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Full-Text Articles in Medicine and Health Sciences
Selective Non-Peptide Mu-Opioid Receptor Antagonist: Design, Synthesis And Biological Studies, Lindsey Aschenbach
Selective Non-Peptide Mu-Opioid Receptor Antagonist: Design, Synthesis And Biological Studies, Lindsey Aschenbach
Theses and Dissertations
There are currently many opioid agonists available for clinical use as analgesics. However, many of these opioid agonists have notorious side effects including respiratory depression and may lead to addiction and dependence. Problems associated with these opioid agonists are determined to come from their interactions with the mu-opioid receptor. Opioid antagonists, such as naltrexone, have shown to aid in the treatment of opioid addiction. Although naltrexone has high affinity to the mu-opioid receptor, it lacks selectivity. Novel selective mu-opioid receptor antagonists were designed based on the identification of important pharmacophore elements in several known mu-opioid receptor agonists and antagonists. These …
Designing Non-Saccharide Heparin/Heparan Sulfate Mimics, Arjun Raghuraman
Designing Non-Saccharide Heparin/Heparan Sulfate Mimics, Arjun Raghuraman
Theses and Dissertations
Glycosaminoglycans (GAGs) are complex biopolymers that play important roles in inflammation, coagulation, angiogenesis, cell adhesion and viral invasion by interacting with several different proteins.1,2 Structurally, GAGs are built up of several different sulfated disaccharide units.3 Specific GAG sequences that uniquely recognize their cognate proteins exist. Such specificity typically arises from the binding of unique sulfation patterns on the linear GAG chain to highly electropositive protein domains. Thus, these highly charged, sulfated biopolymers potentially represent a new class of therapeutics. Yet, the major stumbling block to the development to these agents is their extremely complicated and tedious chemical synthesis. We hypothesized …
5-Ht3 Receptor Ligands And Their Effect On Psychomotor Stimulants, Jessica Nicole Worsham
5-Ht3 Receptor Ligands And Their Effect On Psychomotor Stimulants, Jessica Nicole Worsham
Theses and Dissertations
Drug abuse and addiction are considered to be a result, at least in part, of the rewarding effects produced by increasing dopamine levels. 5-HT3 serotonin receptors have been shown to indirectly affect dopamine levels. Therefore, the effect of the 5-HT3 receptor partial agonist, MD-354, on the actions of psychomotor stimulants was analyzed in mouse locomotor activity assays to determine whether MD-354 is working through a 5-HT3 receptor agonist or antagonist mode of action. Studies with (+)amphetamine and (+)methamphetamine in combination with MD-354 indicated MD-354 is either devoid of action or is behaving similar to the 5-HT3 receptor antagonist, ondansetron. This …
Characterization Of Yeast 18s Rrna Dimethyl Transferase, Dim1p, Nagesh Pulicherla
Characterization Of Yeast 18s Rrna Dimethyl Transferase, Dim1p, Nagesh Pulicherla
Theses and Dissertations
Eukaryotic ribosome biogenesis, a dynamic and coordinated multistep process which requires more than 150 trans-acting factors, has been intensely studied in the yeast Saccharomyces cerevisiae. This evolutionarily conserved process involves numerous cleavages of pre-rRNA, modification of nucleotides, and concomitant assembly of the ribosomal proteins onto the rRNA. Considerable information is available about the importance of conserved pre-rRNA cleavage events in ribosome biogenesis; however, very little is known about the exact role of modified nucleotides, which cluster within the functionally important regions of the ribosome. One conserved group of modifications is the dimethylation of two adjacent adenosines at the 3´ end …