Other Chemicals and Drugs Commons^™

In Vitro Metabolism Of The Synthetic Cannabinoids Px-1, Px-2, Px-3 And A Comparison Of Their Clearance Rates In Human Liver Microsomes, Travon Cooman

Graduate Theses, Dissertations, and Problem Reports (ETD)

Detection of SCs in body fluids continue to be a challenge because of limited metabolism data, lack of standards and reference mass spectrometry data. In vivo and in vitro experiments help elucidate metabolite markers for novel psychoactive substances and can prompt synthesis of standards to verify proposed metabolites. In this study, metabolism of three SCs N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(5-fluoropentyl)-1H-indole-3-carboxamine (PX-1), N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(5-fluropentyl)-1H-indazole-3-carboxamide (PX-2), and N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(cyclohexylmethyl)-1H-indazole-3-carboxamide (PX-3) were investigated using human liver microsomes. Previous studies showed PX-3 as the most potent CB1 and CB2 receptor agonist.

Half-life and clearance data were acquired using liquid chromatography- tandem mass spectrometry. Metabolite elucidation was performed using liquid chromatography …

Targeting Lipoprotein Biogenesis: Considerations Towards Antimicrobials, Toufic El Arnaout, Tewfic Soulimane

Articles

Decades have passed without approval of a new antibiotic class. Several companies have recently halted related discovery efforts because of multiple obstacles. One promising route under research is to target the lipoprotein maturation pathway in light of major recent findings and the virulence roles of lipoproteins. To support the future design of selective drugs, considerations and priority-setting are established for the main lipoprotein processing enzymes (Lgt, LspA, and Lnt) based on microbiology, biochemistry, structural biology, chemical design, and pharmacology. Although not all bacterial species will be similarly impacted by drug candidates, several advantages make LspA a top target to pursue …

Pharmacodynamics Of Monoamine Transporter Releasing Agents And Reuptake Inhibitors, Alexa Holloway

Theses and Dissertations

Ligands of the human monoamine transporters encompass a wide range of both illicit and therapeutic drugs that act upon neural circuitry related to reward, motivation, and the processing of salient stimuli. The present study utilizes two methods for analyzing transporter substrates and inhibitors in order to characterize activity and assess potency. The first measures transient changes in intracellular calcium as a surrogate for transporter activity by harnessing the electrical coupling of monoamine transporters and L-type calcium channels. This is used to analyze novel chimera of the strong hDAT inhibitors methylphenidate and ��-PPP in order to assess the contribution of specific …