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Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling

Hellewell, Susan B., Bruce, Ashley, Feinstein, Glen, Orringer, Jeffrey, Williams, Wanda, Bowen, Wayne D.·1994·European Journal of Pharmacology: Molecular Pharmacology
DOI 10.1016/0922-4106(94)90115-5
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Abstract

Rat liver and kidney were investigated for the presence of sigma (sigma) receptor subtypes by radioligand binding with three highly selective sigma probes and by photoaffinity labeling using [3H]azido-di-o-tolylguanidine ([3H]azido-DTG). [3H](+)-Pentazocine, a highly selective sigma 1 probe, bound to sites in liver membranes with Kd = 7.5 nM and Bmax3 = 2929 fmol/mg protein. [3H](+)-Pentazocine binding sites in kidney had Kd = 23.3 nM and Bmax = 229 fmol/mg protein. [3H]1,3-Di-o-tolylguanidine ([3H]DTG) and [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H](+)-3-PPP) label both sigma 1 and sigma 2 receptors. Parameters for [3H]DTG in the liver were Kd = 17.9 nM and Bmax = 11,895 fmol/mg protein. Similar parameters were observed for [3H](+)-3-PPP, Kd = 51.9 nM and Bmax = 11,070 fmol/mg protein. [3H]DTG bound to rat kidney with Kd = 45.8 nM and Bmax = 1190 fmol/mg protein. The observation that either [3H]DTG or [3H](+)-3-PPP and [3H](+)-3-PPP labeled a higher number of sites relative to [3H](+)-pentazocine suggested that liver and kidney contain both subtypes of sigma receptor. This was confirmed by competition studies vs. [3H](+)-pentazocine and [3H]DTG (in the presence of dextrallorphan to mask sigma 1 sites). In both tissues, [3H](+)-pentazocine labeled sites with high affinity for haloperidol and enantioselectivity for (+)-benzomorphans over (-)-benzomorphans. [3H]DTG + dextrallorphan labeled sites in both tissues which also had high affinity for haloperidol, but whic…

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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 [52]

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Research works printed but not linked: 37

  1. Bowen, 1989, Evidence for a multi-site model of the rat brain sigma receptor, Eur. J. Pharmacol., 163, 309, 10.1016/0014-2999(89)90200-8 · DOI
  2. Bowen, 1992, Sigma-1 and sigma-2 binding sites of rat kidney, Soc. Neurosci. Abstr., 18, 456
  3. Bowen, 1993, [3H](+)-Pentazocine: a potent and highly selective benzomorphan-based probe for sigma-1 receptors, Mol. Neuropharmacol., 3, 117
  4. Bruce, 1990, Characterization of “sigma-like” sites in rat liver membranes: further evidence for sigma-1 and sigma-2 sites, Soc. Neurosci. Abstr., 16, 370
  5. Cheng, 1973, Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (150) of an enzymatic reaction, Biochem. Pharmacol., 22, 3099, 10.1016/0006-2952(73)90196-2 · DOI · Paper page
  6. 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
  7. de Costa, 1992, Synthesis, characterization and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor, J. Med. Chem., 35, 38, 10.1021/jm00079a004 · DOI
  8. Di Paolo, 1991, N-Substituted derivatives of normetazocine: differentiation of sigma-1 and sigma-2 receptors, Soc. Neurosci. Abstr., 17, 814
  9. Ferris, 1991, Sigma receptors: from molecule to man, J. Neurochem., 57, 729, 10.1111/j.1471-4159.1991.tb08213.x · DOI
  10. He, 1993, Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites, J. Med. Chem., 36, 566, 10.1021/jm00057a006 · DOI
  11. Hellewell, 1990, 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, Brain Res., 527, 244, 10.1016/0006-8993(90)91143-5 · DOI · Paper page
  12. Itzhak, 1990, Sigma binding sites in the brain: an emerging concept for multiple sites and their relevance for psychiatric disorders, Life Sci., 47, 1073, 10.1016/0024-3205(90)90165-N · DOI
  13. Itzhak, 1991, Binding of sigma-ligands to C57BL/6 mouse brain membranes: effects of monoamine oxidase inhibitors and subcellular distribution studies suggest the existence of sigma-receptor subtypes, J. Pharmacol. Exp. Ther., 257, 141
  14. Jewell, 1993, Strain differences in rat brain and liver sigma binding: lack of cytochrome P450-2D1 involvement, Eur. J. Pharmacol., 243, 249, 10.1016/0014-2999(93)90182-H · DOI
  15. Karbon, 1991, [3H]DTG and [3H](+)-3-PPP label pharmacologically distinct sigma binding sites in guinea pig brain membranes, Eur. J. Pharmacol., 193, 21, 10.1016/0014-2999(91)90195-V · DOI
  16. Klein, 1991, SKF 525-A and cytochrome P-450 ligands inhibit with high affinity the binding of [3H]dextromethorphan and sigma ligands to guinea pig brain, Life Sci., 48, 543, 10.1016/0024-3205(91)90469-R · DOI
  17. Knight, 1991, The subcellular distribution and pharmacology of the sigma recognition site in the guinea-pig brain and liver, Mol. Neuropharmacol., 1, 71
  18. Laemmli, 1970, Cleavage of structural proteins during the assembly of the head of bacteriophage T4, Nature (London), 227, 680, 10.1038/227680a0 · DOI · Paper page
  19. Lowry, 1951, Protein measurement with the Folin phenol reagent, J. Biol. Chem., 193, 265, 10.1016/S0021-9258(19)52451-6 · DOI
  20. McCann, 1990, Haloperidol-sensitive (+)-[3H]SKF-10,047 binding sites (sigma sites) exhibit a unique distribution in rat brain subcellular fractions, Eur. J. Pharmacol. Mol. Pharmacol. Sect., 188, 211, 10.1016/0922-4106(90)90004-H · DOI
  21. McCann, 1991, Solubilization and characterization of haloperidol-sensitive (+)-[3H]SKF 10,047 binding sites (sigma sites_ from rat liver membranes, J. Pharmacol. Exp. Ther., 257, 547
  22. Monnet, 1993, The cytochromes P-450 are not involved in the modulation of the N-methyl-d-aspartate response by sigma ligands in the rat CA3 dorsal hippocampus, Synapse, 13, 30, 10.1002/syn.890130105 · DOI
  23. Musacchio, 1988, High affinity dextromethophan sites in guinea pig brain: further charcharacterization and allosteric interactions, J. Pharmacol. Exp. Ther., 247, 424
  24. Masacchio, 1989, Dextromethorphan and sigma ligands: common sites but diverse effects, Life Sci., 45, 1721, 10.1016/0024-3205(89)90510-9 · DOI
  25. Quirino, 1992, A proposal for the classification of sigma binding sites, Trends Pharmacol. Sci., 13, 85, 10.1016/0165-6147(92)90030-A · DOI
  26. Radesca, 1991, Synthesis and receptor binding of enantiometric N-substituted cis-N-[2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma ligands, J. Med. Chem., 34, 3058, 10.1021/jm00114a015 · DOI
  27. Ross, 1991, Heterogeneous binding of sigma radioligands in the rat brain and liver: possible relationship to subforms of cytochrome P-450, Pharmacol. Toxicol., 68, 293, 10.1111/j.1600-0773.1991.tb01242.x · DOI
  28. Rothman, 1991, Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands, Mol. Pharmacol., 39, 222
  29. Samovilova, 1988, (+)-[3H]SKF 10,047 binding sites in rat liver, Eur. J. Pharmacol., 147, 259, 10.1016/0014-2999(88)90784-4 · DOI
  30. Su, 1991, Sigma receptors: putative links between nervous, endocrine, and immune systems, Eur. J. Biochem., 200, 633, 10.1111/j.1432-1033.1991.tb16226.x · DOI
  31. Tam, 1992, Is the rat brain sigma receptor the same as cytochrome P-450? Haloperidol down-regulates sigma receptors but not cytochrome P-450, Soc. Neurosci. Abstr., 18, 547
  32. Vilner, 1991, Characterization of [3H]DTG and [3H](+)-3-PPP binding sites of NB41A3 neuroblastoma, C6 glioma, and NG108-15 hybrid cells, Soc. Neurosci. Abstr., 17, 593
  33. Walker, 1990, Sigma receptors: biology and function, Pharmacol. Rev., 42, 355
  34. Walker, 1993, A comparison of (−)-deoxybenzomorphans devoid of opiate activity with their dextrorotatory phenolic counterparts suggests role of sigma-2 receptors in motor function, Eur. J. Pharmacol., 231, 61, 10.1016/0014-2999(93)90684-A · DOI
  35. Weber, 1986, 1,3-Di((2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma that receptors for psychotomimetic opiates and antipsychotic drugs, 83, 8784
  36. Wu, 1991, Electrophysiological and binding studies on intact NCB-202 cells suggest presence of low affinity sigma receptor, J. Pharmacol. Exp. Ther., 257, 351
  37. Zhou, 1991, Computer-assisted modeling of multiple dextromethorphan and sigma binding sites in guinea pig brain, Eur. J. Pharmacol. Mol. Pharmacol. Sect., 206, 261, 10.1016/0922-4106(91)90108-T · DOI

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Metadata

Authors
Hellewell, S. B., Bruce, A., Feinstein, G., Orringer, J., Williams, W., & Bowen, W. D.
Venue
European Journal of Pharmacology: Molecular Pharmacology
Publisher
Elsevier BV
Published
1994-06
Volume
268
Issue
1
Pages
9-18
ISSN
0922-4106
DOI
10.1016/0922-4106(94)90115-5
Cited by
390
References
1
Language
en
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)

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