• Pharmacol. Biochem. Behav. · Nov 2000

    Pharmacological identification of SM-21, the novel sigma(2) antagonist.

    • C Ghelardini, N Galeotti, and A Bartolini.
    • Department of Preclinical and Clinical Pharmacology, Viale G. Pieraccini 6, University of Florence, I-50139, Florence, Italy. ghelard@server1.pharm.unifi.it
    • Pharmacol. Biochem. Behav. 2000 Nov 1;67(3):659-62.

    AbstractSM-21 is a tropane analogue with high affinity and selectivity for sigma(2) receptor subtype. In the absence of highly selective sigma(2) antagonists, the aim of the present study was to determine whether SM-21 is endowed with antagonistic activity. The experiments were conducted in rats by inducing neck dystonia, which is reported to be subsequent to activation of sigma(2) receptors. SM-21 (10 nmol/0.5 microl) was able to prevent torsion of the neck obtained by administration of the sigma(1)-sigma(2) agonist 1,3-di-(2-tolyl)guanidine (DTG, 5 nmol/0.5 microl) in the red nucleus. These data indicate that SM-21 is a potent and selective sigma(2) antagonist.

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