Anticholinesterases
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Anticholinesterases (antiChEs) are agents which inhibit ChE, protect ACh from hydrolysis—produce cholinergic effects in vivo and potentiate ACh both in vivo and in vitro. Some anti ChEs have additional direct action on cholinergic receptors.
ANTICHOLINESTERASES
Anticholinesterases
(antiChEs) are agents which inhibit ChE, protect ACh from hydrolysis—produce
cholinergic effects in vivo and
potentiate ACh both in vivo and in vitro. Some anti ChEs have additional
direct action on cholinergic receptors.
Reversible
Carbamates Acridine
Physostigmine (Eserine) Tacrine
Neostigmine
Pyridostigmine
Edrophonium
Rivastigmine, Donepezil
Galantamine
Irreversible
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Organophosphates |
Carbamates |
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Dyflos (DFP) |
Carbaryl* (SEVIN) |
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Echothiophate |
Propoxur* (BAYGON) |
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Parathion*, Malathion* |
*Insecticides |
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Diazinon* (TIK20) |
£Nerve gases for |
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Tabun£, Sarin£, Soman£ |
chemical warfare |
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Chemistry
AntiChEs
are either esters of carbamic acid or derivatives of phosphoric acid.
The
generic formula of carbamates and organophosphates is shown below:
In carbamates R1
may have a nonpolar tertiary amino N, e.g. in physostigmine, rendering the
compound lipid soluble. In others, e.g. neostigmine, R1 has a
quaternary N+—rendering it lipid insoluble. All organophosphates are
highly lipid soluble except echothiophate which is water soluble.
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