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Activation of TRPA1 channels by fenamate nonsteroidal anti-inflammatory drugs
TLDR
It is concluded that fenamate NSAIDs are a novel class of potent and reversible direct agonists of TRPA1, and should provide a structural basis for developing novel ligands that noncovalently interact withTRPA1 channels.
Influence of nociceptive stimulation on analgesia nociception index (ANI) during propofol-remifentanil anaesthesia.
TLDR
The ability of ANI compared with SPI to detect standardized noxious stimulation during propofol-remifentanil anaesthesia was challenged and it was found that ANI and SPI may improve detection but not prediction of a possible inadequate nociception-anti-nociceptive balance.
Measurement of the nociceptive balance by Analgesia Nociception Index and Surgical Pleth Index during sevoflurane-remifentanil anesthesia.
TLDR
Non-invasive monitoring of ANI and SPI reflected nociceptive stimulation during sevoflurane-remifentanil anesthesia and therefore may indicate the nocICEption - anti-nociception balance.
Molecular approaches to receptors as targets for drug discovery.
TLDR
This review presents an overview of how molecular biological approaches have revealed a plethora of receptor subtypes, led to new definitions of subtypes and isoforms, and played a role in the development of high selective drugs.
The muscarinic antagonists aprophen and benactyzine are noncompetitive inhibitors of the nicotinic acetylcholine receptor.
TLDR
Aprophen and benactyzine are effective noncompetitive inhibitors of the A ChR at concentrations of 1-50 microM, in either Torpedo or mammalian AChR, and correspond very well with the blood level of these drugs found in vivo to produce a therapeutic response against organophosphate poisoning.
The effect of intravesical ketoprofen on acetylcholine-evoked urinary bladder contractility and detrusor overactivity in the anesthetized rabbit model
TLDR
The rabbit model of detrusor overactivity has proven to be an excellent model to study the effects of drugs on detrusors overactivity and the responses to intravesical ketoprofen was evaluated.
Topography of the Acetylcholine Receptor Revealed by Fluorescence Energy Transfer
TLDR
Findings suggest that a likely site for ethidium binding is between hydrophobic segments spanning the membrane portion of the channel rather than associating with in a water-lined channel, and that ethidium is rigidly immobilized in a hydrophilic crevice.
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