Cheng_1998_Pharmacol.Biochem.Behav_60_377

Reference

Title : Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities - Cheng_1998_Pharmacol.Biochem.Behav_60_377
Author(s) : Cheng DH , Tang XC
Ref : Pharmacol Biochem Behav , 60 :377 , 1998
Abstract : Comparative effects of cholinesterase inhibitors (ChEI) huperzine A with E2020 and tacrine on the radial maze performance in ethylcholine mustard aziridinium ion (AF64A)-treated rat and inhibition of cholinesterase activity were studied. The intracerebroventricular (i.c.v.) injection of AF64A (3 nmol/side) caused significant impairment in the rat's ability to fulfill the partially baited maze paradigm. Oral huperzine A (0.5-0.8 mg/kg), E2020 (1.0-2.0 mg/kg), and tacrine (8.0 mg/kg) effectively reversed AF64A-induced working memory deficit. The doses that improved AF64A-induced memory deficit were correlated to about 25-30% (huperzine A) and less than 10% (E2020, tacrine) inhibition of acetylcholinesterase (AChE) activity in the cortex and hippocampus. Huperzine A, E2020 and tacrine all produced dose-dependent inhibition of brain AChE following i.c.v. and oral administration. Oral huperzine A exhibited higher efficacy on the inhibition of AChE in the cortex and hippocampus than those of E2020 and tacrine. Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BCHE) than it was brain AChE. Conversely, the BCHE activity was less affected by huperzine A and E2020. The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus. Huperzine A fits more closely with the established criteria for an ideal AChE inhibitor to be used in clinical studies.
ESTHER : Cheng_1998_Pharmacol.Biochem.Behav_60_377
PubMedSearch : Cheng_1998_Pharmacol.Biochem.Behav_60_377
PubMedID: 9632220

Related information

Citations formats

Cheng DH, Tang XC (1998)
Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities
Pharmacol Biochem Behav 60 :377

Cheng DH, Tang XC (1998)
Pharmacol Biochem Behav 60 :377

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    [author] => Cheng DH || Tang XC
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    [title] => Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities
    [journal] => Pharmacol Biochem Behav
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            [content] => Comparative effects of cholinesterase inhibitors (ChEI) huperzine A with E2020 and tacrine on the radial maze performance in ethylcholine mustard aziridinium ion (AF64A)-treated rat and inhibition of cholinesterase activity were studied. The intracerebroventricular (i.c.v.) injection of AF64A (3 nmol/side) caused significant impairment in the rat's ability to fulfill the partially baited maze paradigm. Oral huperzine A (0.5-0.8 mg/kg), E2020 (1.0-2.0 mg/kg), and tacrine (8.0 mg/kg) effectively reversed AF64A-induced working memory deficit. The doses that improved AF64A-induced memory deficit were correlated to about 25-30% (huperzine A) and less than 10% (E2020, tacrine) inhibition of acetylcholinesterase (AChE) activity in the cortex and hippocampus. Huperzine A, E2020 and tacrine all produced dose-dependent inhibition of brain AChE following i.c.v. and oral administration. Oral huperzine A exhibited higher efficacy on the inhibition of AChE in the cortex and hippocampus than those of E2020 and tacrine. Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BCHE) than it was brain AChE. Conversely, the BCHE activity was less affected by huperzine A and E2020. The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus. Huperzine A fits more closely with the established criteria for an ideal AChE inhibitor to be used in clinical studies.
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