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Opioid agonists binding and responses in SH-SY5Y cellsSH-SY5Y (human neuroblastoma) cultured cells, known to have mu-opioid receptors, have been used to assess and compare the ability of eight representative mu-selective compounds from diverse opioid families to recognize and activate these receptors. A wide range of receptor affinities spanning a factor of 10,000 was found between the highest affinity fentanyl analogs (Ki = 0.1nM) and the lowest affinity analog, meperidine (Ki = 1 microM). A similar range was found for inhibition of PGE1-stimulated cAMP accumulation with a rank order of activities that closely paralleled binding affinities. Maximum inhibition of cAMP accumulation by each compound was about 80%. Maximum stimulation of GTPase activity (approximately 50%) was also similar for all compounds except the lowest affinity meperidine. Both effects were naloxone reversible. These results provide further evidence that mu-receptors are coupled to inhibition of adenylate cyclase and that the SH-SY5Y cell line is a good system for assessment of mu-agonists functional responses.
Document ID
20050000836
Acquisition Source
Legacy CDMS
Document Type
Reprint (Version printed in journal)
Authors
Costa, E. M.
(Molecular Research Institute Palo Alto, CA 94304)
Hoffmann, B. B.
Loew, G. H.
Date Acquired
August 22, 2013
Publication Date
January 1, 1992
Publication Information
Publication: Life sciences
Volume: 50
Issue: 1
ISSN: 0024-3205
Subject Category
Exobiology
Funding Number(s)
CONTRACT_GRANT: 2622
Distribution Limits
Public
Copyright
Other
Keywords
Non-NASA Center
NASA Discipline Exobiology

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