Kappa Opioid Binding Characteristics in Rat Central Nervous System Homogenates (Binding)
Mack, Kenneth Joseph
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https://hdl.handle.net/2142/77643
Description
Title
Kappa Opioid Binding Characteristics in Rat Central Nervous System Homogenates (Binding)
Author(s)
Mack, Kenneth Joseph
Issue Date
1985
Department of Study
Biology
Discipline
Biology
Degree Granting Institution
University of Illinois at Urbana-Champaign
Degree Name
Ph.D.
Degree Level
Dissertation
Keyword(s)
Biology, General
Language
eng
Abstract
Multiple types of opiate receptors have been proposed on the basis of pharmacological and biochemical studies. Mu and delta opiate receptors have been the most widely studied because of the availability of tissues enriched in these specific receptor subtypes and the availability of specific radioligands.
Data presented in this thesis has compared brain and spinal cord kappa opioid binding in an attempt to identify an enriched population of kappa sites for study. The relative percentage of kappa binding was similar in both tissues, although brain contained a higher absolute number of sites. No significant differences in opiate affinity characteristics were identified between the two tissues.
Additionally, paradigms using ('3)H-ethylketocyclazocine and ('3)H-diprenorphine were studied under conditions where mu and delta sites were blocked. Under these blocked conditions, ('3)H-ethylketocyclazoince labelled a single site as defined by kinetic and equilibrium analysis which showed high affinity for prototypic kappa ligands. Blocked ('3)H-diprenorphine binding data suggested the labelling of an additional binding site.
Finally, the effects of GTP and sodium were investigated on putative kappa opioid binding using the blocked ('3)H-ethylketocyclazocine paradigm. These data suggested that kappa sites are GTP and sodium sensitive, however, ('3)H-ethylketocyclazocine binding to kappa sites is less sensitive to GTP than its binding to other sites.
In summary, this thesis has been an effort to understand the binding characteristics of the kappa opioid binding site/receptor. Investigations were performed to compare rationally selected CNS tissue types and available radioligands in order to find an appropriate paradigm that could characterize the kappa opioid binding site. This paradigm was then used to gather information concerning the potential role of the kappa receptor in the modulation of adenylate cyclase.
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