Regulated endocytosis of opioid receptors: cellular mechanisms and proposed roles in physiological adaptation to opiate drugs.

Abstract:

:Opiate drugs such as morphine and heroin are among the most effective analgesics known. Prolonged or repeated administration of opiates produces adaptive changes in the nervous system that lead to reduced drug potency or efficacy (tolerance), as well as physiological withdrawal symptoms and behavioral manifestations such as craving when drug use is terminated (dependence). These adaptations limit the therapeutic utility of opiate drugs, particularly in the treatment of chronically painful conditions, and are thought to contribute to the highly addictive nature of opiates. For many years it has been proposed that physiological tolerance to opiate drugs is associated with a modification of the number or functional activity of opioid receptors in specific neurons. We now understand certain mechanisms of opioid receptor desensitization and endocytosis in considerable detail. However, the functional roles that these mechanisms play in the complex physiological adaptation of the intact nervous system to opiates are only beginning to be explored.

journal_name

Curr Opin Neurobiol

authors

von Zastrow M,Svingos A,Haberstock-Debic H,Evans C

doi

10.1016/s0959-4388(03)00069-2

subject

Has Abstract

pub_date

2003-06-01 00:00:00

pages

348-53

issue

3

eissn

0959-4388

issn

1873-6882

pii

S0959438803000692

journal_volume

13

pub_type

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