Permeability of NS-3, a Thyrotropin-releasing Hormone Analogue,into the Brain After Its Systemic Administration in Rats: A Microdialysis Study

The concentration of NS-3 (montirelin hydrate, CG 3703), a thyrotropin-releasing hormone (TRH) analogue, in the cerebral cortex of urethane-anaesthetized rats was measured after its systemic administration (1 mgkg^?1, i.v.), using in-vivo microdialysis coupled with a radioimmunoassay. The concentration in microdialysates was highest (24nM) during the first 20 min after injection, and it fell below the detection limit (3.5 nM) 100 min after treatment. The maximal interstitial concentration was estimated to be 0.51 μM. From these results, it is suggested that NS-3 can readily penetrate into the brain.