Abstract
Dual dopamine D2/5-HT2A receptor antagonists have potent activity and are referred to atypical antipsychotics due to their lower propensity to elicit EPS and their moderate efficacy toward negative symptoms. However, an on-going challenge in developing atypical antipsychotics drugs is to maintain the favorable profiles and avoid of cardiovascular risk. In this paper, comparative pharmacophore analysis of dual dopamine D2/5-HT2A receptor antagonists, hERG K+ channel blockers, and alA adrenoceptor antagonists is carried out, and the results could give some insight into multi-target drug design.
MeSH terms
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Adrenergic alpha-1 Receptor Antagonists
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Dopamine D2 Receptor Antagonists*
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Drug Delivery Systems*
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Drug Design*
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
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Ether-A-Go-Go Potassium Channels / chemistry
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Molecular Conformation
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Molecular Structure
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Receptor, Serotonin, 5-HT2A / chemistry
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Receptors, Adrenergic, alpha-1 / chemistry
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Receptors, Dopamine D2 / chemistry
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Serotonin 5-HT2 Receptor Antagonists*
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Structure-Activity Relationship
Substances
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Adrenergic alpha-1 Receptor Antagonists
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Dopamine D2 Receptor Antagonists
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Receptor, Serotonin, 5-HT2A
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Receptors, Adrenergic, alpha-1
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Receptors, Dopamine D2
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Serotonin 5-HT2 Receptor Antagonists