A Potentiometric approach to the study of the antagonism between acetazolamide andI-carnitine congeners on carbonic anhydrase activity

The in vitro interactions among carbonic anhydrase (CA), acetazolamide (ACTZ), and some short chain acylcarnitines (l- and d-isomers) were studied by means of a recently developed potentiometric method of analysis, based on a pCO2 sensor. The l- and d-isomers of carnitine (C), acetylcarnitine (AC), propionylcarnitine (PC), and isobutyrrylcarnitine (iBC) were found not to affect CA catalytic activity in the absence of other compounds. Upon testing in the presence of ACTZ, the l-isomers of the carnitine congeners were shown to antagonize the chemical inhibition of carbonic anhydrase II from bovine erythrocytes, whereas in this case the d-isomers did not show any effect. The results obtained in these experiments, carried out at 25 and at 37-degrees-C, confirm the high reliability of this new approach and highlight the positive effect of l-carnitine congeners on CA catalytic activity. The potentiometric method should be suitable for monitoring the interaction of other enzymes and CA

ChemInform Abstract: Synthesis and Inhibitory Activity on Carbonic Anhydrase of Some New Sulpiride Analogues Studied by Means of a New Method.

The pharmacological activity of several new sulpiride analogues was studied by means of a new approach, based on a potentiometric technique with a pCO2 sensor, capable of detecting carbonic anhydrase inhibition at equilibrium conditions. This procedure gives results stated as percent of inhibition of enzymatic activity (IP, inhibitory power). To prove the reliability of the proposed approach and to study structure-activity relationships, several new molecules were synthesized and tested in comparison with the two sulpiride enantiomers. A possible inhibition mechanism is discussed in terms of experimental evidence obtained from the interactions between the molecular structures of the new synthesized compounds and carbonic anhydrase

Synthesis and inhibitory activity on carbonic anhydrase of some new sulpiride analogues studied by means of a new method.

The pharmacological activity of several new sulpiride analogues was studied by means of a new approach, based on a potentiometric technique with a pCO2 sensor, capable of detecting carbonic anhydrase inhibition at equilibrium conditions. This procedure gives results stated as percent of inhibition of enzymatic activity (IP, inhibitory power). To prove the reliability of the proposed approach and to study structure-activity relationships, several new molecules were synthesized and tested in comparison with the two sulpiride enantiomers. A possible inhibition mechanism is discussed in terms of experimental evidence obtained from the interactions between the molecular structures of the new synthesized compounds and carbonic anhydrase

Prevalence and concentrations of drugs found in urine from Mont Blanc climbers.

<p>Prevalence and concentrations of drugs found in urine from Mont Blanc climbers.</p

Combinations of drugs found in urine from Mont Blanc climbers.

<p>Combinations of drugs found in urine from Mont Blanc climbers.</p

Time for change: a roadmap to guide the implementation of the World Anti-Doping Code 2015

A medical and scientific multidisciplinary consensus meeting was held from 29 to 30 November 2013 on Anti-Doping in Sport at the Home of FIFA in Zurich, Switzerland, to create a roadmap for the implementation of the 2015 World Anti-Doping Code. The consensus statement and accompanying papers set out the priorities for the antidoping community in research, science and medicine. The participants achieved consensus on a strategy for the implementation of the 2015 World Anti-Doping Code. Key components of this strategy include: (1) sport-specific risk assessment, (2) prevalence measurement, (3) sport-specific test distribution plans, (4) storage and reanalysis, (5) analytical challenges, (6) forensic intelligence, (7) psychological approach to optimise the most deterrent effect, (8) the Athlete Biological Passport (ABP) and confounding factors, (9) data management system (Anti-Doping Administration &amp; Management System (ADAMS), (10) education, (11) research needs and necessary advances, (12) inadvertent doping and (13) management and ethics: biological data. True implementation of the 2015 World Anti-Doping Code will depend largely on the ability to align thinking around these core concepts and strategies. FIFA, jointly with all other engaged International Federations of sports (Ifs), the International Olympic Committee (IOC) and World Anti-Doping Agency (WADA), are ideally placed to lead transformational change with the unwavering support of the wider antidoping community. The outcome of the consensus meeting was the creation of the ad hoc Working Group charged with the responsibility of moving this agenda forward