University of Tennessee Health Science Center
Validation of ACTOne CB1 and CB2 Assays, Subsequent Characterization of SMM-189, and Development and Characterization of New CB2 Inverse Agonists
Abstract
dc:description.abstract<p>Cannabinoids have emerged on the national scene as a promising untapped therapeutic class. In pursuit of development of cannabinoids for pharmacologic use, I established and validated two high-throughput in vitro pharmacological screening systems, the ACTOne cannabinoid 1 and cannabinoid 2 assays, to aid in evaluating cannabinoid compounds for receptor affinity, pharmacologic potency and efficacy, and for selected compounds, antagonist activity. Our lead compound, SMM-189, was evaluated using the ACTOne assays and determined to be a CB2 inverse agonist. Further investigation revealed SMM-189 to exert anti-inflammatory effects on the brain’s immune cells, microglia, through polarization to a pro-wound healing state. Next generation analogs of SMM-189 were also evaluated in the ACTOne assays in the hopes of developing a molecule with improved biochemical characteristics.</p>
Degree
thesis:*- Name thesis:degree_name
- Doctor of Philosophy (PhD)
- Level thesis:degree_level
- Dissertation
- Discipline thesis:degree_discipline
- Pharmaceutical Sciences
- Year dc:date.available
- 2016
Author and committee
dc:creator, dc:contributor.*- Author dc:creator
-
- Presley, Chaela Sickbert
- Contributors dc:contributor
-
- Bob M. Moore, II, Ph.D.
Subjects
dc:subject × 9Identifiers
dc:identifier.*- Repository record dc:identifier
- https://dc.uthsc.edu/dissertations/418
- OAI identifier oai:identifier
- oai:dc.uthsc.edu:dissertations-1413