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.
","abstract_html":"<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>","abstract_has_math":false,"creators":["Presley, Chaela Sickbert"],"institution":null,"degree_name":"Doctor of Philosophy (PhD)","degree_level":"Dissertation","degree_discipline":"Pharmaceutical Sciences","degree_department":null,"school":null,"contributors":["Bob M. Moore, II, Ph.D."],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2016,"date_issued":"2016-12-01T08:00:00Z","date_published":"2016-12-01T08:00:00Z","updated_at":"2026-07-24T05:00:33Z","subjects":["cannabinoids","CB1","CB2","inverse agonist","microglia","triaryl","Medicine and Health Sciences","Pharmaceutics and Drug Design","Pharmacy and Pharmaceutical Sciences"],"languages":[],"rights":[],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"https://dc.uthsc.edu/dissertations/418","outbound_label":"Repository record","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Bob M. Moore, II, Ph.D."]},{"key":"dc:creator","label":"Author","values":["Presley, Chaela Sickbert"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date.available","label":"Dc Date Available","values":["2117-01-25T08:00:00Z"]},{"key":"thesis:degree_discipline","label":"Discipline","values":["Pharmaceutical Sciences"]},{"key":"thesis:degree_level","label":"Degree Level","values":["Dissertation"]},{"key":"thesis:degree_name","label":"Degree Name","values":["Doctor of Philosophy (PhD)"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["cannabinoids","CB1","CB2","inverse agonist","microglia","triaryl","Medicine and Health Sciences","Pharmaceutics and Drug Design","Pharmacy and Pharmaceutical Sciences"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["https://dc.uthsc.edu/dissertations/418"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description.abstract","label":"Abstract","values":["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.
"]},{"key":"dc:title","label":"Title","values":["Validation of ACTOne CB1 and CB2 Assays, Subsequent Characterization of SMM-189, and Development and Characterization of New CB2 Inverse Agonists"]}]}],"canonical_facts":{"dc:contributor":["Bob M. Moore, II, Ph.D."],"dc:creator":["Presley, Chaela Sickbert"],"dc:date.available":["2117-01-25T08:00:00Z"],"dc:description.abstract":["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.
"],"dc:identifier":["https://dc.uthsc.edu/dissertations/418"],"dc:subject":["cannabinoids","CB1","CB2","inverse agonist","microglia","triaryl","Medicine and Health Sciences","Pharmaceutics and Drug Design","Pharmacy and Pharmaceutical Sciences"],"dc:title":["Validation of ACTOne CB1 and CB2 Assays, Subsequent Characterization of SMM-189, and Development and Characterization of New CB2 Inverse Agonists"],"thesis:degree_discipline":["Pharmaceutical Sciences"],"thesis:degree_level":["Dissertation"],"thesis:degree_name":["Doctor of Philosophy (PhD)"]},"updated_at":"2026-07-24T05:00:33Z"}