Voprosy meditsinskoi khimii (ISSN 0042-8809)

Regulation of opioid receptors by thyroliberin analogues


1. Research Institute for Psychiatry, Ministry of Public Health
2. Research Institute for Drug Abuse, Ministry of Public Health
PubMed Id: 12498084
Year: 2002 vol: 48  issue:5  pages: 436-442
Abstract: The ability of thyroliberin (TRH) tointeract with opioid receptors (OR) was studied using radioligand analysis. TRH did notinfluence specific binding of [3H]-naloxone, but increased affinity of high affinitybinding sites for the ligand in a dose-dependent manner. TRH also decreased affinity oflow- affinity binding sites. Kinetic analysis of low-affinity binding sites suggests theexistence of at least two subpopulations of OR, which differed in their affinity tonaloxone and mode of interaction with TRH. TRH acted as non-competitive and competitiveinhibitor of receptor binding sites with the lowest and moderate affinity, respectively.The allosteric pattern of TRH influence on OR with high and the lowest affinity tonaloxone was suggested.
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Reference: Balashov A.M., Alyabieva T.N., Panchenko L.F., Regulation of opioid receptors by thyroliberin analogues, Voprosy meditsinskoi khimii, 2002, vol: 48(5), 436-442.