PT  - JOURNAL ARTICLE
AU  - T S Rao
AU  - J A Cler
AU  - M R Emmett
AU  - S Mick
AU  - S Iyengar
AU  - P L Wood
TI  - BMY-14802 antagonizes harmaline- and D-serine-induced increases in mouse cerebellar cyclic GMP: neurochemical evidence for a sigma receptor-mediated functional modulation of responses mediated by the N-methyl-D-aspartate receptor complex in vivo.
DP  - 1990 Jun 01
TA  - Molecular Pharmacology
PG  - 978--982
VI  - 37
IP  - 6
4099  - http://molpharm.aspetjournals.org/content/37/6/978.short
4100  - http://molpharm.aspetjournals.org/content/37/6/978.full
SO  - Mol Pharmacol1990 Jun 01; 37
AB  - BMY-14802 [alpha-(4-flurophenyl)-4-(5-fluoro-pyramidinyl)-1-piperazine butanol], a potent sigma ligand with poor affinity for dopamine and phencyclidine receptors in vitro, attenuated parenteral harmaline- and direct intracerebellar D-serine-induced increases in mouse cerebellar cGMP. Intracerebroventricularly injected BMY-14802 also antagonized the effects of intracerebellar D-serine, indicating a central mechanism. However, direct co-injection of BMY-14802 into the cerebellum failed to antagonize the D-serine-induced increases in cGMP, indicating a locus of action outside the cerebellum. In contrast, quisqualate-induced cGMP increases were not attenuated by BMY-14802. These results indicate a functional modulation of the N-methyl-D-aspartate/glycine/phencyclidine/ion channel complex-mediated events by BMY-14802, possibly through a transsynaptic mechanism, thus representing the first in vivo demonstration of a sigma ligand modulation of a response mediated through the N-methyl-D-aspartate receptor complex.