|
|Section2= |Section3= }} AP5 or APV ((2''R'')-amino-5-phosphonovaleric acid; (2''R'')-amino-5-phosphonopentanoate) is a selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors.〔Morris RG. Synaptic plasticity and learning: selective impairment of learning rats and blockade of long-term potentiation in vivo by the N-methyl-D-aspartate receptor antagonist AP5. ''Journal of Neuroscience''. 1989 Sep;9(9):3040-57. PMID 2552039〕 AP5 blocks NMDA receptors in micromolar concentrations (~50 µM). AP5 blocks the cellular analog of classical conditioning in the sea slug ''Aplysia californica'', and has similar effects on ''Aplysia'' long-term potentiation (LTP), since NMDA receptors are required for both. It is sometimes used in conjunction with the calcium chelator BAPTA to determine whether NMDARs are required for a particular cellular process. AP5/APV has also been used to study NMDAR-dependent LTP in the mammalian hippocampus.〔Gustafsson B., Wigström H., Abraham W.C., and Huang Y.Y. Long-Term Potentiation in the Hippocampus Using Depolarizing Current Pulses as the Conditioning Stimulus to Single Volley Synaptic Potentials. ''Journal of Neuroscience.'' 1987 March;7(3):774-780 〕 In general, AP5 is very fast-acting within ''in vitro'' preparations, and can block NMDA receptor action at a reasonably small concentration. The active isomer of AP5 is considered to be the D configuration, although many preparations are available as a racemic mixture of D- and L-isomers. It is useful to isolate the action of other glutamate receptors in the brain, i.e., AMPA and kainate receptors. AP5 can block the conversion of a silent synapse to an active one, since this conversion is NMDA receptor-dependent. AP5 was developed by Jeff Watkins and Harry Olverman. ==See also== *AMPA *AP7 (drug) *Kainate 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「AP5」の詳細全文を読む スポンサード リンク
|