Comparative pharmacophore analysis of dual dopamine D2/5-HT(2A) receptor antagonists.
- Author:
Yan-shen GUO
1
;
Zong-ru GUO
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Adrenergic alpha-1 Receptor Antagonists;
Dopamine D2 Receptor Antagonists;
Drug Delivery Systems;
Drug Design;
ERG1 Potassium Channel;
Ether-A-Go-Go Potassium Channels;
antagonists & inhibitors;
chemistry;
Molecular Conformation;
Molecular Structure;
Receptor, Serotonin, 5-HT2A;
chemistry;
Receptors, Adrenergic, alpha-1;
chemistry;
Receptors, Dopamine D2;
chemistry;
Serotonin 5-HT2 Receptor Antagonists;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2009;44(3):314-320
- CountryChina
- Language:Chinese
-
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.
