Pinnatoxin

Pinnatoxins are paralytic chemical compounds that inhibit neuronal and muscle-type nicotinic acetylcholine receptors.

[17][18][19] Pinnatoxins are potent inhibitors of neuronal and muscle type nicotine acetylcholine receptors (nAChRs).

Different subregions of the pinnatoxin molecule have multiple anchoring points in the receptor-binding site, through which they dictate the tight binding between the opposing loops C and F at the nAChR subunit interface.

[10][16][21] The toxic effects of pinnatoxin E-H have, however, been examined on female Swiss albino mice.

[10][16][21] The symptoms exhibited by mice exposed to a lethal dose of pinnatoxin by intraperitoneal injection are very similar between pinnatoxin E, F, G and H.[10][16][21] The symptoms start off with a period of hyperactivity until 10–20 minutes after injection, when an abrupt decrease in activity occurs.

Death is preceded by a brief period of running movements, the occurrence of cyanosis and severe exophthalmos.

[10] In contrast, the time to death after admission of pinnatoxin H by intraperitoneal injection or gavage did not differ.

[21] The behavioural abnormalities observed in mice after a sublethal dose start off with a hyperactive or immobile period shortly after toxin admission, and end with a full recovery.

Pinnatoxin A (yellow) bound to the Aplysia californica acetylcholine-binding protein, illustrating the binding site at the interfaces between pentamer subunits. From PDB : 4XHE ​. [ 1 ]