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Träfflista för sökning "WFRF:(Dean H) srt2:(2000-2004)"

Sökning: WFRF:(Dean H) > (2000-2004)

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  • Handley, Dean A., et al. (författare)
  • Biological actions of formoterol isomers
  • 2002
  • Ingår i: Pulmonary Pharmacology & Therapeutics. - : Elsevier BV. - 1094-5539 .- 1522-9629. ; 15:2, s. 135-145
  • Tidskriftsartikel (refereegranskat)abstract
    • Racemic β2 agonists, composed of equal amounts of (R)- and (S)-isomers, can display anomalous actions that compromise their effectiveness as asthma therapies. Loss of efficacy during regular use is characteristic of isoprenaline, albuterol and terbutaline and has in part been attributed to the biological effects of the (S)-isomer. This hypothesis was applied to the (R,R)- and (S,S)-isomers of formoterol. (R,R)-formoterol had 1000-times greater affinity (2.9 nm) to the human β2 adrenoceptor than (S,S)-formoterol (3100 nm), with receptor binding modulating intracellular cAMP levels. The minimum lethal intravenous (IV) dose was determined to be 100 mg/kg for (R,R)- and 50 mg/kg for (S,S)-formoterol, suggesting that the toxicity of (S,S)-formoterol may not be related to the binding of β2 adrenoceptors. In tissues pretreated with (S,S)-formoterol but not with (R,R)- or racemic formoterol contractions to high concentrations of carbachol were exaggerated. In vivo experiments with sensitized guinea pigs demonstrated that (R,R)-formoterol inhibited both histamine and antigen-induced bronchoconstriction with greater potency than (R,R/S,S)-formoterol while (S,S)-formoterol was ineffective. Metabolic radiolabeling experiments of (R,R)-, (S,S)- or (R,R/S,S)-formoterol with crude human liver phenolsulfotransferase (PST) determined the Vmax/Km values to be (0.151), (0.74) and (0.143), respectively. The reciprocal plot illustrates a 2-fold reduction in sulfation rate when (R,R)-formoterol is present as a single isomer. The data presented here suggest that (R,R)-formoterol binds to the β2 adrenoceptor and inhibits the contraction of bronchial tissues by spasmogens. However, (S,S)-formoterol exhibits properties inconsistent as an asthma therapeutic and may antagonize the actions of (R,R)-formoterol.
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  • Lipoglavsek, M., et al. (författare)
  • First Observation of Excitation Across the 100Sn Core
  • 2001
  • Ingår i: Nuclear Physics, Section A. - 0375-9474. ; 682, s. 399-403
  • Tidskriftsartikel (refereegranskat)abstract
    • Excited states of nuclei near the doubly-magic nucleus Sn-100 were studied with the Ni-58+Cr-50 reaction. The experimental setup consisted of the GAMMASPHERE array augmented with light charged-particle and neutron detectors. Excited states were identified for the first time in the proton emitting nucleus Sb-105. Excitations across the N=Z=50 doubly closed shell were observed in Cd-99 and In-101. Some results of large-scale shell-model calculations are discussed.
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  • Resultat 1-7 av 7

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