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Waglerin-1 blocks muscle-type nAChRs

Waglerin-1 (Wtx-1) is a peptide originally isolated from the venom of the Wagler’s pit viper (Trimeresurus wagleri). This 22 amino-acid peptide is a competitive antagonist of muscle nicotinic acetylcholine receptors. Waglerin-1 competes with α-bungarotoxin.

Waglerin-1 is an interesting tool to discriminate between fetal and adult muscle nAChRs as it binds to the α-ε subunit interface with a ~ 2000 fold higher affinity than to the α-γ or α-δ subunits. Waglerin-1 is known to bind 100 fold more potently to nAChR from adult mice than that from rat or humans. It blocks muscle nAChR from adult mice with an IC50 value of 50nM.

Some studies have demonstrated that Waglerin-1 has an effect on ionotropic GABA receptors. It may potentiate or depress I(GABA) depending on the neurons.

Some derivatives of Waglerin-1 are currently used in cosmetics to reduce wrinkles.

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AA sequence:  Gly-Gly-Lys-Pro-Asp-Leu-Arg-Pro-Cys9-His-Pro-Pro-Cys13-His-Tyr-Ile-Pro-Arg-Pro-Lys-Pro-Arg-OH
Disulfide bonds: Cys9-Cys13
Length (aa): 22
Formula: C112H175N37O26S2
Molecular Weight: 2520 Da
Appearance: White lyophilized solid
Solubility: water or saline buffer
CAS number: NA
Source: Synthetic

Peptide-toxin tools for probing the expression and function of fetal and adult subtypes of the nicotinic acetylcholine receptor

Conformational analysis of a toxic peptide from Trimeresurus wagleri which blocks the nicotinic acetylcholine receptor

Identification of residues at the alpha and epsilon subunit interfaces mediating species selectivity of Waglerin-1 for nicotinic acetylcholine receptors

Waglerin-1 selectively blocks the epsilon form of the muscle nicotinic acetylcholine receptor

Waglerin-1 inhibits GABA(A) current of neurons in the nucleus accumbens of neonatal rats. Brain Res

Waglerin-1 modulates gamma-aminobutyric acid activated current of murine hypothalamic neurons

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