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σ receptors

Putative links between nervous, endocrine and immune systems

  • Chapter
EJB Reviews 1991

Part of the book series: EJB Reviews 1991 ((EJB REVIEWS,volume 1991))

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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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