The sympathetic nervous system plays a central role in the pathophysiology not only of hypertension and other cardiovascular diseases but also metabolic disorders including disturbances of glucose and lipid homeostasis. A centrally acting sympathetic agent is therefore attractive not only for lowering blood pressure, but also intervening with multiple disease processes. Older agents such as clo...

The agonists of imidazoline I-1 receptors (I-1R) are widely used to lower blood pressure. It has been indicated that guanidinium derivatives show an ability to activate imidazoline receptors. Also, allantoin has a chemical stricture similar to guanidinium derivatives. Thus, it is of special interest to characterize the effect of allantoin on I-1R. In conscious male spontaneous hypertensive rats...

TAARs (trace amine-associated receptors) are G-protein-coupled receptors that respond to low abundance, endogenous amines such as tyramine and tryptamine, and represent potential targets for neuropsychiatric diseases. However, some members of this receptor subfamily either have no ligand identified or remain difficult to express and characterize using recombinant systems. In the present paper w...

An integrated online screening system was developed to rapidly screen homogeneous catalysts for activity toward a selected synthesis. The continuous-flow system comprises standard HPLC pumps for the delivery of substrates, an HPLC autosampler for the injection of homogeneous catalysts, a thermostated reactor to mediate synthesis, and a single-stage quadrupole mass spectrometer (MS) equipped wit...

Calluses from two ecotypes of reed (Phragmites communis Trin.) plant (dune reed [DR] and swamp reed [SR]), which show different sensitivity to salinity, were used to study plant adaptations to salt stress. Under 200 mm NaCl treatment, the sodium (Na) percentage decreased, but the calcium percentage and the potassium (K) to Na ratio increased in the DR callus, whereas an opposite changing patter...

Under controlled conditions the effects of various "sympatholytic" agents on the cardiovascular responses to epinephrine and norepinephrine were compared in man. The dosages of the sympatholytic drugs administered approximated those usually employed clinically. Such basic data are given for the following agents: Dibenamine, the imidazoline derivatives [Priscoline and Regitine (C-7337)], the dih...

Under controlled conditions the effects of various “sympatholytic” agents on the cardiovascular responses to epinephrine and norepinephrine were compared in man. The dosages of the sympatholytic drugs administered approximated those usually employed clinically. Such basic data are given for the following agents: Dibenamine, the imidazoline derivatives [Priscoline and Regitine (C-73i)], the dihy...

Six novel imidazoline derivatives were synthesized and tested in antifungal assays. One of the compounds, N-cyclohexyl-2-imino-3-(4-nitrophenyl)imidazolidine-1-carboxamide showed moderate activity against several clinical strains of Candida albicans. Its structure was solved by X-ray crystallography and its mode of action was deduced using molecular modelling. It was found to be similar to that...

Under controlled conditions the effects of various "sympatholytic" agents on the cardiovascular responses to epinephrine and norepinephrine were compared in man. The dosages of the sympatholytic drugs administered approximated those usually employed clinically. Such basic data are given for the following agents: Dibenamine, the imidazoline derivatives [Priscoline and Regitine (C-7337)], the dih...

Human semicarbazide-sensitive amine oxidase (SSAO) is a target for novel anti-inflammatory drugs that inhibit enzymatic activity. However, progress in developing such drugs has been hampered by an incomplete understanding of mechanisms involved in substrate turnover. We report here results of a comparative study of human and bovine SSAO enzymes that reveal binding of substrates and other ligand...