Molecular Targets
- Alpha-agatoxin: blocks the glutamate-activated receptor channels in the neuronal postsynaptic terminals insects and mammalian. alpha-agatoxin has an antagonistic function in mammalian, including both NMDA and AMPA receptors.
- Mu-agatoxin: is a specific modifier for sodium channels (presynaptic voltage-activated sodium channels), in the neuromuscular joint of an insect. Mu-agatoxin will have no effect in other species.
- Omega-agatoxin: in general type IA and type IIA affect the calcium channels of insects, while type IIIA and IVA affect the calcium channels in vertebrates. There are two major groups within the voltage activated calcium channels; the high voltage activated calcium channel and the low voltage activated calcium channel. The low activated calcium channels are activated by a smaller depolarisation and they show a rapid voltage-dependent inactivation. High voltage activated channels are activated by a large depolarisation and inactivate more slowly. ω-agatoxin only blocks the P/Q type calcium channels which are a voltage activated.
- Type IA and IIA block the presynaptic calcium channels in the presynaptic terminals of the neuromuscular junction of insects. Thereby, type IIA can also block the presynaptic calcium channels in neuromuscular junction of vertebrates.
- Type IIIA blocks ionic L-type current in myocardial cells. It also blocks other neuronal calcium channels, including N-, P/Q, and R-type calcium channels.
- Type IVA has a high affinity and specificity for P- and Q-type calcium channels.
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