[Comparative pharmacophore analysis of dual dopamine D2/5-HT(2A) receptor antagonists].
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.
Guo
Yan-shen
YS
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Guo
Zong-ru
ZR
D058668:Adrenergic alpha-1 Receptor Antagonists; D065127:Dopamine D2 Receptor Antagonists; D016503:Drug Delivery Systems; D015195:Drug Design; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors / Q000737:chemistry; D008968:Molecular Conformation; D015394:Molecular Structure; D044402:Receptor, Serotonin, 5-HT2A / Q000737:chemistry; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry; D017448:Receptors, Dopamine D2 / Q000737:chemistry; D058830:Serotonin 5-HT2 Receptor Antagonists; D013329:Structure-Activity Relationship
D058668:Adrenergic alpha-1 Receptor Antagonists; D065127:Dopamine D2 Receptor Antagonists; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; D044402:Receptor, Serotonin, 5-HT2A; D018340:Receptors, Adrenergic, alpha-1; D017448:Receptors, Dopamine D2; D058830:Serotonin 5-HT2 Receptor Antagonists