A neurotoxin, ethylcholine mustard aziridinium ion, an irreversible LIGAND for the choline REUPTAKE system. AF-64A has been proposed as an agent capable of producing selective loss of CHOLINERGIC neurons or, if not loss of neurons, at least reduced cholinergic function. It has not been widely used, because it often has been found to produce CAVITATION in tissue. This non-selective toxic property has been difficult to separate from the selective. It has been suggested that at very low concentrations AF-64A is selective for the high affinity CHOLINE uptake system, which is specifically found on cholinergic neurons, while higher concentrations affect both high and low affinity choline uptake systems (the low affinity system being present on a wide variety of cells).
The success of selective neurotoxins such as 6-HYDROXYDOPAMINE stimulated a great interest in the possibility of finding a lesioning agent selective for cholinergic neurons. However, the non-selective effects of AF-64A have very seriously inhibited its use.
References
Hanin I. (1990) AF64A-induced cholinergic hypofunction, in Aquilonius S.-M. & Gillberg P.-G. (eds) Progress in Brain Research, vol. 84, pp. 289–299, Elsevier Science Publishers, B.V.
This is the complete article, containing 180 words
(approx. 1 page at 300 words per page).
