A human neuroblastoma cell line expresses mu and delta opioid receptor sites

• Published in: The Journal of biological chemistry Vol. 261; no. 3; pp. 1065 - 1070
• Main Authors: Yu, V C, Richards, M L, Sadée, W
• Format: Journal Article
• Language: English
• Published: Bethesda, MD Elsevier Inc 25.01.1986; American Society for Biochemistry and Molecular Biology
• Subjects: Biological and medical sciences; Bone Neoplasms - metabolism; Cell Line; Cell receptors; Cell structures and functions; Child, Preschool; Diprenorphine - metabolism; Enkephalin, Ala-MePhe-Gly; Enkephalin, Leucine - analogs & derivatives; Enkephalin, Leucine - metabolism; Enkephalin, Leucine-2-Alanine; Enkephalins - metabolism; Etorphine - pharmacology; Female; Fundamental and applied biological sciences. Psychology; Guanylyl Imidodiphosphate - pharmacology; Humans; Kinetics; Molecular and cellular biology; Naloxone - metabolism; Neuroblastoma - metabolism; Receptors, Opioid - metabolism; Receptors, Opioid, delta; Receptors, Opioid, mu; Sodium Chloride - pharmacology; Human; Opiate receptor; Cell culture; Cell line; Molecular interaction; Binding site; Neuroblastoma; Gene expression
• ISSN: 0021-9258; 1083-351X
• DOI: 10.1016/S0021-9258(17)36053-2

A series of neuroblastoma cell lines were screened for the presence of opioid receptor sites with the tracers [3H]diprenorphine (mu, delta, kappa ligand) and [3H]naloxone (mu-selective ligand). One human neuroblastoma cell line, SK-N-SH, displayed avid binding for both tracers. Binding experiments with multiple tracers revealed the presence of both mu and delta sites. These sites were stereospecific, saturable, and proteinaceous in character. Saturation binding experiments provided an estimate of 50,000 mu and 10,000 delta sites/cell. NaCl (100 mM) and guanine nucleotide, guanylyl imidodiphosphate (50 microM), reduced opioid agonist but not antagonist binding to these sites. Etorphine at 1 nM inhibited prostaglandin E1-stimulated cyclic AMP production by approximately 20%, which was reversible by naloxone. The opioid-binding sites on SK-N-SH cells closely resemble the previously reported mu and delta sites in human and rodent brain. Therefore, the SK-N-SH neuroblastoma cell line represents a useful tool to study the molecular functions of opioid receptors.