PMID: 8947921Nov 1, 1996Paper

Sigma binding in a human neuroblastoma cell line

Neurochemical Research
J Ryan-MoroGavril W Pasternak

Abstract

Behaviorally, sigma1 agents modulate opioid analgesia. To examine possible mechanisms responsible for these interactions, we have identified a cell line containing both sigma1 and opioid receptors. [3H](+)-pentazocine binding in BE(2)-C human neuroblastoma cells is high affinity (KD 3.4 +/- 0.7 nM) and high density (Bmax 2.98 +/- 0.14 pmol/mg protein). Competition studies reveal a selectivity profile similar to that of sigma1 sites in guinea pig brain. (+)-Pentazocine has no effect upon either basal or forskolin-stimulated cyclase in the BE(2)-C cells, but cAMP accumulation is inhibited by the morphine, DPDPE and naloxone benzoylhydrazone. (+)-Pentazocine at concentrations as high as 10 microM does not affect this opioid effect, implying that sigma1/opioid interactions are not mediated at the level of the cell. This suggest that their behavioral interactions result from interacting neural circuits. Although (+)-pentazocine is without effect in the cyclase system, it does block carbachol-stimulated phosphoinositol turnover (IC50 6.5 +/- 1.14 microM). The specificity of the effect is confirmed by the ability of haloperidol (1 microM) to shift the IC50 value of (+)-pentazocine 2-fold to the right.

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Citations

Jul 4, 2001·Biochemical Pharmacology·J Mei, G W Pasternak
Nov 18, 2000·European Journal of Pharmacology·W Hong, L L Werling
Sep 6, 2002·Pharmacology, Biochemistry, and Behavior·S M RawlsMartin W Adler
Jun 10, 2015·Journal of Receptor and Signal Transduction Research·Colin G Rousseaux, Stephanie F Greene
Feb 28, 2002·The Journal of Pharmacology and Experimental Therapeutics·Jianfeng Mei, Gavril W Pasternak
Sep 6, 2013·Molecular Pharmacology·Joel M SchrockFelix J Kim
May 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Magali ToussaintPeter Brust
Feb 27, 2017·Cancer Research·Jeffrey D ThomasFelix J Kim
Aug 4, 2004·Cancer Research·Ebru AydarMustafa B A Djamgoz

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