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A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain

Hellewell, Susan B., Bowen, Wayne D.·1990·Brain Research
DOI 10.1016/0006-8993(90)91143-5
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Abstract

Two highly selective radiolabeled probes for sigma receptors were found to bind with high affinity and capacity to membranes from undifferentiated PC12 cells. [3H]1,3-di-o-tolylguanidine [( 3H]DTG) bound with Kd = 23.7 +/- 4.6 nM and Bmax = 2025 +/- 660 fmol/mg protein. The Kd and Bmax for [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H](+)-3-PPP) were 86.3 +/- 21.6 nM and 1539 +/- 242 fmol/mg protein, respectively. These binding parameters were comparable to those observed in guinea pig brain, although the Kd for [3H](+)-3-PPP was 3-fold higher in the PC12 membranes. Both the PC12 and guinea pig brain sites exhibited high affinity for haloperidol, moderate affinity for phencyclidine (PCP), and negligible affinity for MK-801, apomorphine, and (-)-sulpiride. These data suggest a relationship of the PC12 site to sigma receptors. However, all (+)-opiates [+)-benzomorphans and (+)-morphinans) tested bound with markedly lower affinity to the PC12 site compared to guinea pig brain. These include (+)-N-allylnormetazocine [+)-SKF 10,047), (+)-pentazocine, and dextrallorphan. In fact, PC12 sites exhibited preference for (-)-benzomorphans, the reverse stereoselectivity of guinea pig brain sites. Binding of [3H]N-[1-(2-thienyl)cyclohexyl]piperidine [( 3H]TCP) could not be detected, demonstrating absence of PCP receptors on this cell line. Differentiation of cells by treatment with nerve growth factor had no effect on sigma binding parameters. Membranes from guinea pig brain and…

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  • S2R activity was initially localized to a ~20 kDa membrane protein and first thought to be progesterone receptor membrane component 1 (PGRMC1).

    “S2R activity was initially localized to a ~20 kDa membrane protein [51,52] and first thought to be progesterone receptor membrane component 1 (PGRMC1), based on mass spectrophotometry identification following an immunoaffinity pull down with an irreversible S2R ligand binder WC-11, physiochemical properties, and pharmacological evidence [53,54].”

    From Sigma-2 Receptors—From Basic Biology to Therapeutic Target: A Focus on Age-Related Degenerative Diseases (2023) · cites this paper as [51]

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Research works printed but not linked: 38

  1. Adams, 1987, Labeling of the haloperidol-sensitive sigma receptor in NCB-20 hybrid neuroblastoma cells with [3H]-(1,3)-di-ortho-tolyl-guanidine and identification of the binding subunit by photoaffinity labeling with [3H]-m-azido-di-ortho-tolyl-ganidine, Soc. Neurosci. Abstr., 13, 1703
  2. Bowen, 1988, Characterization of sigma receptors on PC12 cells: pharmacological differences from rat and guinea pig brain indicate sigma receptor heterogeneity, Soc. Neurosci. Abstr., 14, 703
  3. Bowen, 1989, Evidence for a multisite model of the rat brain sigma receptor, Eur. J. Pharmacol., 163, 309, 10.1016/0014-2999(89)90200-8 · DOI
  4. Bowen, 1988, Sigma receptors negatively modulate agonist-stimulated phosphoinositide metabolism in rat brain, Eur. J. Pharmacol., 149, 399, 10.1016/0014-2999(88)90678-4 · DOI
  5. Bowen, W.D., Tolentino, P.J., Kirschner, B.N., Varghese, P., de Costa, B.R. and Rice, K.C., Sigma receptors and signal transduction: negative modulation of signalling through phosphoinositide-linked receptor systems. In E.B. DeSouza, E.D. London and D.H. Clouet (Eds.),Sigma, PCP, and NMDA Receptor Systems — National Institute on Drug Abuse Research Monograph Series, U.S. Government Printing Office, Washington, DC, in press. · DOI
  6. Bowen, 1988, Altered haloperidol-sensitive sigma receptors in the genetically dystonic (dt) rat, Eur. J. Pharmacol., 147, 153, 10.1016/0014-2999(88)90647-4 · DOI
  7. Campbell, 1987, Both the sigma receptor-specific ligand (+)3-PPP and the PCP receptor-specific ligand TCP act in the mouse vas deferensvia augmentation of electrically evoked norepinephrine release, Eur. J. Pharmacol., 138, 447, 10.1016/0014-2999(87)90487-0 · DOI
  8. Campbell, 1989, Sigma receptors inhibit contractions of the guinea pig ileum longitudinal muscle/myentric plexus preparation elicited by both electrical stimulation and exogenous serotonin, J. Neurosci., 9, 3380, 10.1523/JNEUROSCI.09-10-03380.1989 · DOI
  9. Ceci, 1988, Activation of the A10 mesolimbic system by the sigma-receptor agonist (+)SKF 10,047 can be blocked by rimcazole, a novel putative antipsychotic, Eur. J. Pharmacol., 154, 53, 10.1016/0014-2999(88)90362-7 · DOI
  10. Cheng, 1973, Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction, Biochem. Pharmacol., 22, 3099, 10.1016/0006-2952(73)90196-2 · DOI · Paper page
  11. de Costa, 1989, Synthesis and evaluation of optically pure [3H](+)-pentazocine, a highly potent and selective radioligand for sigma receptors, FEBS lett., 251, 53, 10.1016/0014-5793(89)81427-9 · DOI
  12. Goldstein, 1989, Motor effects of two sigma ligands mediated by nigrostriatal dopamine neurons, Synapse, 4, 254, 10.1002/syn.890040311 · DOI
  13. Greene, 1980, The nerve growth factor: biochemistry, synthesis, and mechanism of action, Annu. Rev. Neurosci., 3, 353, 10.1146/annurev.ne.03.030180.002033 · DOI
  14. Greene, 1977, Nerve growth factor-induced increase in electrical excitability and acetylcholine sensitivity of a rat pheochromocytoma cell line, Nature, 268, 501, 10.1038/268501a0 · DOI
  15. Gundlach, 1986, Autoradiographic localization of sigma receptor binding sites in guinea pig and rat central nervous system with (+)3H-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine, J. Neurosci., 6, 1757, 10.1523/JNEUROSCI.06-06-01757.1986 · DOI
  16. Gundlach, 1985, Phencyclidine and sigma opiate receptors in brain: biochemical and autoradiographical differentiation, Eur. J. Pharmacol., 113, 465, 10.1016/0014-2999(85)90100-1 · DOI
  17. Hellewell, 1988, Photolabelling of sigma receptors in guinea pig brain, rat brain, and PC-12 cells using [3H]azido-di-tolylguanidine: evidence for receptor heterogeneity, Soc. Neurosci. Abstr., 14, 703
  18. Jumblatt, 1982, Regulation of muscarinic ligand binding sites by nerve growth factor in PC 12 phaeochromocytoma cells, Nature, 297, 152, 10.1038/297152a0 · DOI
  19. Kushner, 1988, Characterization of opioid, sigma, and phencyclidine receptors in the neuroblastoma-brain hybrid cell line NCB-20, Mol. Pharmacol., 34, 689
  20. Largent, 1986, Sigma receptors on NCB-20 hybrid neurotumor cells labeled with (+)[3H]SKF 10,047 and (+)[3H]3-PPP, Eur. J. Pharmacol., 124, 183, 10.1016/0014-2999(86)90142-1 · DOI
  21. Loo, 1987, The novel anticonvulsant MK-801 interacts with central phencyclidine recognition sites in rat brain, Eur. J. Pharmacol., 135, 261, 10.1016/0014-2999(87)90624-8 · DOI
  22. Lowry, 1951, Protein measurement with the Folin phenol reagent, J. Biol. Chem., 193, 265, 10.1016/S0021-9258(19)52451-6 · DOI
  23. Luckenbill-Edds, 1979, Fine structure of initial outgrowth of processes induced in a pheochromocytoma cell line (PC 12) by nerve growth factor, J. Neurocyt., 8, 493, 10.1007/BF01214805 · DOI
  24. Maruyama, 1987, myc and E1A oncogene alter the responses of PC 12 cells to nerve growth factor and block differentiation, Oncogene, 1, 361
  25. Matsumoto, 1988, Inhibition of rubral neurons by a specific ligand for sigma receptors, Eur. J. Pharmacol., 158, 161, 10.1016/0014-2999(88)90268-3 · DOI
  26. Matsumoto, 1990, Drug specificity of pharmacological dystonia, Pharmacol. Biochem. Behav., 36, 151, 10.1016/0091-3057(90)90141-4 · DOI
  27. Mendelsohn, 1985, Sigma opioid receptor: characterization and co-identity with the phencyclidine receptor, 233, 597
  28. Reid, 1988, Evidence for two populations of haloperidol-sensitive sigma binding sites in guinea pig brain, Soc. Neurosci. Abstr., 14, 703
  29. Sircar, 1986, Characterization and autoradiographic visualization of (+)-[3H]SKF10,047 binding in rat and mouse brain: further evidence for phencyclidine/‘sigma opiate’ receptor commonality, J. Pharmacol. Exp. Ther., 237, 681
  30. Su, 1982, Evidence for sigma opioid receptor: binding of [3H]SKF 10,047 to etorphine inaccessible sites in guinea-pig brain, J. Pharmacol. Exp. Ther., 223, 284
  31. Tam, 1985, (+)-[3H]SKF-10,047, (+)-[3H]ethylketocyclazocine, mu, kappa, delta, and phencyclidine binding sites in guinea pig brain membranes, Eur. J. Pharmacol., 109, 33, 10.1016/0014-2999(85)90536-9 · DOI
  32. Tischler, 1975, Nerve growth factor-induced process formation by cultured rat pheochromocytoma cells, Nature, 258, 341, 10.1038/258341a0 · DOI
  33. Vaupel, 1987, Guinea-pig vas deferens preparation may contain both sigma receptors and phencyclidine receptors, Eur. J. Pharmacol., 139, 125, 10.1016/0014-2999(87)90507-3 · DOI
  34. Walker, 1988, Evidence for a role of haloperidol-sensitive sigma ‘opiate’ receptors in the motor effects of antipsychotic drugs, Neurology, 38, 961, 10.1212/WNL.38.6.961 · DOI
  35. Weber, 1986, 1,3-Di[2-(5-3H]tolyl)guadinine: a selective ligand that labels sigma type receptors for psychotomimetric opiates and antipsychotic drugs, 83, 8784
  36. West, 1983, [3H]ethylketocyclazocine binding to NCB-20 hybrid neurotumor cells, Mol. Pharmacol., 23, 486
  37. Wolfe, 1989, Sigma receptors in endocrine organs: identification, characterization, and autoradiographic localization in rat pituitary, adrenal, testes, and ovary, Endocrinology, 124, 1160, 10.1210/endo-124-3-1160 · DOI
  38. Wong, E.H., Kemp, J.A., Priestley, T., Knight, A.R., Woodruff, G.N. and Iversen, L.L., The anticonvulsant MK-801 is a potentN-methyl-d-aspartate antagonist,Proc. Natl. Acad. Sci.

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Metadata

Authors
Hellewell, S. B., & Bowen, W. D.
Venue
Brain Research
Publisher
Elsevier BV
Published
1990-09
Volume
527
Issue
2
Pages
244-253
ISSN
0006-8993
DOI
10.1016/0006-8993(90)91143-5
Cited by
341
References
1
Language
en
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)

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