European Journal of Pharmacology 1992-12-01

Effects of philanthotoxin-343 on CA1 pyramidal neurons of rat hippocampus in vitro.

N B Fedorov, V G Screbitsky, K G Reymann

Index: Eur. J. Pharmacol. 228 , 201-206, (1992)

Full Text: HTML

Abstract

A synthetic analog of philanthotoxin-433, philanthotoxin-343 (PhTX-343), was tested in hippocampal pyramidal neurons in vitro. PhTX-343 (2 microM) did not significantly change synaptic transmission mediated by AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid)/kainate receptors in the CA1 region of hippocampus. However, PhTX-343 significantly suppressed both the synaptic N-methyl-D-aspartate receptor-induced current (NMDA) obtained in the presence of CNQX(6-cyano-7-nitroquinoxaline-2,3-dione)/picrotoxin (10 microM) and the directly evoked NMDA receptor-induced current to pressure ejection of NMDA in the presence of tetrodotoxin (0.5 microM). A short transient facilitation of both types of NMDA response was seen immediately after the beginning of PhTX-343 application. Our results suggest that at high concentration (2 microM) PhTX-343 inhibits the NMDA-gated current, while the early facilitation occurred during an initial low concentration of the compound. Both facilitative and depressive actions of PhTX-343 are localized at the postsynaptic membrane.

Related Compounds

  • Philanthotoxin 343
  • PhTX-433

Related Articles:

Open-channel blockade is less effective on GluN3B than GluN3A subunit-containing NMDA receptors

2012-07-05

[Eur. J. Pharmacol. 686(1-3) , 22-31, (2012)]

Neuroactive polyamine wasp toxins: nuclear magnetic resonance spectroscopic analysis of the protolytic properties of philanthotoxin-343.

1996-01-19

[J. Med. Chem. 39(2) , 515-21, (1996)]

A sequential high-yielding large-scale solution-method for synthesis of philanthotoxin analogues.

2003-01-01

[Eur. J. Med. Chem. 38(1) , 117-22, (2003)]

Potent and voltage-dependent block by philanthotoxin-343 of neuronal nicotinic receptor/channels in PC12 cells.

1997-09-01

[Br. J. Pharmacol. 122(2) , 379-85, (1997)]

Possible influence of intramolecular hydrogen bonds on the three-dimensional structure of polyamine amides and their interaction with ionotropic glutamate receptors.

2000-01-01

[Receptors Channels 7(3) , 227-36, (2000)]

More Articles...