Ifenprodil and SL 82.0715 potently inhibit binding of [3H](+)-3-PPP to sigma binding sites in rat brain.
SL 82.0715 and ifenprodil are potent anti-ischemic agents, which are believed to be due to non-competitive antagonism of N-methyl-D-aspartate (NMDA). It has been proposed that SL 82.0715 and ifenprodil non-competitively antagonize the actions of NMDA by interacting as antagonists with a polyamine site associated with the NMDA/phencyclidine (PCP)/glycine complex. The present study demonstrates that the actions of SL 82.0715 and ifenprodil may also be due in part to an interaction with sigma binding sites, a property that is not shared with polyamines.
Contreras
P C
PC
CNS Diseases Research, G.D. Searle & Co., St. Louis, MO 63198.
Bremer
M E
ME
Gray
N M
NM
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D015259:Dopamine Agents / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D010880:Piperidines / Q000378:metabolism* / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017480:Receptors, sigma; D014316:Tritium
D015259:Dopamine Agents; D010880:Piperidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; D014316:Tritium; C026539:preclamol; C010739:ifenprodil; C058083:eliprodil