Tetrahydroaminoacridine affects the cholinergic function of blood-brain barrier

In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. THA resulted to be a more potent inhibitor of BuChE than AChE. Lineweaver-Burk plots showed that Km (...

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Veröffentlicht in:	Life sciences (1973) 1993, Vol.53 (14), p.1165-1172
Hauptverfasser:	Catalán, R.E., Martínez, A.M., Aragonés, M.D., Miguel, B.G., Hernández, F., Cruz, E.
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - drug effects Animals Biological and medical sciences Blood-Brain Barrier - drug effects Butyrylcholinesterase - drug effects Cerebral circulation. Blood-brain barrier. Choroid plexus. Cerebrospinal fluid. Circumventricular organ. Meninges Dose-Response Relationship, Drug Fundamental and applied biological sciences. Psychology In Vitro Techniques Microcirculation - enzymology Rats Tacrine - pharmacology Time Factors Vertebrates: nervous system and sense organs
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Zusammenfassung:	In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. THA resulted to be a more potent inhibitor of BuChE than AChE. Lineweaver-Burk plots showed that Km (app) and V were altered by THA, indicating mixed competitive/non-competitite inhivition. The results of the present study also established that the three molecular forms of BuChE (G 1, G 2 and G 4), recently described to be present in brain microvessels, are inhibited after THA treatment.
ISSN:	0024-3205 1879-0631
DOI:	10.1016/0024-3205(93)90553-F