Pyrrolidines

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  Subject Areas on Research

  • 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. 
  • 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. 
  • A phase I-II study of docetaxel and atrasentan in men with castration-resistant metastatic prostate cancer. 
  • A randomized proof-of-mechanism trial applying the 'fast-fail' approach to evaluating κ-opioid antagonism as a treatment for anhedonia. 
  • A thalamocorticostriatal dopamine network for psychostimulant-enhanced human cognitive flexibility. 
  • Activation of kappa opioid receptors by U50488H and morphine enhances the release of substance P from rat trigeminal nucleus slices. 
  • Activation state of the M3 muscarinic acetylcholine receptor modulates mammalian odorant receptor signaling. 
  • Activity of Galidesivir in a Hamster Model of SARS-CoV-2. 
  • Acute effects of the selective cholinergic channel activator (nicotinic agonist) ABT-418 in Alzheimer's disease. 
  • Addendum to Letter to the Editor: Safety, efficacy, and authorization of eliglustat as a first-line therapy in Gaucher disease type 1. 
  • Advanced prostate cancer: the future. 
  • An update on the progress of galidesivir (BCX4430), a broad-spectrum antiviral. 
  • Anti-estrogenic compounds increase prolactin and growth hormone synthesis in clonal strains of rat pituitary cells. 
  • Associations between dopamine D2 receptor availability and BMI depend on age. 
  • Bepridil and cetiedil. Vasodilators which inhibit Ca2+-dependent calmodulin interactions with erythrocyte membranes. 
  • Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity. 
  • Bioavailabilities of rectal and oral methadone in healthy subjects. 
  • Calcium-independent phospholipase A2 participates in KCl-induced calcium sensitization of vascular smooth muscle. 
  • Chronic administration of U50,488H fails to produce hypothalamo-pituitary-adrenal axis tolerance in neonatal rats. 
  • Clinical pharmacology of an atrasentan and docetaxel regimen in men with hormone-refractory prostate cancer. 
  • Comparative toxicity of kainic acid and other acidic amino acids toward rat hippocampal neurons. 
  • Cupric-amyloid beta peptide complex stimulates oxidation of ascorbate and generation of hydroxyl radical. 
  • Daclatasvir in combination with asunaprevir and beclabuvir for hepatitis C virus genotype 1 infection with compensated cirrhosis. 
  • Degeneration of hippocampal CA3 pyramidal cells induced by intraventricular kainic acid. 
  • Detection of previously unidentified metastatic disease as a leading cause of screening failure in a phase III trial of zibotentan versus placebo in patients with nonmetastatic, castration resistant prostate cancer. 
  • Differences in the absorption, metabolism and biliary excretion of a diastereomeric pair of alphavbeta3-antagonists in rat: limited role of P-glycoprotein. 
  • Disposition of nasal, intravenous, and oral methadone in healthy volunteers. 
  • Early ontogeny of kappa-opioid receptor regulation of prolactin secretion in the rat. 
  • Effect of hippocampal lesions produced by intracerebroventricular kainic acid on alcohol drinking in the rat. 
  • Effect of the nitric oxide donor V-PYRRO/NO on portal pressure and sinusoidal dynamics in normal and cirrhotic mice. 
  • Effects of TNFalpha on expression of ICAM-1 in human airway epithelial cells in vitro: oxidant-mediated pathways and transcription factors. 
  • Effects of specific mu and kappa opiate tolerance and abstinence on hypothalamo-pituitary-adrenal axis secretion in the rat. 
  • Eight Weeks of Treatment With Glecaprevir/Pibrentasvir Is Safe and Efficacious in an Integrated Analysis of Treatment-Naïve Patients With Hepatitis C Virus Infection. 
  • Eliglustat maintains long-term clinical stability in patients with Gaucher disease type 1 stabilized on enzyme therapy. 
  • Endothelin receptor blockade during hypothermic perfusion preservation mitigates the adverse effect of preretrieval warm ischemic injury on posttransplant glomerular filtration rate. 
  • Endothelin-receptor blockade mitigates the adverse effect of preretrieval warm ischemia on posttransplantation renal function in rats. 
  • Endotoxin stress-response in cardiomyocytes: NF-kappaB activation and tumor necrosis factor-alpha expression. 
  • 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. 
  • Evidence from lesion studies for epileptogenic and non-epileptogenic neurotoxic interactions between kainic acid and excitatory innervation. 
  • Evidence of functional mossy fiber sprouting in hippocampal formation of kainic acid-treated rats. 
  • FTO affects food cravings and interacts with age to influence age-related decline in food cravings. 
  • Fate of the hippocampal mossy fiber projection after destruction of its postsynaptic targets with intraventricular kainic acid. 
  • Female steroid hormones and lipoprotein synthesis in the cockerel: effects of progesterone and nafoxidine on the estrogenic stimulation of very low density lipoproteins (VLDL) synthesis. 
  • Fixed-dose combination therapy with daclatasvir, asunaprevir, and beclabuvir for noncirrhotic patients with HCV genotype 1 infection. 
  • Fluorine-18 Labeling of the MDM2 Inhibitor RG7388 for PET Imaging: Chemistry and Preliminary Evaluation. 
  • Glecaprevir and pibrentasvir yield high response rates in patients with HCV genotype 1-6 without cirrhosis. 
  • Gold(I)-catalyzed intramolecular amination of allylic alcohols with alkylamines. 
  • Increases in cortical glutamate concentrations in transgenic amyotrophic lateral sclerosis mice are attenuated by creatine supplementation. 
  • Induction of bladder sphincter dyssynergia by kappa-2 opioid receptor agonists in the female rat. 
  • Inhibition of the transcriptional activator protein nuclear factor kappaB prevents hemodynamic instability associated with the whole-body inflammatory response syndrome. 
  • Intraventricular kainic acid preferentially destroys hippocampal pyramidal cells. 
  • Kainic acid lesioning of alkaloid-sensitive brain sites and ethanol ingestion in the rat. 
  • Kainic acid neurotoxicity toward hippocampal formation: dependence on specific excitatory pathways. 
  • Kainic acid: neurophysiological and neurotoxic actions. 
  • Loss and reacquisition of hippocampal synapses after selective destruction of CA3-CA4 afferents with kainic acid. 
  • Microfluidic chip with electrochemiluminescence detection using 2-(2-aminoethyl)-1-methylpyrrolidine labeling. 
  • Minireview. Kainic acid as a tool for the study of temporal lobe epilepsy. 
  • Mu- and kappa-opiate receptor control of prolactin secretion in rats: ontogeny and interaction with serotonin. 
  • Muscarinic acetylcholine receptor M3 modulates odorant receptor activity via inhibition of β-arrestin-2 recruitment. 
  • NF-kappaB p65 involves in reperfusion injury and iNOS gene regulation in skeletal muscle. 
  • New Treatment Options for Hepatitis C Virus Infection in End-Stage Kidney Disease: To Treat or Not to Treat. 
  • Nitric oxide-releasing silica nanoparticle inhibition of ovarian cancer cell growth. 
  • Ontogeny of mu- and kappa-opiate receptor control of the hypothalamo-pituitary-adrenal axis in rats. 
  • Optimal Timing of Administration of Direct-acting Antivirals for Patients With Hepatitis C-associated Hepatocellular Carcinoma Undergoing Liver Transplantation. 
  • Oral platelet glycoprotein IIb/IIIa inhibition. 
  • Patient engagement and study design of PROP UP: A multi-site patient-centered prospective observational study of patients undergoing hepatitis C treatment. 
  • Phase 1 study of TAS-102 administered once daily on a 5-day-per-week schedule in patients with solid tumors. 
  • Phase 3, randomized, placebo-controlled study of zibotentan (ZD4054) in patients with castration-resistant prostate cancer metastatic to bone. 
  • Phase I clinical study of three times a day oral administration of TAS-102 in patients with solid tumors. 
  • Phase I study to determine the safety and pharmacokinetics of oral administration of TAS-102 in patients with solid tumors. 
  • Phase III, randomized, placebo-controlled study of docetaxel in combination with zibotentan in patients with metastatic castration-resistant prostate cancer. 
  • Polymeric coatings on silver nanoparticles hinder autoaggregation but enhance attachment to uncoated surfaces. 
  • Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder. 
  • RNA-Seq and ChIP-Seq reveal SQSTM1/p62 as a key mediator of JunB suppression of NF-κB-dependent inflammation. 
  • Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[(11)C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography. 
  • Real-world effectiveness of eliglustat in treatment-naïve and switch patients enrolled in the International Collaborative Gaucher Group Gaucher Registry. 
  • Recommendations for the use of eliglustat in the treatment of adults with Gaucher disease type 1 in the United States. 
  • Reduced kainic acid binding in rat hippocampal formation after limbic kindling. 
  • Regional distribution of [3H]kainic acid after intraventricular injection. 
  • Role of excitatory pathways in the hippocampal damage produced by kainic acid. 
  • Safety, efficacy, and authorization of eliglustat as a first-line therapy in Gaucher disease type 1. 
  • Simplified monitoring for hepatitis C virus treatment with glecaprevir plus pibrentasvir, a randomised non-inferiority trial. 
  • Spontaneous Eye Blink Rate (EBR) Is Uncorrelated with Dopamine D2 Receptor Availability and Unmodulated by Dopamine Agonism in Healthy Adults. 
  • Stereoselective determination of methadone and the primary metabolite EDDP in human plasma by automated on-line extraction and liquid chromatography mass spectrometry. 
  • Striatal dopamine D2/D3 receptor availability in male smokers. 
  • Suppression of food intake by glucagon-like peptide-1 receptor agonists: relative potencies and role of dipeptidyl peptidase-4. 
  • Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors. 
  • Synthesis of isomeric 3-piperidinyl and 3-pyrrolidinyl benzo[5,6]cyclohepta[1,2-b]pyridines: sulfonamido derivatives as inhibitors of Ras prenylation. 
  • TP53 wild-type/PPM1D mutant diffuse intrinsic pontine gliomas are sensitive to a MDM2 antagonist. 
  • TRIPSTAR: prioritizing oral triptan treatment attributes in migraine management. 
  • Tepoxalin enhances the activity of an antioxidant, pyrrolidine dithiocarbamate, in attenuating tumor necrosis factor alpha-induced apoptosis in WEHI 164 cells. 
  • The glutamate transport inhibitor L-trans-pyrrolidine-2,4-dicarboxylate indirectly evokes NMDA receptor mediated neurotoxicity in rat cortical cultures. 
  • To oxidize or not to oxidize? 
  • Treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin improves fasting islet-cell function in subjects with type 2 diabetes. 
  • V-PYRRO/NO: an hepato-selective nitric oxide donor improves porcine liver hemodynamics and function after ischemia reperfusion. 
  • Vernakalant hydrochloride for rapid conversion of atrial fibrillation: a phase 3, randomized, placebo-controlled trial. 
  • Voltage-dependent effects of opioid peptides on hippocampal CA3 pyramidal neurons in vitro. 
  • mu-Opioid agonists stimulate growth hormone secretion in immature rats. 
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  Keywords of People

  • Bennett, Vann, George Barth Geller Distinguished Professor of Molecular Biology, Duke Cancer Institute