Biochemical and behavioral effects of PDE10A inhibitors: Relationship to target site occupancy
详细信息 查看全文
- 作者：Yu-Wen Lia ; yu-wen.li@bms.com" class="auth_mail" title="E-mail the corresponding author ; Matthew A. Seagera ; Trevor Wojcika ; Karen Hemana ; Thaddeus F. Molskia ; Alda Fernandesa ; Shaun Langdona ; Annapurna Pendrib ; Samuel Gerritzb ; Yuan Tianc ; Yang Hongc ; Lizbeth Gallagherd ; James R. Merritte ; 1 ; Chongwu Zhange ; Ryan Westphala ; 2 ; Robert Zaczeka ; 3 ; John E. Macorb ; Joanne J. Bronsonb ; Nicholas J. Lodgea
- 关键词：PDE10A ; Antipsychotic ; Conditioned avoidance response ; Catalepsy ; Radioligand ; Occupancy
- 刊名：Neuropharmacology
- 出版年：2016
- 出版时间：March 2016
- 年：2016
- 卷：102
- 期：Complete
- 页码：121-135
- 全文大小：3757 K
文摘
- •
[3H]BMS-843496, a potent and selective PDE10A radioligand, was characterized.
- •
Radioligand binding was highest in striatum, subthalamic n. and substantia nigra.
- •
PDE10A occupancy correlated with striatal pCREB expression.
- •
≥40% PDE10A occupancy was required to achieve antipsychotic-like effects.
- •
Cataleptic effects of PDE10A inhibitors were not consistently related to occupancy.