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...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.