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Iloperidone binding to human and rat dopamine and 5-HT receptors.

Abstract：

:Iloperidone (HP 873; 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy] -3- methoxyphenyl]ethanone) is a compound currently in clinical trials for the treatment of schizophrenia. Iloperidone displays affinity for dopamine D2 receptors and for 5-HT2A receptors and has a variety of in vivo activities suggestive of an atypical antipsychotic. Here we present an examination of the affinity of iloperidone to a variety of human and rat homologs of dopamine and 5-HT receptor subtypes. We employed receptor binding assays using membranes from cells stably expressing human dopamine D1, D2S, D2L, D3, D4 and D5 and 5-HT2A and 5-HT2C receptors and rat 5-HT6 and 5-HT7 receptors. Iloperidone displayed higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displayed high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively), and was found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). The potential implications of this receptor binding profile are discussed in comparison with data for other antipsychotic compounds.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Kongsamut S,Roehr JE,Cai J,Hartman HB,Weissensee P,Kerman LL,Tang L,Sandrasagra A

doi

10.1016/s0014-2999(96)00840-0

subject

Has Abstract

pub_date

1996-12-19 00:00:00

pages

417-23

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(96)00840-0

journal_volume

317

pub_type

杂志文章

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