N-Glucuronidation in vitro of six 4-arylalkyl-1H-imidazoles (both enantiomers of medetomidine, detomidine, atipamezole, and two other closely related compounds) by rat, dog, and human liver microsomes and by four expressed human UDP-glucuronosyltransferase isoenzymes was studied. Human liver microsomes formed N-glucuronides of 4-arylalkyl-1H-imidazoles with high activity, with apparent V(max) v...

Muscle metabolism, including the role of pyruvate dehydrogenase (PDH) in muscle lactate (Lac-) production, was examined during incremental exercise before and after 7 days of submaximal training on a cycle ergometer [2 h daily at 60% peak O2 uptake (V˙o 2 max)]. Subjects were studied at rest and during continuous steady-state cycling at three stages (15 min each): 30, 65, and 75% of the pretrai...

During ventricular fibrillation (VF) only 39% of the variation in action potential duration (APD) is accounted for by the previous diastolic interval [DI((n-1))], i.e., restitution, and the previous APD [APD((n-1))], i.e., memory. We tested the hypothesis that a characteristic of the AP upstroke, the maximum rate of depolarization (V(max)), also helps account for its APD. A floating microelectr...

Bevirimat [BVM, PA-457, 3-O-(3',3'-dimethylsuccinyl)-betulinic acid], a new anti-human immunodeficiency virus drug candidate, is metabolized to two monoglucuronides [mono-BVMG (I) and mono-BVMG (II)] and one diglucuronide (di-BVMG) both in vivo and in vitro. UDP-glucuronosyltransferase (UGT) reaction screening, enzyme kinetics, and species differences for the glucuronidation of BVM in vitro wer...

Glutamate dehydrogenase (NAD) activity was measured in liver and diaphragm mitochondria from 48 h fasted rats. Kinetic studies were performed with diaphragm enzyme and the effects of L-leu, ADP and L-ala on the K(1)m and V(1)max for NH(4)+, and α-ketoglutarate were evaluated. L-leucine increases by 2-8 fold the V(1)max for all three substrates with no significant changes in the K(1)m. ADP incre...

We study the phases of the Nagel-Schreckenberg traffic model with open boundary conditions as a function of the randomization probabilities p>0 and the maximum velocity v(max)>1. Due to the existence of "buffer sites" which enhance the free-flow region, the behavior is much richer than that of the related, parallel updated asymmetric exclusion process [(ASEP), v(max)=1]. Such sites exist for v(...

The photosynthetic enzyme ribulose bisphosphate carboxylase-oxygenase [EC 4.1.1.39] (RuBPCase) plays a key role in the carbon reduction system of plants. In this study, we determined the kinetic variability of RuBPCase among 46 varieties of Hordeum vulgare L. at two ages. The V(max) CO(2) and K(m) CO(2) of RuBPCase was determined for each cultivar. Varietal differences were found in K(m) CO(2) ...

A physiological strain index (PSI) based on rectal temperature (Tre) and heart rate (HR) was recently suggested to evaluate exercise-heat stress. The purpose of this study was to evaluate PSI for gender differences under various combinations of exercise intensity and climate. Two groups of eight men each were formed according to maximal rate of O2 consumption (V˙o 2 max). The first group of men...