Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT2A receptor antagonists/inverse agonists
- Resource Type
- ACADEMIC JOURNAL
- Authors
- Ma, Mingxu a, 1; Yang, Yifei a, 1; Du, Guangying a; Dai, Yusen b; Zhu, Xiaoyin a; Wang, Wenyan a; Xu, Hengwei b; Zhang, Jianzhao a; Zheng, Lixia a; Zou, Fangxia a; Yang, Huijie b; Liu, Bin a; Liu, Wanhui a, b; Ye, Liang c, ∗∗; Zhang, Rui b, ∗∗∗; Tian, Jingwei a, ∗
- Source
- In European Journal of Medicinal Chemistry 15 April 2022 234
- Subject
- Language
- English
- ISSN
- 0223-5234
- E-ISSN
- DOI
- 10.1016/j.ejmech.2022.114246
@@@@Highlights •A novel class of 5-HT2A receptor antagonists/inverse agonists were designed and synthesized.•The effects on 5-HT2A receptor antagonists/inverse agonists of all compounds were evaluated.•7–16 exhibited 50-fold higher 5-HT2A antagonist and 23-fold higher inverse agonist activities than pimavanserin.•In vivo functional activity showed that compound 7–16 attenuated DOI-induced head twitches in rats.