title: Similar potency of the enantiomers of huperzine A in inhibition of [(3)H]dizocilpine (MK-801) binding in rat cerebral cortex.
abstract: The inhibition of huperzine A, a potential therapeutic agent to treat Alzheimer's disease, on rat cortical acetylcholinesterase was found to be highly stereospecific. In the present study the effect of the enantiomers of huperzine A on [(3)H]dizocilpine (MK-801) binding to synaptic membrane of rat cerebral cortex was compared. The natural (-)-huperzine A and the synthetic (+)-huperzine A inhibited the specific binding of [(3)H]MK-801 with a similar potency. The IC(50) values were 65+/-7 and 82+/-12 microM (n=5 for each enantiomer, P=0.248), respectively. The result indicates that huperzine A inhibits N-methyl-D-aspartate (NMDA) receptor in rat cerebral cortex without stereoselectivity.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences, Chinese Academy of Sciences, 294, Tai-Yuan Road, 200031, PR, Shanghai, China.
authors.forename: Y H
authors.initials: YH
authors.lastname: Zhang
authors.forename: X Q
authors.initials: XQ
authors.lastname: Chen
authors.forename: H H
authors.initials: HH
authors.lastname: Yang
authors.forename: G Y
authors.initials: GY
authors.lastname: Jin
authors.forename: D L
authors.initials: DL
authors.lastname: Bai
authors.forename: G Y
authors.initials: GY
authors.lastname: Hu
mesh_terms: D000470:Alkaloids; D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D001665:Binding Sites / Q000187:drug effects* / Q000502:physiology; D002540:Cerebral Cortex / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000494:pharmacology; D016291:Dizocilpine Maleate / Q000493:pharmacokinetics*; D004347:Drug Interactions / Q000502:physiology; D009474:Neurons / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D018696:Neuroprotective Agents / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects* / Q000378:metabolism; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013570:Synaptic Membranes / Q000187:drug effects* / Q000378:metabolism
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D018696:Neuroprotective Agents; D016194:Receptors, N-Methyl-D-Aspartate; D012717:Sesquiterpenes; C050426:huperzine A; D016291:Dizocilpine Maleate