9 research outputs found

    Influence of various concentrations of 24-epibrassinolide on the kinetic parameters during isothermal dehydration of two maize hybrids

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    24-epibrassinolide (24-EBL) is plant steroid hormone that can regulate several physiological effects in plants, including promotion of cell growth and induction of heat stress tolerance. The purpose of this work is to investigate the influence of various concentrations of 24-EBL on the dehydration mechanism of seedlings of two maize hybrids (ZP434 and ZP704). Control and treated samples were subjected to isothermal conditions for dehydration processes. The effects of carbohydrates and mineral contents on the possible changes in the dehydration mechanism (from kinetics standpoint) were investigated. Comparing control samples to samples treated with 24-EBL, it was found that different dehydration mechanisms exist. The differences arise from the influence of 24-EBL, that causes a significant increase of phosphorus values for ZP704, whilst the reverse was identified for ZP434. It was assumed that the plumule sensitivity to dehydration stress originates from the interaction of water with primary amino groups as cations in polyamines, for lower concentrations of 24-EBL. It was found that the temperature variation (105ā€“130 Ā°C) leads to situations where trehalose does not arrive fast enough to ā€œreplace the waterā€ because its handicap to binds (by hydrogen bonds) to biomolecules instead of water. It was found that 24-EBL cause changes of carbohydrates properties, which are important for the defense mechanism from environmental stresses. Ā© 2018 SAABSupplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3014

    Evaluation of MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human

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    Antagonism of the central opioid receptor like-1 receptor (ORL1) has been implicated in cognition, and has been a focus of drug discovery efforts to ameliorate the cognitive deficits that remain during the stable treatment of schizophrenia with current antipsychotics. In order to facilitate dose selection for phase II clinical testing an ORL1-specific PET tracer was developed to determine drug plasma concentration versus occupancy relationships in order to ensure that the doses selected and the degree of target engagement were sufficient to ensure adequate proof of concept testing. MK-0911 is a selective, high affinity antagonist for the ORL1 receptor radiolabeled with high specific activity (18)F for positron emission tomography (PET) studies. Evaluation of [(18)F]MK-0911 in rhesus monkey PET studies showed a pattern of brain uptake which was consistent with the known distribution of ORL1. In vitro autoradiography with [(18)F]MK-0911 in rhesus monkey and human brain tissue slices showed a regional distribution that was consistent with in vivo imaging results in monkey. Pre-treatment of rhesus monkeys with high doses of structurally diverse ORL1 antagonists MK-0584, MK-0337, or MK-5757 achieved blockade of [(18)F]MK-0911 in all gray matter regions. Baseline PET studies with [(18)F]MK-0911 in healthy human subjects showed tracer distribution and kinetics similar to that observed in rhesus monkey. Quantification of [(18)F]MK-0911 uptake in repeat human baseline PET studies showed a test-retest variability in volume of distribution (V(T)) averaging 3% across brain regions. Humans dosed orally with MK-5757 showed reduced [(18)F]MK-0911 tracer concentration in brain proportional with MK-5757 dose and plasma level. [(18)F]MK-0911 was useful for determining MK-5757-induced receptor occupancy of ORL1 to guide MK-5757 dose-selection for clinical proof-of-concept studies. Additionally, [(18)F]MK-0911 may be a useful tool for studying the pharmacology of ORL1 in various human populations and disease states.publisher: Elsevier articletitle: Evaluation of [18F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human journaltitle: NeuroImage articlelink: http://dx.doi.org/10.1016/j.neuroimage.2012.11.053 content_type: article copyright: Copyright Ā© 2012 Elsevier Inc. All rights reserved.status: publishe
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