Refeeding activates neurons in the dorsomedial hypothalamus to inhibit food intake and promote positive valence.

Objective: The regulation of food intake is a major research area in the study of obesity, which plays a key role in the development of metabolic syndrome. Gene targeting studies have clarified the roles of hypothalamic neurons in feeding behavior, but the deletion of a gene has a long-term effect on neurophysiology. Our understanding of short-term changes such as appetite under physiological conditions is therefore still limited.

Prostaglandin in the ventromedial hypothalamus regulates peripheral glucose metabolism.

The hypothalamus plays a central role in monitoring and regulating systemic glucose metabolism. The brain is enriched with phospholipids containing poly-unsaturated fatty acids, which are biologically active in physiological regulation. Here, we show that intraperitoneal glucose injection induces changes in hypothalamic distribution and amounts of phospholipids, especially arachidonic-acid-containing phospholipids, that are then metabolized to produce prostaglandins.

8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists.

Structure-activity relationships of 2-alkynyladenine derivatives were explored by varying substituents at the 9-, 8- and 2-positions of the purine moiety in order to optimize A2A adenosine receptor antagonist activity in vitro. A propargyl group at the 9-position was found to be important for A2A antagonist activity, and the introduction of a halogen, aryl, or heteroaryl at the 8-position further enhanced activity. A series of 8-substituted 2-alkynyl-N(9)-propargyladenine derivatives exhibited potent antagonist activity, with IC50 values in the low nM range.

The influence of water on the stability of lyophilized formulations with inositol and mannitol as excipients.

The stability of a moisture-sensitive drug in lyophilized products was investigated under conditions with varying water content and temperature using two model formulations: a formulation containing inositol (IF) as the excipient and a formulation containing mannitol (MF) as the excipient. IF showed better chemical stability (a lower hydrolysis rate) than MF when both formulations contained 2% water. However, in the case of formulations with 8% water, MF showed similar or better stability than IF.

Investigation of intermolecular interaction in molecular complex of tryptamine and benzoic acid by solid-state 2D NMR.

Solid-state NMR spectra and powder X-ray diffraction of the two-component molecular complex composed of tryptamine and benzoic acid were observed to investigate the intermolecular interaction in the molecular complex. 1D (13)C CP/MAS NMR spectrum and powder X-ray diffraction pattern of the complex was clearly different from the convolution of each spectrum of the single component. 2D (1)H-(13)C heteronuclear-correlation (HETCOR) NMR technique indicated that the intermolecular interaction between the primary amine of tryptamine and the carboxyl group of benzoic acid must be related to the complex formation.