The first enantioselective organocatalytic hydride reduction has been accomplished. The use of iminium catalysis has provided a new organocatalytic strategy for the enantioselective reduction of beta,beta-substituted alpha,beta-unsaturated aldehydes to generate beta-stereogenic aldehydes. The use of imidazolidinone 2 as the asymmetric catalyst has been found to mediate the transfer of hydrogen ...

timolol is a non-selective beta-adrenergic receptor antagonist administered for treating glaucoma, heart attacks and hypertension. in the present study, we set out to determine whether or not timolol can provoke cataract formation, thus the influence of timolol on the amyloid-type aggregation of crystallin was investigated. we then provided experimental evidence of crystallin aggregation and it...

a case of acute extrapyramidal manifestations consisting of dystonia and akathisia following abrupt discontinuation of propranolol is reported. she responded well to oral propranolol and intramuscular diazepam. extrapyramidal symptoms have commonly been associated with acute or chronic administration of neuroleptic drugs. there have been reports of a substantial number of cases with similar cli...

Dorsal root ganglion (DRG) neurons can be categorised into at least three types, based upon their neurotrophin requirement for survival. We have analysed the expression of the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs) in NGF, NT-3 and BDNF dependent neurons isolated from embryonic day (E)13.5 mouse DRG. We show that each population of neurons expressed each of the three...

Thyroid hormone (triiodothyronine, T(3)) is known to activate transcription by binding heterodimers of thyroid hormone receptors (TRs) and retinoid X receptors (RXRs). RXR-TRs bind to T(3) response elements (TREs) composed of direct repeats of the sequence AGGTCA spaced by four nucleotides (DR-4). In other TREs, however, the half-sites can be arranged as inverted palindromes and palindromes (Pa...

The adrenal cortical enzyme systems, 11 beta-hydroxylase, P-450 11 beta, and the side-chain cleavage complex, P-450 scc, differ only in their cytochrome P-450s. Structural modifications of metyrapone, an inhibitor of cytochrome P-450 enzyme systems, have been made to determine the requirement for the A- or B-pyridyl ring for inhibition of P-45011 beta and P-450 scc activities. Three new analogs...

In order to study the mode of action of beta-adrenoreceptor antagonists in essential tremor the efficacy of single oral doses of 2, 4 and 10 mg LI 32-468, a peripherally acting, selective beta-2 adrenoreceptor antagonist, was compared with a single oral dose of 120 mg propranolol in a randomised, double blind, placebo controlled trial. Both the lowest dose of LI and propranolol were shown to be...

Adrenaline (0.001-1,000 muM) strongly stimulated adenosine-3',5'cyclic monophosphate (cAMP) generation in cultured human microvascular-derived endothelial cells (HMEC-1). Isoprenaline mimicked the action of adrenaline, whereas noradrenaline appeared to be decisively less potent. Experiments carried out with an array of compounds acting selectively on different types/subtypes of adrenergic recep...

The halophilic methanogen Methanohalophilus portucalensis synthesizes three distinct zwitterions, (beta)-glutamine, N(sup(epsilon))-acetyl-(beta)-lysine (NA(beta)Lys), and glycine betaine, as osmolytes when it is grown at high concentrations of external NaCl. The selective distribution of these three species was determined by growing cells in the presence of osmolyte biosynthetic precursors. Gl...

Degradations by proteolytic enzymes and intestinal epithelial permeability represent two major drawbacks to the transfer of food protein antigens to blood. These steps were studied in vitro for the milk protein antigens beta-lactoglobulin (beta-Lg), alpha-Lactalbumin (alpha-La) and beta-casein (beta-cas). Pepsin-trypsin hydrolysis and permeability in isolated rabbit ileum in Ussing chamber were...