Protein Information

Name sodium channel (protein family or complex)
Synonyms Sodium channel

Compound Information

Name tetramethrin
CAS

Reference List

PubMed Abstract RScore(About this table)
2454144 Takeda K, Narahashi T: Chemical modification of sodium channel inactivation: separate sites for the action of grayanotoxin and tetramethrin. Brain Res. 1988 May 17;448(2):308-12.
168(2,2,3,3) Details
8720856 Song JH, Nagata K, Tatebayashi H, Narahashi T: Interactions of tetramethrin, fenvalerate and DDT at the sodium channel in rat dorsal root ganglion neurons. Brain Res. 1996 Feb 5;708(1-2):29-37.
164(2,2,2,4) Details
6286960 Narahashi T: Modulation of nerve membrane sodium channels by chemicals. J Physiol. 1981 May;77(9):1093-101.

The tail current associated with step repolarization during the slow current in grayanotoxins decays with a dual exponential time course. 5. (+)-trans tetramethrin and (+)-trans allethrin also modify a fraction of sodium channel population in generating a slow current, which attains a maximum slowly and decays very slowly during a maintained depolarizing step.
84(1,1,1,4) Details
8613953 Song JH, Narahashi T: Modulation of sodium channels of rat cerebellar Purkinje neurons by the pyrethroid tetramethrin. J Pharmacol Exp Ther. 1996 Apr;277(1):445-53.

Chloramine-T at 200 microM removed the sodium channel inactivation and increased the percentage of sodium channel modification by tetramethrin through open channel modification.
83(1,1,1,3) Details
11456334 Motomura H, Narahashi T: Interaction of tetramethrin and deltamethrin at the single sodium channel in rat hippocampal neurons. Neurotoxicology. 2001 Jun;22(3):329-39.
83(1,1,1,3) Details
2423191 Yamamoto D, Yeh JZ, Narahashi T: Ion permeation and selectivity of squid axon sodium channels modified by tetramethrin. Brain Res. 1986 Apr 30;372(1):193-7.

It was concluded that tetramethrin modifies the sodium channel gating machinery without affecting the pore properties.
82(1,1,1,2) Details
8597060 Narahashi T, Carter DB, Frey J, Ginsburg K, Hamilton BJ, Nagata K, Roy ML, Song JH, Tatebayashi H: Sodium channels and GABAA receptor-channel complex as targets of environmental toxicants. Toxicol Lett. 1995 Dec;82-83:239-45.

In rat cerebellar Purkinje neurons and dorsal root ganglion neurons, only about 1% of sodium channel population needed to be modified by the pyrethroid tetramethrin to increase the depolarizing after-potential to the level of the threshold membrane potential for generation of repetitive after-discharges.
82(1,1,1,2) Details
10960151 Motomura H, Narahashi T: Temperature dependence of pyrethroid modification of single sodium channels in rat hippocampal neurons. J Membr Biol. 2000 Sep 1;177(1):23-39.

Tetramethrin at 10 microm modified 17 and 23% of channels at 22 and 12 degrees C, respectively, indicating that the sensitivity of the sodium channel of rat hippocampal neurons to tetramethrin was almost the same as that of tetrodotoxin-sensitive sodium channels of rat dorsal root ganglion neurons and rat cerebellar Purkinje neurons.
81(1,1,1,1) Details
9495855 Tabarean IV, Narahashi T: Potent modulation of tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels by the type II pyrethroid deltamethrin. J Pharmacol Exp Ther. 1998 Mar;284(3):958-65.

These results suggest that the deltamethrin and tetramethrin share a binding site on the sodium channel and that the slow onset and offset of deltamethrin action are controlled by the rates at which deltamethrin moves and unbinds from the membrane lipid phase rather than by the rate of deltamethrin binding to the sodium channel site.
81(1,1,1,1) Details
6275321 Lund AE, Narahashi T: Modification of sodium channel kinetics by the insecticide tetramethrin in crayfish giant axons. Neurotoxicology. 1981 Oct;2(2):213-29.
81(1,1,1,1) Details
6270310 Lund AE, Narahashi T: Kinetics of sodium channel modification by the insecticide tetramethrin in squid axon membranes. J Pharmacol Exp Ther. 1981 Nov;219(2):464-73.
81(1,1,1,1) Details
8071852 Tatebayashi H, Narahashi T: Differential mechanism of action of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J Pharmacol Exp Ther. 1994 Aug;270(2):595-603.

The steady-state sodium channel inactivation curve was shifted by tetramethrin in the hyperpolarizing direction in both TTX-S and TTX-R channels.
81(1,1,1,1) Details
8814900 Song JH, Narahashi T: Differential effects of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant single sodium channels. Brain Res. 1996 Mar 18;712(2):258-64.

The differential effects of the pyrethroid tetramethrin on tetrodotoxin-sensitive (TTX-S) and tetrodotoxin-resistant (TTX-R) single sodium channel currents in rat dorsal root ganglion (DRG) neurons were investigated using the outside-out configuration of patch-clamp technique.
12(0,0,2,2) Details
2434060 Narahashi T: Nerve membrane ionic channels as the target of toxicants. Arch Toxicol Suppl. 1986;9:3-13.

Fenvalerate, a cyano-containing type II pyrethroid, prolongs the sodium channel open time much more drastically than tetramethrin.
8(0,0,1,3) Details
2433987 Narahashi T: Toxins that modulate the sodium channel gating mechanism. . Ann N Y Acad Sci. 1986;479:133-51.

In the presence of type I pyrethroids which lack a cyano group at the alpha position (e.g., allethrin and tetramethrin), a large steady-state sodium current appears during a step depolarization and a large slowly decaying sodium tail current appears upon repolarization.
5(0,0,0,5) Details
11714887 Tabarean IV, Narahashi T: Kinetics of modulation of tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels by tetramethrin and deltamethrin. J Pharmacol Exp Ther. 2001 Dec;299(3):988-97.

Both types prolong the sodium channel current thereby causing hyperexcitability, yet details of modulation of current kinetics remain largely to be seen.
3(0,0,0,3) Details
18538810 Meacham CA, Brodfuehrer PD, Watkins JA, Shafer TJ: Developmentally-regulated sodium channel subunits are differentially sensitive to alpha-cyano containing pyrethroids. Toxicol Appl Pharmacol. 2008 Sep 15;231(3):273-81. Epub 2008 Apr 29.

Permethrin and tetramethrin did not modify currents mediated by either subunit combination.
2(0,0,0,2) Details
6128164 Narahashi T: Modification of nerve membrane sodium channels by the insecticide pyrethroids. Comp Biochem Physiol C. 1982;72(2):411-4.

The synthetic pyrethroids exert potent and selective actions on nerve membrane sodium channels. (+)-trans tetramethrin and (+)-trans allethrin cause repetitive discharges to be produced in the isolated crayfish and squid giant axons in response to a single stimulus as a result of an increase in depolarizing after-potential. 2.
The latter effect is due to slowing of the sodium channel kinetics which causes a prolonged sodium current following the normal peak sodium current. 3.
2(0,0,0,2) Details
11504804 Spencer CI, Yuill KH, Borg JJ, Hancox JC, Kozlowski RZ: Actions of pyrethroid insecticides on sodium currents, action potentials, and contractile rhythm in isolated mammalian ventricular myocytes and perfused hearts. J Pharmacol Exp Ther. 2001 Sep;298(3):1067-82.

The type I pyrethroid tetramethrin had little effect in any of the preparations.
Cardiac myocytes are also rich in sodium channels but comparatively little is known about the effect of pyrethroids on the heart, or on the cardiac sodium channel isoform.
1(0,0,0,1) Details
6324913 Yamamoto D, Yeh JZ, Narahashi T: Voltage-dependent calcium block of normal and tetramethrin-modified single sodium channels. Biophys J. 1984 Jan;45(1):337-44.

The results suggest that the Ca-induced decrease of the macroscopic sodium current results from a reduced single sodium channel conductance.
1(0,0,0,1) Details
6685257 Gammon DW, Ruzo LO, Casida JE: A new pyrethroid insecticide with remarkable potency on nerve axons. . Neurotoxicology. 1983 Summer;4(2):165-9.

The analog of cis-tetramethrin with a 2,2-dimethyl-cyclopropyl replacement for the 2-methyl-1-propenyl group, i.e., "methanotetramethrin", is one of the most neuroactive compounds ever described.
The remarkable potency of methanotetramethrin, giving consistent repetitive firing in this nerve assay at 10 (-18) M, and the speculation that it may undergo reversible covalent binding via Michael addition indicate that it could be a useful neurophysiological probe and candidate affinity label for the sodium channel.
1(0,0,0,1) Details
2549473 Salgado VL, Herman MD, Narahashi T: Interactions of the pyrethroid fenvalerate with nerve membrane sodium channels: temperature dependence and mechanism of depolarization. Neurotoxicology. 1989 Spring;10(1):1-14.

Even when applied directly to the internal face of the membrane, the effect of fenvalerate on the sodium channel developed slowly, taking more than 90 min to reach its final level.
Membrane depolarization caused by tetramethrin and fenvalerate was greater at 10 degrees C than at 21 degrees C, and was reversible upon changing the temperature.
1(0,0,0,1) Details
6302535 Narahashi T: Cellular and molecular mechanisms of action of insecticides: neurophysiological approach. Neurobehav Toxicol Teratol. 1982 Nov-Dec;4(6):753-8.

Type I pyrethroids as represented by allethrin and tetramethrin which lack a cyano group cause repetitive discharges in nerve fibers and nerve terminals leading to hyperexcitation of the animal.
Thus, it is concluded that the site of action of pyrethroids is the sodium channel, and that pyrethroids interact with the channel macromolecules that control the gating mechanism.
1(0,0,0,1) Details
8531109 Song JH, Narahashi T: Selective block of tetramethrin-modified sodium channels by (+/-)-alpha-tocopherol (vitamin E). J Pharmacol Exp Ther. 1995 Dec;275(3):1402-11.

Because the sodium channel is the major target site of pyrethroids, it is possible that vitamin E interferes with pyrethroid modification of the sodium channel.
1(0,0,0,1) Details
2422892 Narahashi T: Modulators acting on sodium and calcium channels: patch-clamp analysis. Adv Neurol. 1986;44:211-24.


Tetramethrin also modifies the single sodium channel in a similar manner to BTX, but fails to affect the amplitude of single-channel current.
0(0,0,0,0) Details