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Full-Text Articles in Medicine and Health Sciences
Design And Synthesis Of Salvinorin-Based Compounds For The Opioid Receptors., Nicholas S. Akins
Design And Synthesis Of Salvinorin-Based Compounds For The Opioid Receptors., Nicholas S. Akins
Electronic Theses and Dissertations
Opioid receptors (OR) are expressed throughout both the peripheral and central nervous system and play crucial roles in the modulation of antinociception, addiction, anxiety, and depression. Salvinorin A, the main isolate of the hallucinogenic plant Salvia divinorum, is one of the most potent naturally occurring kappa opioid receptor agonists. Salvinorin A possesses beneficial effects as a therapeutic in a variety of CNS disorders, but due to its strong hallucinating, anxiogenic effects, and short half-life(t1/2), it has never advanced to clinical trials. Instead, salvinorin A has been used as an important prototype for the development of related drug candidates. Our initial …
Characterization Of G-Protein Coupled Receptors In Pain, Depression And Anxiety, Neil Lax
Characterization Of G-Protein Coupled Receptors In Pain, Depression And Anxiety, Neil Lax
Electronic Theses and Dissertations
Chronic pain and major depressive disorder are widespread conditions in the world. Interestingly, these conditions often occur comorbidly, with each individual disease amplifying the symptoms of the other. A significant amount of preclinical research in pain and depression focuses on G-protein coupled receptors (GPCRs), implying that GPCRs may be useful in treating this comorbidity. Our efforts have sought to characterize several poorly understood GPCRs, including the serotonin receptor subtypes 2C and 7 (5-HT2CR and 5-HT7R) and metabotropic glutamate receptor 5 (mGluR5), along with more well-known GPCRs such as the mu opioid receptor (MOR), and the role that they play in …
Functional Studies Of Novel Bioactives From Complex Host-Microbiomes As Drug Leads For Cancer, Infectious Disease, Depression And Pain, John Jason Bowling
Functional Studies Of Novel Bioactives From Complex Host-Microbiomes As Drug Leads For Cancer, Infectious Disease, Depression And Pain, John Jason Bowling
Electronic Theses and Dissertations
The drug discovery process has become increasingly complex in comparison to early efforts particularly those involving diseases or conditions that affect large numbers of the human population. It is difficult to point directly to one factor leading evolution of the process but the definition of a mechanism of pharmacological action for a drug lead has noticeably become a higher priority. This evolution has helped diminish the stigma of natural products and compound supply issues. The issue of compound supply has also been addressed to some extent with the emergence of recombinant technologies and new synthetic methodology. With approximately 60 years …