (07) : 397 - 414
[38] Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors?
D. M. Jackson
Hakån Wikström
Y. Liao
[J]. Psychopharmacology, 1998, 138 : 213 - 214
[39] Modeling of Dopamine D2 Receptor and its Agonist DOCK Analyses
朱七庆
郭宗儒
[J]. Journal of Chinese Pharmaceutical Sciences, 1998, (03) : 3 - 8
[40] Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors?
Jackson, DM
Wikström, H
Liao, Y
[J]. PSYCHOPHARMACOLOGY, 1998, 138 (02) : 213 - 214

← 1 2 3 4 5 →