tetrodotoxin

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

A-803467 is a selective NaV1.8 channel blocker.

VSTx-3 is a potassium voltage-gated channel (K_V) blocker, which has also been shown to be a potent tetrodotoxin-sensitive (TTX-sensitive) sodium channel inhibitor, with particular efficacy against NaV1.8 channels, as evidenced by its half-maximal inhibitory concentration (IC_50) values of 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7, and 0.77 μM for hNaV1.8 channels.

Hardwickiic acid ((-)-Hardwikiic acid) is a natural compound derived from Pulicaria gnaphalodes and is an anti-injury receptor compound. hardwickiic acid blocks tetrodotoxin-sensitive voltage-dependent sodium channels. hardwickiic acid Hardwickiic acid has anti-inflammatory and insecticidal activity.

Jingzhaotoxin-V, a 29-residue polypeptide from Chilobrachys jingzhao spider venom, selectively inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons, with IC50 values of 27.6 nM and 30.2 nM, respectively. Furthermore, it suppresses Kv4.2 potassium currents in Xenopus laevis oocytes, with an IC50 of 604.2 nM [1].

Jingzhaotoxin-V is a peptide that suppresses potassium currents in Xenopus laevis oocytes, exhibiting an IC50 of 604.2 nM, while concurrently targeting both tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively [1].

Jingzhaotoxin-34, a 35-residue neurotoxic polypeptide, selectively inhibits tetrodotoxin-sensitive (TTX-S) sodium currents in rat dorsal root ganglion neurons with an IC50 of approximately 85 nM and exerts negligible influence on tetrodotoxin-resistant (TTX-R) sodium currents [1].

Carsatrin succinate is the salt form of Carsatin, a purinylpiperazine derivative used as a cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin.

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

3- Deoxyaconitine is a derivative of Aconitine (A189875), which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction.

Carsatrin is purinylpiperazine derivative. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin

Hainantoxin-IV acts as a specific antagonist for tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels, with His28 and Lys32 being critical residues for binding to the target. This compound also features an inhibitor cystine knot motif [1].

μ-Conotoxin SIIIA, a tetrodotoxin (TTX)-resistant sodium channel blocker, is a toxic peptide derived from Conus snail venom. It has applications in researching neurological diseases, including neuropathic pain [1].

Oe-9000 is a blocker of voltage-gated Na(+) currents in neurons. It reversibly reduces rapidly activating and inactivating TTX-sensitive (TTX-S) Na(+) currents as well as slowly activating and inactivating tetrodotoxin-resistant (TTX-R) Na(+) currents at

Jingzhaotoxin-IX is a C-terminally amidated peptide neurotoxin consisting of 35 amino acid residues. It inhibits both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms of voltage-gated sodium channels, as well as the Kv2.1 channel. However, Jingzhaotoxin-IX does not affect the delayed rectifier potassium channels Kv1.1, Kv1.2, and Kv1.3 [1].

mHuwentoxin-IV, a naturally modified form of Huwentoxin-IV, selectively inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels in dorsal root ganglion neurons with an IC50 value of 54.16 nM. Notably, the inhibitory effect of mHuwentoxin-IV on these sodium channels is unaffected by strong depolarization voltages [1].

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ