Journal article

BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.

FY Carroll, A Stolle, PM Beart, A Voerste, I Brabet, F Mauler, C Joly, H Antonicek, J Bockaert, T Müller, JP Pin, L Prézeau

Molecular Pharmacology | Published : 2001

Abstract

L-Glutamate (Glu) activates at least eight different G protein-coupled receptors known as metabotropic glutamate (mGlu) receptors, which mostly act as regulators of synaptic transmission. These receptors consist of two domains: an extracellular domain in which agonists bind and a transmembrane heptahelix region involved in G protein activation. Although new mGlu receptor agonists and antagonists have been described, few are selective for a single mGlu subtype. Here, we have examined the effects of a novel compound, BAY36-7620 [(3aS,6aS)- 6a-Naphtalen-2-ylmethyl-5-methyliden-hexahydro-cyclopental[c]furan-1-on], on mGlu receptors (mGlu1-8), transiently expressed in human embryonic kidney 293 c..

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