Brain distribution and muscarinic receptor occupancy of an active metabolite of fesoterodine in rats
Year: 2024
Type: article
Abstract: values and muscarinic receptor affinity retrieved from literature, revealed a significant correlation between the calculated and measured values. These results indicate that 5-HMT has low brain distribution and muscarinic receptor occupancy, which might be the reasons for the insignificant effect of fesoterodine on cognitive function. SIGNIFICANCE STATEMENT: This study reports that 5-hydroxymethyl tolterodine, the active metabolite of fesoterodine, has much lower brain distribution and muscarinic receptor occupancy compared with oxybutynin and trihexyphenidyl based on brain microdialysis and in vivo receptor-binding analysis with unlabeled muscarinic tracer in rats. The low brain distribution and muscarinic receptor occupancy of 5-hydroxymethyl tolterodine might be the reasons for the insignificant effect of fesoterodine on cognitive function.
Authors: Mizuki Shiho, Shimako Tanaka, Eriko Nakatani, Toshiki Kurosawa, Yoshiyuki Kubo, Yoshiharu Deguchi, Takashi Okura
Institution: Teikyo University
Language: English
Subfield: Urology
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $3,750
OpenAlex ID: W4405175535