신규개발된 중추성 근이완제 2-methyl-3-aminopropiophenone 유도체의 혈액 : 뇌관문 투과기구

Abstract

The [(4'-Ethly-2-methyl-3-pyrrolidino)propiophenone HCI derivative (HY-770) of 2-methyl-3-aminopropiophenone (MP) has been developed as central muscle relaxants and is readly transported through the central nervous system. The unidirectional extraction for HY-770 was measured by the brain uptake index method in adult male Wistar rats under ketamin-xylazine anesthesia. The brain extraction of HY770 was ver high, almost 100%. The coinjection of [^14C]HY-770 and unlabelled HY-770 resulted in a dose-dependent inhibition of HY-770 transport through the blood-brain barrier(BBB) and saturation in 50mM HY-770. Therefore, it is indicated that BBB transport of HY-770 is mediated by a low-affifinity, high capacity saturable transport system. BBB permeability of HY-770 was significantly inhibited by MP derivatives, e.g., tolperisone, eperisone and eprazinone. Basic lipophilic drugs such as lidocaine and propranolol significantly inhibited the BBB transport of HY-770.