Sigma-1 receptors

Characterization of Phencyclidine and Sigma Receptor-Binding Sites in Brain... 

Tam, S.W. Naloxone-inaccessible sigma receptor in rat central nervous sytem. Proc Natl Acad Sci USA 80 6703-6707, 1983. 

In order to determine the potential correlation between any of these variables and affinity for the PCP/sigma receptor, we determined the concentration of these drugs required to displace specific binding of 3H-PCP to rat cortical membranes (Johnson and Snell 1985). In other experiments, we determined the effect of... 

Two points need to be emphasized concerning the data on ACh release. First, PCP, etoxadrol, and cyclazocine are very potent, being effective in the same range in which they compete with 3H-PCP for binding to the PCP/sigma receptor recognition site. 

The most interesting aspects of the studies reviewed here are that the drugs having discriminative stimulus properties similar to PCP also produce ipsilateral turning and that this behavior is well correlated with both affinity for the PCP/sigma receptor and the ability to inhibit the effects of NMDA on transmitter release in the striatum. Although inhibition of NMDA-induced DA release was... 

If PCP produces its multitude of effects by activating PCP (sigma) receptors, then chronic exposure to agonists should elicit the development of tolerance. Tolerance to plasma prolactin suppression by PCP is observed in rats following daily administration for 28 days (Quirion et al. 1982). Chronic PCP treatment has been also shown to reduce the number of PCP sites (receptors) in rodent brains (Quiriun et al. 1983). Behavioral studies have documented the development of tolerance to and dependence on PCP (Balster and Woolverton 1980 Flint and Ho 1980). A tolerance syndrome develops in humans, in which the user is compelled to increase his intake of drug (Jain et al. 1977). 

Guitart, X., Codony, X., Monroy, X. Sigma receptors biology and therapeutic potential. Psychopharmacology. 174 301, 2004. 

Matsumoto, R.R., Liu, Y., Lemer, M., Howard, E.W., Brackett, DJ. Sigma receptors potential medications development target for anti-cocaine agents. Eur. J. Pharmacol. 469 1, 2003. 

Nguyen, E.C., McCracken, K.A., Liu, Y., Pouw, B., Matsumoto, R.R. Involvement of sigma (sigma) receptors in the acute actions of methamphetamine receptor binding and behavioral studies. Neuropharmacology. 3 00, 2005. 

Matsumoto, R.R. et al., Involvement of sigma receptors in the behavioral effects of cocaine evidence from novel ligands and antisense oligodeoxynucleotides, Neuropharmacology. 42, 1043, 2002. 

Flavonoids Sigma receptor binding PKC inhibitor PTKinase inhibitor IL-6 inhibitor Opioid jL/ and k binding... 

Sigma receptors Ibogaine binds to both crl and o2 receptors, with affinities in the range of 1.5-3 pM (Itzhak and Ali 1998). Some have... 

Raffa RB. (1998). Screen of receptor and uptake-site activity of hypericin component of St. John s wort reveals sigma receptor binding. Life Sci. 62(16) PL265-70. 

Bouchard P, Roman F, Junien JL, Quirion R. 1996. Autoradiographic evidence for the modulation of in vivo sigma receptor labeling by neuropeptide Y and calcitonin gene-related peptide in the mouse brain. J Pharmacol Exp Ther 276 223-230. 

It has been proposed, on the basis of observations made using the benzo-morphan derivative (MR 2034) (8), that all kappa agonists may cause undesired dysophoria and even psychotomimesis in man [27]. Benzomorphans such as MR 2034 with affinity for sigma receptors are well-known to be associated with dysphoria. To date, there has been no report of a dose-ranging clinical study with a truly kappa selective agonist which describes the analgesic effects and the onset of dysphoric symptoms. 

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