Biological activity :
BTX is the most active alkaloid binding at
receptor site-2 on sodium channels. It activates the sodium channel even
at very negative membrane potentials and keeps it open permanently by
preventing channel inactivation. BTX also changes the selectivity of the
channel to Na+ ions and makes it less selective, enabling larger ions to pass through the pore. EC50 (in vitro): 0.1 to 100 nanomolar.
BTX binding induces many allosteric effects on
other channel regions, and increases the binding of scorpion
alpha-toxins to receptor site-3, of brevetoxin to receptor site-5, and
of pyrethroid insecticides to receptor site-7.
Field of use :
Batrachotoxin-sensitive sodium channels are
expressed in central and peripheral neurons and in both striated and
cardiac muscle, where they regulate excitability. A number of channel
subtypes exist. Research tool applicable to the study of the function of
sodium channel and the effects of other toxins and of a variety of
drugs, including anesthetics, analgesics, antiarrhythmics,
anticonvulsants and antidepressants.
Recommended doses: < 1 microgram/kg
Recommended concentrations: 0.01 to 10 micromolar.
Purity : min. 90 %. (HPLC, TLC, Toxicity)
Toxicity (LD50) :
Mice (sc): LD50: 2 micrograms/kg. Convulsions and death after 8 min at 10 micrograms/kg
Storage and reconstitution recommendations :
Stable at room temperature, store preferably at 4°C. Solid and
solutions can be kept in deep freeze for a long time without any change
in their activity. Reconstitution: dissolve in ethanol or methanol.
Safety recommendations : Highly toxic.
Bibliographic references :
1. T. Tokuyama et al, J. Am Chem. Soc 91:3931 (1969)
2. E. X. Albuquerque et al, Science 172:995 (1971)
3. W. A. Catterall et al, J. Biol. Chem. 256:8922 (1981)
4. T. Tokuyama and J.W. Daly, Tetrahedron 39:41-47 (1983)
5. G.B. Brown, Internat. Rev. Neurobiol. 29: 77-116 (1988)
6. M. Kurosu et al., J. Am Chem.. Soc. 120: 6629 (1998)
7. S. J. Wang and G. K. Wang, Cellular Signaling 15: 151 (2003)
8. Batrachotoxin. RN 23509-16-2. STN Registry file (27 February 2006)
External Links : Batrachotoxin on PubMed