In insulin-producing cells of the RINm5F line, the nonmetabolized analogue of L-leucine, 2-aminobicyclo[2,2,1]heptane-2-carboxylic acid decreases O2 consumption, lowers ATP content, and inhibits insulin release despite stimulation of both NH4 production and 14CO2 output from cells prelabeled with L-[U-14C]glutamine. The metabolic and secretory effects of 2-aminobicyclo[2,2,1]heptane-2-carboxyli...

The anorexigen (+)-fenfluramine was used for treatment of obesity until the association of use with valvular heart disease and primary pulmonary hypertension. (+)-Fenfluramine has been found in Chinese and Korean slimming pills. The hepatic metabolite of (+)-fenfluramine, (+)-norfenfluramine, has affinity for 5-hydroxytryptamine (5-HT)(2A) and 5-HT(2B) receptors. We tested the hypothesis that (...

1. 4-Amino-7-hydroxy-2-methyl-5,6,7,8,-tetrahydrobenzo[b]thieno[2,3-b]pyrid ine-3-carboxylic acid, but-2-ynyl ester (SB-205384) and other gamma-aminobutyric acid(A) (GABA(A)) receptor modulators were tested for their effects on GABA-activated chloride currents in rat cerebellar granule cells by use of the whole-cell patch clamp technique. 2. The major effect of SB-205384 on GABA(A)-activated cu...

In insulin-producing cells of the RINmSF line, the nonmetabolized analogue of i.-leucine, 2-aminobicyclo|2,2,1 |heptane-2-carboxylic acid de creases <), consumption, lowers ATP content, and inhibits insulin release despite stimulation of both Ml, production and "(<)., output from cells prelabeled with L-|i/-uC]glutamine. The metabolic and secretory effects of 2-aminobicyclo|2,2,l|heptane-2-carb...

There are only a few studies of noncovalent association in fluorous solvents and even fewer that are quantitative. A full understanding, particularly of stoichiometry and binding strength of noncovalent interactions in fluorous solvents could be very useful in improved molecular-receptor-based extractions, advancements in sensor technologies, crystal engineering, and supramolecular chemistry. T...

In a screening for antifungal metabolites, two indole compounds of mixed biogenesis, 1H-indole-3-carboxylic acid, 1-(1,1-dimethyl-2-propenyl) methyl ester and 1H-indole-3-carboxylic acid, 1-(2,3-dihydroxy-1,1-dimethylpropyl) methyl ester were isolated from a culture of the basidiomycete Aporpiums caryae. The structural elucidation of these compounds was accomplished by spectroscopic methods.

Azetidine-2-carboxylic acid has been recognized as an important constituent of the 70% ethanolsoluble-nitrogen fraction of many liliaceous plants (Fowden, 1956; Fowden & Steward, 1957). ConvaUaria majali8 (lily of the valley) and Polygonatum multiflorum (a Solomon's seal) are two common representatives of these plants im Britain, and part 6 of this series (Fowden & Bryant, 1959) described exper...

5-Phenyl-furan-2-carboxylic acids have emerged as a new, promising class of antimycobacterial agents that the ability to interfere with iron homeostasis. Considering lack structural data on these compounds, we analyzed crystal fluorinated ester derivative 5-(4-nitrophenyl)furan-2-carboxylic acid, one most potent candidates in series. Here, describe preparation methyl 5-(2-fluoro-4-nitrophenyl)f...