Albensi B C, Alasti N, Mueller A L
NPS Pharmaceuticals, Inc., Salt Lake City, Utah 84108, USA.
J Neurosci Res. 2000 Oct 15;62(2):177-85. doi: 10.1002/1097-4547(20001015)62:2<177::AID-JNR3>3.0.CO;2-D.
The role of the NMDA receptor (NMDAR) in long-term potentiation (LTP) is now well established. All potent NMDAR antagonists known to date inhibit the induction of LTP at the Schaffer collateral-CA1 pyramidal cell synapse in rat hippocampus, regardless of their site and mechanism of action. Arylalkylamine toxins are noncompetitive NMDAR antagonists in the mammalian central nervous system (CNS). The synthetic toxins argiotoxin-636 (Arg-636), Joro spider toxin (JSTX-3), alpha-agatoxin-489 and -505 (Agel-489 and Agel-505) and philanthotoxin-433 (delta-PhTX) were found in the present study to have no effect on the induction of LTP in the Schaffer collateral-CA1 pyramidal cell pathway in rat hippocampal slices maintained in vitro. Arylalkylamine toxins represent a class of potent NMDAR antagonists that fail to affect hippocampal LTP, and thus provide novel structural leads for the development of NMDAR antagonists that do not impair cognition.
N-甲基-D-天冬氨酸受体(NMDAR)在长时程增强(LTP)中的作用现已得到充分证实。迄今为止已知的所有强效NMDAR拮抗剂,无论其作用位点和作用机制如何,均能抑制大鼠海马体中谢弗侧支- CA1锥体细胞突触处LTP的诱导。芳基烷基胺毒素是哺乳动物中枢神经系统(CNS)中的非竞争性NMDAR拮抗剂。在本研究中发现,合成毒素银环蛇毒素-636(Arg-636)、乔罗蜘蛛毒素(JSTX-3)、α-阿加毒素-489和-505(Agel-489和Agel-505)以及 philanthotoxin-433(δ-PhTX)对体外培养的大鼠海马切片中谢弗侧支- CA1锥体细胞通路中LTP的诱导没有影响。芳基烷基胺毒素代表一类强效的NMDAR拮抗剂,它们不会影响海马体LTP,因此为开发不损害认知功能的NMDAR拮抗剂提供了新的结构线索。