The N-methyl-D-aspartate (NMDA) class of excitatory amino acid receptors regulates the strength and stability of excitatory synapses and appears to play a major role in excitotoxic neuronal death associated with stroke and epilepsy. The conductance increase gated by NMDA is potentiated by the amino acid glycine, which acts at an allosteric site tightly coupled to the NMDA receptor. Indole-2-car...

Mechanistic investigations have shown that, upon agonist activation, hydroxy-carboxylic acid receptor-1(HCA1) couples to a Gi protein and inhibits adenylate cyclase activity, leading to inhibition of liberation of free fatty acid. However, the underlying molecular mechanisms for HCA1 signaling remain largely unknown. Using CHO-K1 cells stably expressing HCA1, and L6 cells, which endogenously ex...

Anionic polyurethane dispersants APUDs were used as dispersing agents in formulation of waterborne paints. The APUDs were synthesized by three steps. In the first step, macromonomer diisocyanate having carboxylic acid was prepared by isophorone diisocyanate IPDI, dimethylol propionic acid DMPA in presence of acetone as solvent and dibutyltin dilaurate DBTDL as catalyst. Then, carboxylic polyure...

Prostaglandin (PG) E2 binds to PGE receptor EP3 subtype and induces Gi activity. To assess the role of the interaction of the carboxylic acid group of agonists and its putative binding site, Arg-309 in the seventh transmembrane domain of EP3alpha receptor, in receptor activation, we have mutated the positively charged Arg-309 to the polar but uncharged Gln (EP3alpha-R309Q) and Asn (EP3alpha-R30...

2,3,4,7-Tetrahydro-1H -inden-2-ol (1) has been synthesised by Birch reduction of indan-2-ol. A single-crystal X-ray structur analysis of 1 shows the compound to exist as hydrogen-bonded polymers along the c-axis due to the presence of a series of hydrogen bonds between hydroxo functions. The ferrocene ester derivatives, ferrocene carboxylic acid 2,3,4,7-tetrahydro-1H -inden-2-yl este (2) and fe...

Protaetia brevitarsis seulensis (Kolbe) has been temporarily registered as a food material by the Ministry of Food and Drug Safety of Korea (MFDS). The current study aimed to discover small antithrombotic molecules from this edible insect. Five indole alkaloids, 5-hydroxyindolin-2-one (1), (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (2), (1S,3S)-1-methyl-1,2,3,4-tetrahydro...

Angiotensin-converting enzyme inhibitors limit infarct size in animal models of myocardial ischemia reperfusion injury. This effect has been shown to be due to inhibition of bradykinin degradation rather than inhibition of angiotensin II formation. The purpose of this study was to determine whether angiotensin AT1 receptor blockade by losartan or its active metabolite EXP3174 protects against m...