Heteronuclear NMR in combination with isotope labelling is used to study folding of polypeptides induced by metals the case metallothioneins, binding peptidic allosteric modulator ?-TIA human G-protein coupled ?1b adrenergic receptor, development therapeutic drugs that interfere biosynthesis outer membrane Gram-negative bacteria, and a system which protein assembly upon peptide addition. these ...

Administration of enantiomerically pure β-adrenergic agonists and antagonists increases their activity and reduces side effects. We report here a small-molecule artificial receptor (SMAR) that, by mimicking the β-adrenergic receptor, is able to enantioselectively extract commercial β-adrenergic interacting drugs. The selectivity is justified according to DFT calculations and X-ray diffraction e...

The ability of topical timolol and epinephrine to decrease the 0-adrenergic responsiveness of the cornea and iris-ciliary body of albino and pigmented rabbits is reported. The time course of the decrease in responsiveness was determined by comparing in vitro, /?-adrenergic stimulated cyclic AMP synthesis in these tissues from in vivo drug treated and contralateral, untreated eyes. In the cornea...

Background and objectives: Pain is a primarily protective in nature, but often causes discomfort. Currently available analgesic drugs are not useful in all cases due to their side effects. Medicinal plants are believed to be an important source of new chemical substances with potential therapeutic effects, such as, Teucrium polium (TP) used traditionally to relieve hea...

In this study the effect of adrenergic receptor agonists and antagonists on physostigmine induced yawning was investigated. Intraperitoneal injection of different doses of physostigmine (0.03, 0.05, 0.1 and 0.2 mg/kg) caused yawning in white rats. The greatest response was seen at a dose of 0.2 mg/kg physostigmine. Phenylephrine, an α1 agonist, and clonidine, an α2 agonist, led to a decrease in...

The effects of endogenous and of exogenous norepinephrine were studied in isolated rings of canine left circumflex coronary artery and its first ventricular branch. Norepinephrine was released from adrenergic nerve endings by transmural electrical stimulation and by tyramine. In rings contracted with prostaglandin F2 alpha, transmural electrical stimulation resulted in frequency-dependent relax...

beta-Adrenergic receptors play a critical role in signal transduction in the cardiovascular system. Regulation of beta-adrenergic receptor expression depends on multiple factors, including rates of synthesis and degradation of receptor protein and trafficking of receptors between the cell surface and putative intracellular compartments. To characterize the subcellular distribution of beta-adren...

Discontinuous density sucrose gradient centrifugation was used to isolate membrane vesicles from the left ventricle of three normal subjects (one prospective organ donor and two traffic victims whose hearts were obtained 1 hour after death) and nine patients undergoing cardiac transplantation as a consequence of idiopathic dilated cardiomyopathy. Sarcolemma-enriched subcellular fractions, detec...

OBJECTIVE We tested the hypothesis that adrenergic activation, cholinergic activation, or both, mediate the effect of recent antecedent hypoglycemia to reduce the sympathoadrenal response to subsequent hypoglycemia, the key feature of hypoglycemia-associated autonomic failure in diabetes, in humans. RESEARCH DESIGN AND METHODS Seventeen healthy adults were studied on 2 consecutive days on thr...

To elucidate the mechanisms responsible for the increase in alpha 1-adrenergic receptors during ischemia in vivo, we developed a procedure for measuring alpha 1-adrenergic receptors in isolated, calcium-tolerant adult canine myocytes. Specific [3H]prazosin binding was rapid, saturable, reversible, and demonstrated the expected order of potency and stereospecificity for the alpha 1-adrenergic re...