Abstract
The σ receptor is a neuronal substrate that binds several psychoactive compounds. These include cocaine, some steroids, dextromethorphan, phencyclidine (PCP), and benzomorphans such as pentazocine and N-allyl-normatezocine (SKF-10047). Many newer atypical antipsychotic drugs also bind to the σ receptor. The σ receptor, however, is not the PCP receptor. The σ receptor exists in the central nervous system, endocrine, immune and certain peripheral tissues. Progesterone and certain steroids have been shown to represent endogenous ligands for the σ receptor. The σ receptor resides likely in the nonsynaptic region of the plasma membrane. The σ receptor exists in two forms: high-affinity and low-affinity. The solubilized σ receptor retains all of the pharmacological characteristics of a membrane-bound receptor. A major physiological role of the σ receptor may involve the modulation of a tonic potassium channel.
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Abbreviations
- BMY-14802:
-
α-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-l-piperazinebutanol
- BW234U:
-
cis-9-[3-(3,5-dimethyl-l-piperazinyl)propyl]carbazole dihydrochloride
- DTG:
-
N,N′-di-(o-tolyl)guanidine
- HPA axis:
-
hypothalamic-pituitary-adrenal axis
- JO 1784:
-
(+)-N-cyclopropylmethyl-N-methyl-1,4-diphenyl-1–ethylbut-3-en-1-ylamine hydrochloride
- MK-801:
-
(+)-5-methyl-10,ll-dihydro-5H-dibenzo-[a,d]cyclohepten-5,10-imine maleate
- NA:
-
noradrenaline
- MeAsp, NMDA:
-
N-methyl-D-aspartate
- NPY:
-
neuropeptide Y
- PCP:
-
phencyclidine
- 3-PPP:
-
(+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine
- PYY:
-
peptide YY
- SCH-23390:
-
7-chloro-8-hydroxyphenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
- SKF-10047:
-
N-allylnormetazocine
- SKF-525A (proadifen):
-
2-(diethylamino)ethyl-2,2-diphenylvalerate
- TCP:
-
1-[1-(2-thienyl)cyclohexyl]piperidine
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Su, TP. (1991). σ receptors. In: Christen, P., Hofmann, E. (eds) EJB Reviews 1991. EJB Reviews 1991, vol 1991. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-77200-9_13
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