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Subject:
From:
Ghislain De Roeck <[log in to unmask]>
Reply To:
Informed Discussion of Beekeeping Issues and Bee Biology <[log in to unmask]>
Date:
Fri, 19 Apr 2013 11:56:14 +0200
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Randy said:
Dr. John Casida personally confirmed to me that the effect is reversible,
not irreversible, as is often stated.

Mark said:
I have been searching for the irreversible mechanism of imidacloprid.  I
haven't found any compelling paper so far that shows or suggest that
imidacloprid is irreversible.

Christina said:
In animals, "irreversible receptor binding" is usually taken to mean the
receptor will not recover, because either there is no metabolic breakdown in
the synapse (thus releasing the ligand from the receptor), and/or binding to
the receptor is chemically irreversible (binding affinity is very
high--makes covalent bonds or the like) and will not go away until the
neuron is dead.

Submit for the cause of education only:

>This high activity is brought about by binding of imidacloprid to the
nicotinergic acetylcholine receptor in the insects nervous system, which
interferes with chemical signal transmission.
>Methods for isolating nicotinergic acetylcholine receptors from the heads
of Stomoxys calcitrans and for measuring the binding affinity, if any, of a
substance on such receptors have been developed.
>The neurophysiological properties of the nicotinergic acetylcholine
receptors of Stomoxys calcitrans, which include the binding of imidacloprid,
are described in detail. Imidacloprid is the first highly effective
insecticide whose mode of action has been found to derive from almost
complete and virtually irreversible blockage of postsynaptic nicotinergic
acetylcholine receptors in the central nervous system of the insect pest
Stomoxys calcitrans.

"The biochemistry of imidacloprid" (1991) - Planzenschutz - Nachrichten
Bayer; Abbink. J. (Bayerwerk AG, Wuppertal - Eberfeld, Germany) - Pharma
Forschungszentrum.

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