Inhibition of voltage-gated Ca2+ channels by antazoline.

Didier Milhaud, Laurent Fagni, Joël Bockaert, Mireille Lafon-Cazal

Index: Neuroreport 13(14) , 1711-4, (2002)

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Abstract

We showed recently that imidazolines exert neuroprotection against hypoxia and NMDA toxicity in cerebellar and striatal neuronal cultures, through a voltage-dependent blockade of glutamatergic NMDA receptors. Here, we report that in striatal neuronal cultures from mouse embryos the imidazoline compound, antazoline, inhibits voltage-gated Ca2+ channels by acting at a phencyclidine-like site. This effect was fast, fully reversible, voltage-dependent and predominant on P/Q- and N-type Ca2+ channels. Taken together, these results suggest that imidazolines may elicit neuroprotective effects also by decreasing the release of glutamate through inhibition of presynaptic Ca2+ channels.Copyright 2002 Lippincott Williams & Wilkins