Characterization of opioid, σ, and phencyclidine receptors in the neuroblastoma-brain hybrid cell line NCB-20

L. Kushner, S. R. Zukin, R. Suzanne Zukin

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Abstract

Opioid, σ, and phencyclidine (PCP) receptors were characterized in the mouse neuroblastoma - Chinese hamster brain hybrid cell line NCB-20. Quantitative receptor assays under equilibrium binding conditions with highly specific radioligands demonstrated the presence of δ, but not μ or κ, opioid receptors on NCB-20 cell membranes. NCB-20 cells were shown to possess two distinct sites specific for σ opioids and PCP derivatives. One site was labeled by (+)-[3H]N-allylnormetazocine [(+)-[3H]SKF-10,047] (K(d) = 69 nM; B(max) = 4100 fmol/mg of protein). The rank order of potency of drugs at this site was (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine [(+)-3-PPP] > haloperidol > (+)-SKF-10,047 > (±)-ethylketocyclazocine > (±)-bremazocine > N-[1-(2-thienyl)cyclohexyl]piperidine (TCP) > dexoxadrol. This site is similar in its ligand selectivity to the haloperidol-sensitive σ receptor of rat brain. The other site was labeled by the potent phencyclidine derivative [3H]TCP (K(d) = 335 nM; B(max) = 9300 fmol/mg of protein). This density is equivalent to approximately 60,000 sites/cell. The rank order of potency of drugs at this site was TCP > (+)-3-PPP > PCP > dexoxadrol > haloperidol > cyclazocine > levoxadrol > (+)-SKF-10,047; μ and δ ligands were inactive. This site is similar to the rat brain PCP receptor. The NCB-20 cell line is the only cultured cell line that has been demonstrated to have PCP receptors.

Original languageEnglish (US)
Pages (from-to)689-694
Number of pages6
JournalMolecular Pharmacology
Volume34
Issue number5
StatePublished - 1988

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Phencyclidine Receptors
Hybrid Cells
Opioid Receptors
Neuroblastoma
Haloperidol
Cell Line
Brain
Opioid Analgesics
Cyclazocine
Ethylketocyclazocine
Ligands
Phencyclidine
Cricetulus
Pharmaceutical Preparations
Cultured Cells
Proteins
Cell Membrane
piperidine

ASJC Scopus subject areas

  • Pharmacology

Cite this

Characterization of opioid, σ, and phencyclidine receptors in the neuroblastoma-brain hybrid cell line NCB-20. / Kushner, L.; Zukin, S. R.; Zukin, R. Suzanne.

In: Molecular Pharmacology, Vol. 34, No. 5, 1988, p. 689-694.

Research output: Contribution to journalArticle

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abstract = "Opioid, σ, and phencyclidine (PCP) receptors were characterized in the mouse neuroblastoma - Chinese hamster brain hybrid cell line NCB-20. Quantitative receptor assays under equilibrium binding conditions with highly specific radioligands demonstrated the presence of δ, but not μ or κ, opioid receptors on NCB-20 cell membranes. NCB-20 cells were shown to possess two distinct sites specific for σ opioids and PCP derivatives. One site was labeled by (+)-[3H]N-allylnormetazocine [(+)-[3H]SKF-10,047] (K(d) = 69 nM; B(max) = 4100 fmol/mg of protein). The rank order of potency of drugs at this site was (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine [(+)-3-PPP] > haloperidol > (+)-SKF-10,047 > (±)-ethylketocyclazocine > (±)-bremazocine > N-[1-(2-thienyl)cyclohexyl]piperidine (TCP) > dexoxadrol. This site is similar in its ligand selectivity to the haloperidol-sensitive σ receptor of rat brain. The other site was labeled by the potent phencyclidine derivative [3H]TCP (K(d) = 335 nM; B(max) = 9300 fmol/mg of protein). This density is equivalent to approximately 60,000 sites/cell. The rank order of potency of drugs at this site was TCP > (+)-3-PPP > PCP > dexoxadrol > haloperidol > cyclazocine > levoxadrol > (+)-SKF-10,047; μ and δ ligands were inactive. This site is similar to the rat brain PCP receptor. The NCB-20 cell line is the only cultured cell line that has been demonstrated to have PCP receptors.",
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