Azetidines

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  Subject Areas on Research

  • 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling. 
  • 2-[18F]F-A-85380: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans. 
  • 2-[18F]F-A-85380: a PET radioligand for alpha4beta2 nicotinic acetylcholine receptors. 
  • 5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors. 
  • 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomography. 
  • 6-[18F]fluoro-A-85380, a novel radioligand for in vivo imaging of central nicotinic acetylcholine receptors. 
  • A simplified method for the measurement of nonmetabolized 2-[18F]F-A-85380 in blood plasma using solid-phase extraction. 
  • Achievement of recommended lipid and lipoprotein levels with combined ezetimibe/statin therapy versus statin alone in patients with and without diabetes. 
  • An update on the IMProved reduction of outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) design. 
  • Assessing the effects of chronic sazetidine-A delivery on nicotine self-administration in both male and female rats. 
  • Baricitinib plus Remdesivir for Hospitalized Adults with Covid-19. 
  • Baricitinib versus dexamethasone for adults hospitalised with COVID-19 (ACTT-4): a randomised, double-blind, double placebo-controlled trial. 
  • Can group medical clinics improve lipid management in diabetes? 
  • Chronic sazetidine-A at behaviorally active doses does not increase nicotinic cholinergic receptors in rodent brain. 
  • Cilofexor, a Nonsteroidal FXR Agonist, in Patients With Noncirrhotic NASH: A Phase 2 Randomized Controlled Trial. 
  • Combination Therapies Including Cilofexor and Firsocostat for Bridging Fibrosis and Cirrhosis Attributable to NASH. 
  • Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement: a phase 2 dose-finding study. 
  • Cost-effectiveness of ximelagatran for stroke prevention. 
  • Costs and effectiveness of ximelagatran for stroke prophylaxis in chronic atrial fibrillation. 
  • Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands. 
  • Differential efficacies of the nicotinic α4β2 desensitizing agents in reducing nicotine self-administration in female rats. 
  • Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. 
  • Effect of extended-release niacin on new-onset diabetes among hyperlipidemic patients treated with ezetimibe/simvastatin in a randomized controlled trial. 
  • Effect of ezetimibe/simvastatin compared with atorvastatin on lipoprotein subclasses in patients with type 2 diabetes and hypercholesterolaemia. 
  • Effect of secondhand smoke on occupancy of nicotinic acetylcholine receptors in brain. 
  • Effectiveness and tolerability of adding ezetimibe to niacin-based regimens for treatment of primary hyperlipidemia. 
  • Effectiveness and tolerability of ezetimibe add-on therapy to a bile acid resin-based regimen for hypercholesterolemia. 
  • Effects of chronic sazetidine-A, a selective α4β2 neuronal nicotinic acetylcholine receptors desensitizing agent on pharmacologically-induced impaired attention in rats. 
  • Effects of ezetimibe, simvastatin and ezetimibe/simvastatin on correlations between apolipoprotein B, LDL cholesterol and non-HDL cholesterol in patients with primary hypercholesterolemia. 
  • Effects of sazetidine-A, a selective alpha4beta2 nicotinic acetylcholine receptor desensitizing agent on alcohol and nicotine self-administration in selectively bred alcohol-preferring (P) rats. 
  • Effects of sazetidine-A, a selective α4β2* nicotinic receptor desensitizing agent, on body temperature regulation in mice and rats. 
  • Effects of the sazetidine-a family of compounds on the body temperature in wildtype, nicotinic receptor β2-/- and α7-/- mice. 
  • Efficacy and safety of alirocumab vs ezetimibe in statin-intolerant patients, with a statin rechallenge arm: The ODYSSEY ALTERNATIVE randomized trial. 
  • Efficacy and safety of alirocumab, a monoclonal antibody to PCSK9, in statin-intolerant patients: design and rationale of ODYSSEY ALTERNATIVE, a randomized phase 3 trial. 
  • Efficacy and safety of ezetimibe co-administered with simvastatin compared with atorvastatin in adults with hypercholesterolemia. 
  • Evaluating cardiovascular event reduction with ezetimibe as an adjunct to simvastatin in 18,144 patients after acute coronary syndromes: final baseline characteristics of the IMPROVE-IT study population. 
  • Evaluation of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine and its analogues as PET radioligands for imaging nicotinic acetylcholine receptors. 
  • Ezetimibe Added to Statin Therapy after Acute Coronary Syndromes. 
  • Ezetimibe plus a Statin after Acute Coronary Syndromes. 
  • Ezetimibe/simvastatin vs atorvastatin in patients with type 2 diabetes mellitus and hypercholesterolemia: the VYTAL study. 
  • Graphical analysis of 2-[18F]FA binding to nicotinic acetylcholine receptors in rhesus monkey brain. 
  • Greater nicotinic acetylcholine receptor density in smokers than in nonsmokers: a PET study with 2-18F-FA-85380. 
  • Impact of short access nicotine self-administration on expression of α4β2* nicotinic acetylcholine receptors in non-human primates. 
  • In vitro characterization of 6-[18F]fluoro-A-85380, a high-affinity ligand for alpha4beta2* nicotinic acetylcholine receptors. 
  • In vivo imaging of brain nicotinic acetylcholine receptors with 5-[123I]iodo-A-85380 using single photon emission computed tomography. 
  • In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. 
  • JAK inhibitor blocks COVID-19 cytokine-induced JAK/STAT/APOL1 signaling in glomerular cells and podocytopathy in human kidney organoids. 
  • Janus kinase inhibitors for atopic dermatitis: a promising treatment modality. 
  • Lack of trophic pancreatic effects in humans with long-term administration of ximelagatran. 
  • Learning to walk before we run: the mechanics of medical intervention for peripheral arterial disease. 
  • Lipid-altering efficacy and safety of ezetimibe/simvastatin coadministered with extended-release niacin in patients with type IIa or type IIb hyperlipidemia. 
  • Lipid-altering efficacy and safety profile of combination therapy with ezetimibe/statin vs. statin monotherapy in patients with and without diabetes: an analysis of pooled data from 27 clinical trials. 
  • Long-term efficacy and safety of ezetimibe/simvastatin coadministered with extended-release niacin in hyperlipidaemic patients with diabetes or metabolic syndrome. 
  • Long-term safety and efficacy of triple combination ezetimibe/simvastatin plus extended-release niacin in patients with hyperlipidemia. 
  • Measurement of the alpha4beta2* nicotinic acetylcholine receptor ligand 2-[(18)F]Fluoro-A-85380 and its metabolites in human blood during PET investigation: a methodological study. 
  • Mutually augmenting interactions of dextromethorphan and sazetidine-A for reducing nicotine self-administration in rats. 
  • NIDA522131, a new radioligand for imaging extrathalamic nicotinic acetylcholine receptors: in vitro and in vivo evaluation. 
  • Novel constructs for thrombin inhibition. 
  • Novel medication targets for the treatment of alcoholism: preclinical studies. 
  • Oral direct thrombin inhibitor ximelagatran compared with warfarin for the prevention of venous thromboembolism after total knee arthroplasty. 
  • Oral sazetidine-A, a selective α4β2* nicotinic receptor desensitizing agent, reduces nicotine self-administration in rats. 
  • Premature release of data from clinical trials of ezetimibe. 
  • Quantification of alpha4beta2* nicotinic receptors in the rat brain with microPET and 2-[18F]F-A-85380. 
  • Quantification of nicotinic acetylcholine receptors in human brain using [123I]5-I-A-85380 SPET. 
  • Quantification of nicotinic acetylcholine receptors in the human brain with PET: bolus plus infusion administration of 2-[18F]F-A85380. 
  • Radiosynthesis and preliminary evaluation of 5-[123/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors. 
  • Rationale and design of IMPROVE-IT (IMProved Reduction of Outcomes: Vytorin Efficacy International Trial): comparison of ezetimbe/simvastatin versus simvastatin monotherapy on cardiovascular outcomes in patients with acute coronary syndromes. 
  • Reducing cardiac events after acute coronary syndromes. 
  • Relationships between metabolic syndrome and other baseline factors and the efficacy of ezetimibe/simvastatin and atorvastatin in patients with type 2 diabetes and hypercholesterolemia. 
  • Safety considerations with gastrointestinally active lipid-lowering drugs. 
  • Sazetidine-A, a selective alpha4beta2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. 
  • Sazetidine-A, a selective α4β2 nicotinic acetylcholine receptor ligand: effects on dizocilpine and scopolamine-induced attentional impairments in female Sprague-Dawley rats. 
  • Study of Heart and Renal Protection (SHARP): randomized trial to assess the effects of lowering low-density lipoprotein cholesterol among 9,438 patients with chronic kidney disease. 
  • Synthesis of C3 heteroatom-substituted azetidinones that display potent cholesterol absorption inhibitory activity. 
  • Therapy and clinical trials. 
  • Up-regulation of nicotinic acetylcholine receptors in menthol cigarette smokers. 
  • Validation of an extracerebral reference region approach for the quantification of brain nicotinic acetylcholine receptors in squirrel monkeys with PET and 2-18F-fluoro-A-85380. 
  • Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjects. 
  • Ximelagatran versus warfarin for the prevention of venous thromboembolism after total knee arthroplasty. A randomized, double-blind trial. 
  • α4β2 Nicotinic receptor desensitizing compounds can decrease self-administration of cocaine and methamphetamine in rats.