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

Abstract

Opioid, sigma, 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 delta, but not mu or kappa, opioid receptors on NCB-20 cell membranes. NCB-20 cells were shown to possess two distinct sites specific for sigma opioids and PCP derivatives. One site was labeled by (+)-[3H]N-allylnormetazocine [(+)-[3H]SKF-10,047] (Kd = 69 nM; Bmax = 4100 fmol/mg of protein). The rank order of potency of drugs at this site was (+)-3-(3-hydroxy-phenyl)-N-(1-propyl)piperidine [(+)-3-PPP] greater than haloperidol greater than (+)-SKF-10,047 greater than (+/-)-ethylketocyclazocine greater than (+/-)-bremazocine greater than N-[1-(2-thienyl) cyclohexyl]piperidine (TCP) greater than dexoxadrol. This site is similar in its ligand selectivity to the haloperidol-sensitive sigma receptor of rat brain. The other site was labeled by the potent phencyclidine derivative [3H]TCP (Kd = 335 nM; Bmax = 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 greater than (+)-3-PPP greater than PCP greater than dexoxadrol greater than haloperidol greater than cyclazocine greater than levoxadrol greater than (+)-SKF-10,047; mu and delta 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.

• Authors: L Kushner, S R Zukin, R S Zukin
• Journal: Molecular pharmacology (Mol Pharmacol) Vol. 34 Issue 5 Pg. 689-94 (Nov 1988) ISSN: 0026-895X [Print] United States
• PMID: 2848188 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Receptors, N-Methyl-D-Aspartate
• Receptors, Neurotransmitter
• Receptors, Opioid
• Receptors, Phencyclidine
• Receptors, sigma
• SK&F 10047
• tenocyclidine
• Phenazocine
• Phencyclidine

Topics

• Animals
• Brain Chemistry
• Cell Line
• Cricetinae
• Hybrid Cells
• Kinetics
• Mice
• Neuroblastoma (analysis)
• Phenazocine (analogs & derivatives, metabolism)
• Phencyclidine (analogs & derivatives, metabolism)
• Receptors, N-Methyl-D-Aspartate
• Receptors, Neurotransmitter (analysis)
• Receptors, Opioid (analysis)
• Receptors, Phencyclidine
• Receptors, sigma