研究目的
To develop a selective high-affinity antagonist for the dopamine D3 receptor (D3R) for treating substance use disorders and to evaluate its potential as a PET radioligand for imaging D3R in vivo.
研究成果
[11C]BAK4-51 was successfully synthesized and evaluated as a PET radioligand for D3R imaging. However, its avid substrate behavior for brain efflux transporters and lack of D3R-specific signal in vivo indicate its ineffectiveness for PET imaging of brain D3 receptors in rodents and monkeys. Future research should focus on developing radioligands with higher D3R affinity and selectivity, and minimal interaction with efflux transporters.
研究不足
The study found that [11C]BAK4-51 is an avid substrate for brain efflux transporters, which limits its utility as a PET radioligand for D3R imaging. The lack of D3R-specific signal in vivo suggests the need for radioligands with higher D3R affinity and selectivity, and possibly reduced interaction with efflux transporters.
