ω-Agatoxin IVa trifluoroacetate salt

Names

[ Name ]:
ω-Agatoxin IVa trifluoroacetate salt

Biological Activity

[Description]:

ω-Agatoxin IVA is a potent, selective P/Q type Ca2+ channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Neurological Disease

[Target]

IC50: 2 nM (P-type Ca2+ channels), 90 nM (Q-type Ca2+ channels)[1]

[References]

[1]. T Teramoto, et al. A novel type of calcium channel sensitive to omega-agatoxin-TK in cultured rat cerebral cortical neurons. Brain Res. 1997 May 9;756(1-2):225-30.

[2]. M Kimura, et al. Involvement of P-type calcium channels in high potassium-elicited release of neurotransmitters from rat brain slices. Neuroscience. 1995 Jun;66(3):609-15.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁₇H₃₆₀N₆₈O₆₀S₁₀

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

P-type calcium channels blocked by the spider toxin omega-Aga-IVA.

Nature 355 , 827-829, (1992)

Voltage-dependent calcium channels mediate calcium entry into neurons, which is crucial for many processes in the brain including synaptic transmission, dendritic spiking, gene expression and cell dea...

P-type calcium channels in rat central and peripheral neurons.

Neuron 9 , 85-95, (1992)

The peptide toxin omega-Aga-IVA blocked P-type Ca2+ channel current in rat Purkinje neurons (KD approximately 2 nM) but had no effect on identified T-type, L-type, or N-type currents in a variety of c...

Calcium channels coupled to glutamate release identified by omega-Aga-IVA.

Science 258 , 310-313, (1992)

Presynaptic calcium channels are crucial elements of neuronal excitation-secretion coupling. In mammalian brain, they have been difficult to characterize because most presynaptic terminals are too sma...