Iloperidone binding to human and rat dopamine and 5-HT receptors.
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Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A
Iloperidone binding to human and rat dopamine and 5-HT receptors.
Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23.
- PubMed ID
- 8997630 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Iloperidone 5-hydroxytryptamine receptor 2A Protein Humans YesAntagonistDetails Iloperidone Dopamine D2 receptor Protein Humans YesAntagonistDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Clozapine 5-hydroxytryptamine receptor 2C Ki (nM) 10.7 N/A N/A Details Clozapine Dopamine D1 receptor Ki (nM) 196 N/A N/A Details Haloperidol 5-hydroxytryptamine receptor 2A Ki (nM) 186 N/A N/A Details Haloperidol Dopamine D1 receptor Ki (nM) 82 N/A N/A Details Iloperidone 5-hydroxytryptamine receptor 2A Ki (nM) 5.6 N/A N/A Details Iloperidone Dopamine D1 receptor Ki (nM) 216 N/A N/A Details Olanzapine 5-hydroxytryptamine receptor 2A Ki (nM) 24.2 N/A N/A Details Olanzapine 5-hydroxytryptamine receptor 2C Ki (nM) 6.4 N/A N/A Details Olanzapine Dopamine D1 receptor Ki (nM) 35 N/A N/A Details Olanzapine Dopamine D5 receptor Ki (nM) 74 N/A N/A Details Quetiapine 5-hydroxytryptamine receptor 2A Ki (nM) 636 N/A N/A Details Quetiapine 5-hydroxytryptamine receptor 2C Ki (nM) 1184 N/A N/A Details Quetiapine Dopamine D1 receptor Ki (nM) 1277 N/A N/A Details Quetiapine Dopamine D5 receptor Ki (nM) 1513 N/A N/A Details