Caffeine is a secondary metabolite of tea and coffee plants. It is the active psychostimulant ingredient of widely consumed beverages, chocolate and some drugs as well. The major pathways for caffeine including interaction with adenosine receptors have been identified but caffeine has several minor pathways as well that remain poorly understood including the cholinergic system. Given the role of caffeine in the cholinergic system, some molecular targets have been tracked and a mechanism of its action has been proposed in research studies. However, the biological effect of caffeine on the cholinergic system is not completely understood. The present review focuses on the role of caffeine in the cholinergic system.

• MeSH
• acetylcholin metabolismus   MeSH
• adenosin antagonisté a inhibitory   MeSH
• antiflogistika nesteroidní izolace a purifikace   farmakologie   MeSH
• cholinergní látky izolace a purifikace   farmakologie   MeSH
• cholinesterasy metabolismus   MeSH
• cytokiny biosyntéza   imunologie   MeSH
• kofein izolace a purifikace   farmakologie   MeSH
• lidé MeSH
• receptory cholinergní metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH

Trimedoxime is a bisquaternary oxime that is widely used in the treatment of organophosphorous poisoning caused by tabun and paraoxon. We tested its affinity to acetylcholinesterase (AChE), its mechanism of interaction and effect on the cholinergic system of the rat bladder. The half maximal inhibitory concentration (IC50) of trimedoxime to recombinant AChE was found to be 82.0 mM ± 30.1 mM. This represents a weak inhibition. Its interaction with AChE seems to be very similar to obidoxime - one aromatic nucleus interacts with the peripheral anionic site and the other with the residues TYR337 and TYR341 inside the cavity. Also the oxime moiety is moving towards the catalytic triade ready for the reactivation of the inhibited AChE. In the organ bath experiment no significant effect of trimedoxime was observed on the contraction of the detrusor caused by the muscarinic agonist metacholine.

• Klíčová slova
• acetylcholinesterase, trimedoxime, antidote, muscaricnic receptors, reactivation,
• MeSH
• acetylcholinesterasa farmakokinetika   farmakologie   účinky léků   MeSH
• antidota farmakologie   terapeutické užití   MeSH
• cholinergní antagonisté farmakokinetika   farmakologie   terapeutické užití   MeSH
• cholinergní látky farmakologie   imunologie   izolace a purifikace   MeSH
• experimenty na zvířatech MeSH
• financování organizované MeSH
• močový měchýř MeSH
• organofosforové sloučeniny farmakokinetika   farmakologie   toxicita   MeSH
• pesticidy farmakokinetika   farmakologie   toxicita   MeSH
• potkani Sprague-Dawley MeSH
• reaktivátory cholinesterázy farmakokinetika   farmakologie   terapeutické užití   MeSH
• receptory muskarinové účinky léků   MeSH
• synergismus léků MeSH
• trimedoxim farmakokinetika   farmakologie   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH