( sup 3 H)(D-PEN sup 2 , D-PEN sup 5 ) enkephalin binding to delta opioid receptors on intact neuroblastoma-glioma (NG 108-15) hybrid cells

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(90)90462-Z· OSTI ID:6939650

Knapp, R J; Yamamura, H I ^[1]

---

1. Univ. of Arizona College of Medicine, Tucson (USA)

({sup 3}H)(D-Pen{sup 2}, D-Pen{sup 5})enkephalin binding to intact NG 108-15 cells has been measured under physiological conditions of temperature and medium. The dissociation constant, receptor density, and Hill slope values measured under these conditions are consistent with values obtained by others using membranes prepared from these cells. Kinetic analysis of the radioligand binding to these cells show biphasic association and monophasic dissociation processes suggesting the presence of different receptor affinity states for the agonist. The data show that the binding affinity of ({sup 3}H)(D-Pen{sup 2}, D-Pen{sup 5})enkephalin under physiological conditions is not substantially different to that measured in 50 mM Tris buffer using cell membrane fractions. Unlike DPDPE, the {mu} opioid agonists morphine, normorphine, PL-17, and DAMGO, have much lower affinity for the {delta} receptor measured under these conditions than is observed by studies using 50 mM Tris buffer. The results described here suggest that this assay may serve as a useful model of {delta} opioid receptor binding in vivo.

• OSTI ID: 6939650
• Journal Information: Life Sciences; (USA), Vol. 46:20; ISSN 0024-3205
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
ENDORPHINS
RECEPTORS
ENKEPHALINS
BIOCHEMICAL REACTION KINETICS
AFFINITY
BIOASSAY
CELL MEMBRANES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
AUTONOMIC NERVOUS SYSTEM AGENTS
CELL CONSTITUENTS
DRUGS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MEMBRANE PROTEINS
MEMBRANES
NEUROREGULATORS
ORGANIC COMPOUNDS
PEPTIDES
POLYPEPTIDES
PROTEINS
REACTION KINETICS
550201* - Biochemistry- Tracer Techniques