UNASSIGNED: Organophosphorus nerve agents inhibit @entity10810 ( @entity10810 ) which causes the breakdown of the transmitter @entity934 ( @entity1617 ) in the synaptic cleft. Overstimulation of cholinergic receptors (muscarinic and nicotinic) by excessive amounts of @entity1617 causes several health problems and may even cause @entity204 . Reversible @entity10810 inhibitors play an important role in prophylaxis against nerve agents. The presented study investigated whether @entity68729 (7-MEOTA) and 7-MEOTA- @entity8124 derivatives can act as central and peripheral reversible @entity10810 inhibitors and simultaneously antagonize muscarinic and nicotinic receptors. The possible mechanism of action was studied on cell cultures (patch clamp technique, @entity460 mobilization assay) and on isolated smooth muscle tissue (contraction study). Furthermore, the kinetics of the compounds were also examined. CNS availability was predicted by determining the passive blood-brain barrier penetration estimated via a modified PAMPA assay. In conclusion, this study provides promising evidence that the new synthesized 7-MEOTA- @entity8124 derivatives have the desired anticholinergic effect; they can inhibit @entity10810 , and nicotinic and muscarinic receptors in the micromolar range. Furthermore, they seem to penetrate readily into the CNS. However, their real potency and benefit must be verified by in vivo experiments.

Cholinergic properties of new @entity68729 - XXXX derivatives.

@entity1617 :: ('CHEBI:22614', 'Chemical') :: ['ACh'] @entity68729 :: ('MESH:C016222', 'Chemical') :: ['7-methoxytacrine'] @entity460 :: ('MESH:D002118', 'Chemical') :: ['calcium'] @entity10810 :: ('43', 'Gene') :: ['AChE', 'acetylcholinesterase'] @entity8124 :: ('MESH:C076946', 'Chemical') :: ['donepezil'] @entity204 :: ('MESH:D003643', 'Disease') :: ['death'] @entity934 :: ('MESH:D000109', 'Chemical') :: ['acetylcholine']
@entity8124 :: (MESH:C076946,Chemical) :: ['donepezil']
