Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
Asenapine is a novel psychopharmacologic agent under development for the treatment of schizophrenia and bipolar disorder. We determined and compared the human receptor binding affinities and functional characteristics of asenapine and several antipsychotic drugs. Compounds were tested under comparable assay conditions using cloned human receptors. In comparison with the antipsychotics, ... asenapine showed high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [8.9], alpha2A [8.9], alpha2B [9.5] and alpha2C [8.9]), dopamine receptors (D1 [8.9], D2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2]). It had much lower affinity (pKi
Mesh Terms:
Benzodiazepines, Bipolar Disorder, Clinical Trials as Topic, Cloning, Molecular, Clozapine, Heterocyclic Compounds with 4 or More Rings, Histamine Release, Humans, Inhibitory Concentration 50, Molecular Structure, Psychotropic Drugs, Radioligand Assay, Receptors, Adrenergic, Receptors, Dopamine, Receptors, Dopamine D2, Receptors, Muscarinic, Receptors, Serotonin, Schizophrenia, Substrate Specificity
Benzodiazepines, Bipolar Disorder, Clinical Trials as Topic, Cloning, Molecular, Clozapine, Heterocyclic Compounds with 4 or More Rings, Histamine Release, Humans, Inhibitory Concentration 50, Molecular Structure, Psychotropic Drugs, Radioligand Assay, Receptors, Adrenergic, Receptors, Dopamine, Receptors, Dopamine D2, Receptors, Muscarinic, Receptors, Serotonin, Schizophrenia, Substrate Specificity
J. Psychopharmacol. (Oxford)
Date: Jan. 01, 2009
PubMed ID: 18308814
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