Chapter title |
Agonist induced constitutive receptor activation as a novel regulatory mechanism. Mu receptor regulation.
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Chapter number | 12 |
Book title |
The Brain Immune Axis and Substance Abuse
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Published in |
Advances in experimental medicine and biology, January 1995
|
DOI | 10.1007/978-1-4615-1951-5_12 |
Pubmed ID | |
Book ISBNs |
978-1-4613-5801-5, 978-1-4615-1951-5
|
Authors |
Wolfgang Sadée, Zaijie Wang, Sadée, Wolfgang, Wang, Zaijie |
Abstract |
We propose the hypothesis that certain G protein coupled receptors can become constitutively activated during agonist stimulation so that the receptor remains active even after the agonist is removed. This new paradigm of receptor regulation may account for some long term effects of neurotransmitters and hormones. We have tested the hypothesis that constitutive mu receptor activation represents a crucial step driving narcotic tolerance and dependence. Our results indeed support the conversion of mu to a constitutively active state, mu*, observed in neuroblastoma SK-N-SH and SH-SY5Y tissue culture, in U293 cells transfected with the mu receptor gene, and in vivo. Constitutive mu activation may result from receptor phosphorylation to yield mu*, and further, in vivo studies indicate that formation of mu* could account for narcotic tolerance and dependence. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 6 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 4 | 67% |
Professor > Associate Professor | 2 | 33% |
Readers by discipline | Count | As % |
---|---|---|
Medicine and Dentistry | 3 | 50% |
Chemistry | 1 | 17% |
Social Sciences | 1 | 17% |
Unknown | 1 | 17% |