Biomedical sciences publications
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Nociceptin/Orphanin FQ Inhibition with SB612111 Ameliorates Dextran Sodium Sulfate-Induced Colitis
In this study, we asked whether the small molecule N/OFQ antagonist (−)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB612111) would inhibit the development of dextran sodium sulfate-induced colitis in C57BL/6 mice.
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Radiosynthesis of a 125I Analog of a Highly Selective Alpha3beta4 Nicotinic Acetylcholine Receptor Antagonist Ligand for Use in Autoradiography Studies
Our laboratory has discovered a series of very high affinity and highly selective ligands for the α3β4 nAChR subtype. We now report the synthesis of a radiolabeled 125I analog of N-(2-iodophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine (AT-1012), a…
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Effects of Bacterial and Presystemic Nitroreductase Metabolism of 2-Chloro-5-Nitro-N-Phenylbenzamide on its Mutagenicity and Bioavailability
Studies were initiated to assess its bacterial mutagenicity and pharmacokinetic profile in two animal species prior to subchronic oral toxicity evaluations and the results are reported here.
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Evaluation of Arylimidamides DB1955 and DB1960 as Candidates Against Visceral Leishmaniasis and Chagas’ Disease: In Vivo Efficacy, Acute Toxicity, Pharmacokinetics, and Toxicology Studies
These two mesylate salts exhibited dose-dependent activity in the murine model of VL, with DB1960 inhibiting liver parasitemia and DB1955 reducing liver parasitemia.
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N-Glycan Cryptic Antigens as Active Immunological Targets in Prostate Cancer Patients
We report here a carbohydrate microarray analysis of a number of tumor-associated carbohydrates for their serum antibody reactivities and potential immunogenicity in humans
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Heightened Awareness in Insomnia
... investigate the possibility of hyperarousal in insomnia leading to the possibility of conscious awareness occurring in the context of what we have traditionally viewed to be EEG evidence of…
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Synthesis of 14C-Acanthoic Acid
14C-Acanthoic acid was prepared in four steps by a degradation/reconstitution strategy.
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Lead Optimization of 3-Carboxyl-4(1 H)-Quinolones to Deliver Orally Bioavailable Antimalarials
Herein, we report the lead optimization of 4(1H)-quinolones with a focus on improving both antimalarial potency and bioavailability.
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Design Considerations for Liposomal Vaccines: Influence of Formulation Parameters on Antibody and Cell-Mediated Immune Responses to Liposome Associated Antigens
We present a comprehensive review of the physicochemical properties of liposomal vaccines and how they influence immune responses. A discussion of novel and emerging immunomodulators that are suitable for inclusion…
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Nicotine Reduces Antipsychotic-Induced Orofacial Dyskinesia in Rats
In this study, we investigated whether nicotine administration could reduce tardive dyskinesia because nicotine attenuates other drug-induced abnormal movements.
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Thermodynamics and Docking of Agonists to the β 2- Adrenoceptor Determined Using [ 3H](R,R′)-4-Methoxyfenoterol as the Marker Ligand
To better understand the molecular interactions of fenoterol analogs with the β2-adrenergic receptor, we developed a new agonist radioligand for binding assays.
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Ionizing Radiation Regulates the Expression of AMP-Activated Protein Kinase (AMPK) in Epithelial Cancer Cells: Modulation of Cellular Signals Regulating Cell Cycle and Survival
Purpose:To analyze the expression of AMPK in a variety of epithelial cancer cells, regulation of AMPK subunit expression by ionizing radiation and impact of AMPK on signaling pathways regulating cell…