Sigma antagonists

Ujike, H., Kanzaki, A., Okumuma, K., Akiyama, K., Otsuki, S. Sigma antagonist BMY 14802 prevents methamphetamine-induced sensitization. Life Sci. 50 PL129, 1992. 

Iwamoto, E.T. Locomotor activity and antinociception after putative mu, kappa and sigma opioid receptor agonists in the rat Influence of dopaminergic agonists and antagonists. J Pharmacol Exp Ther 217 451-460, 1981. 

Agonistic and Antagonistic Effects of PCP-Derivatives and Sigma Opioids in PCP Behavioral and Receptor Assays... 

Maurice, T., Martin-Fardon, R., Romieu, P., Matsumoto, R.R. Sigma(l) (sigma(l)) receptor antagonists represent a new strategy against cocaine addiction and toxicity. Neurosci. Biobehav. Rev. 26 499, 2002. 

Wood, P. L., Scotland, M., Richard, J. W., and Rackham, A. (1980) Actions of mu, kappa, sigma, delta and agonist/antagonist opiates on striatal dopaminergic function. J. Pharmacol. Exp. Then, 215 697-703. 

The mechanisms of action of phencyclidine and ketamine are complex (Gorelick Balster, 1995). The drugs are non-competitive antagonists at NMDA receptors, and also bind to associated phencyclidine/sigma opioid receptors. They also have agonist actions at dopamine receptors, complex interactions with both nicotinic and muscarinic acetylcholine receptors and poorly understood interactions with noradrenergic and serotonergic systems. These multiple actions may combine to produce delirium and psychotic reactions. 

In addition to its NMDA antagonistic activity, ifenprodil also interacts non-specifically with other receptor systems (e.g. sigma, 5HT3, a1 McCool et al., 1995 Moebius et al., 1997 Chenard et al., 1999). However, eliprodil, a back-up compound for ifenprodil and the newer NR2B-specific antagonists proved to be far more specific (Chenard et al., 1991). 

Remoxipride is a selective D2 antagonist with higher affinity for the D2S subtype of receptors. It has no affinity for 5-HT, adrenergic, muscarinic or histamine receptors but, unlike the other atypical neuroleptics, does bind to sigma receptors (see p. 453 for possible importance of sigma receptors). 

Javitt DC, Jotkowitz A, Sircar R, Zukin SR. 1987. Noncompetitive regulation of phencyclidine/sigma-receptors by the N-methyl-D-aspartate receptor antagonist D-(-)-2-amino-5-phosphonovaleric acid. Neurosci Lett... 

NMDA-Glu-R antagonist [25 nM 34 nM] (sigma-R) [cerebral peripheral vasodilator]... 

Fluvoxamine also has antagonist properties at sigma 1 receptors... 

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