Characterization by Scanning Precession Electron Diffraction of an Aggregate of Bridgmanite and Ferropericlase Deformed at HP-HT.

Scanning precession electron diffraction is an emerging promising technique for mapping phases and crystal orientations with short acquisition times (10-20 ms/pixel) in a transmission electron microscope similarly to the Electron Backscattered Diffraction (EBSD) or Transmission Kikuchi Diffraction (TKD) techniques in a scanning electron microscope. In this study, we apply this technique to the characterization of deformation microstructures in an aggregate of bridgmanite and ferropericlase deformed at 27 GPa and 2,130 K. Such a sample is challenging for microstructural characterization for two reasons: (i) the bridgmanite is very unstable under electron irradiation, (ii) under high stress conditions, the dislocation density is so large that standard characterization by diffraction contrast are limited, or impossible. Here we show that detailed analysis of intracrystalline misorientations sheds some light on the deformation mechanisms of both phases. In bridgmanite, deformation is accommodated by localized, amorphous, shear deformation lamellae whereas ferropericlase undergoes large strains leading to grain elongation in response to intense dislocation activity with no evidence for recrystallization. Plastic strain in ferropericlase can be semiquantitatively assessed by following kernel average misorientation distributions.

Bioisosteres of 9-carboxymethyl-4-oxo-imidazo[1,2-a]indeno-[1,2-e]pyrazin-2-carboxylic acid derivatives. Progress towards selective, potent in vivo AMPA antagonists with longer durations of action.

A novel series of 2- and 9-disubstituted heterocyclic-fused 4-oxo-indeno[1,2-e]pyrazin derivatives was synthesized. One of them, the 9-(1H-tetrazol-5-ylmethyl)-4-oxo-5,10-dihydroimidazo[1,2-a]indeno[1,2-e]pyrazin-2-yl phosphonic acid 4i exhibited a strong and a selective binding affinity for the AMPA receptor (IC50 = 13 nM) and demonstrated potent antagonist activity (IC50 = 6nM) at the ionotropic AMPA receptor. This compound also displayed good anticonvulsant properties against electrically-induced convulsions after ip and iv administration with ED50 values between 0.8 and 1 mg/kg. Furthermore, a strong increase in potency was observed when given iv 3 h before test (ED50 = 3.5 instead of 25.6 mg/kg for the corresponding 9-carboxymethyl-2-carboxylic acid analogue). These data confirmed that there is an advantage in replacing the classical carboxy substituents by their bioisosteres such as tetrazole or phosphonic acid groups.