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The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates
journal contributionposted on 2023-06-08, 12:31 authored by John R Atack, Wai-Si Eng, Ray E Gibson, Christine Ryan, Barbara Francis, Bindi Sohal, Gerard R Dawson, Richard J Hargreaves, H Donald Burns
Rat plasma EC(50) values did not vary as a function of time indicating that alpha5IA dissociates readily for the GABA(A) receptor in vivo. These data also suggest that despite the different assays used (terminal assays of [(3)H]flumazenil in vivo binding in rats and [(123)I]iomazenil gamma-scintigraphy in anaesthetized rhesus monkeys), these techniques produced similar plasma alpha5IA EC(50) values (52 and 57 ngxmL(-1) respectively) and that the plasma-occupancy relationship for alpha5IA translates across these two species.
JournalBritish Journal of Pharmacology
Department affiliated with
- Biochemistry Publications
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