Novel GABA(A) Receptor Modulators


Photo credit for the Micrurus mipartitus: Alejandro Solórzano

MmTX1 (#STM-550) and MmTX2 (#STM-600) (Micrurotoxin 1 & 2 respectively) peptide toxins, are two novel and highly potent allosteric modulators of GABA (A) receptors. They were originally identified and isolated from Micrurus mipartitus (Red-tailed coral snake) venom (Rosso, J.P. et al. (2015) Proc. Natl. Acad. Sci. U.S.A. 112, E891.).

Both, MmTX1 and MmTX2 tightly bind to GABA(A) receptors at subnanomolar concentrations and allosterically increase GABA(A) receptor susceptibility to agonistic actions, thereby potentiating receptor opening and desensitization. They may be a priceless tool in evoking seizures for testing novel antiepileptic drugs or as lead molecules for designing therapeutics that modulate GABAA receptor activity (Rosso, J.P. et al. (2015) Proc. Natl. Acad. Sci. U.S.A. 112, E891.).



Alomone Labs MmTX1 (200 nM) modulates GABA(A) receptors expressed in Xenopus oocytes.A. Representative time course of GABA(A) α1/β2 current activated at a holding potential of -80 mV by 100 nM Muscimol hydrobromide (#M-240) applications (black bars), and modulated by co-application of 200 nM MmTX1 (#STM-550), as indicated (green bar). A significant modulation of receptor desensitization and reactivation rates is observed. B. Superimposed traces of GABA(A) receptor currents upon application of 100 nM Muscimol (black) or co-application of 100 nM Muscimol and 200 nM MmTX1 (green). Taken from the recording in A.



Alomone Labs MmTX2 modulates GABA(A) receptors expressed in Xenopus oocytes.A. Representative time course of GABA(A) α1/β2 currents activated at a holding potential of -80 mV with 50 nM Muscimol hydrobromide (#M-240) application (black bars), and modulated by co-application of 200 nM MmTX2 (#STM-600), as indicated (green bar). A significant modulation of receptor desensitization rate is observed. B. Superimposed traces of GABA(A) currents upon application of 50 nM Muscimol hydrobromide (black) or co-application of 50 nM Muscimol hydrobromide and 200 nM MmTX2 (green). Taken from the recording in A.


You are eligible to receive free samples of MmTX1 (#STM-550) and MmTX2 (#STM-600) to try!