Pentapeptide-3

Pentapeptide-3 Related Research

1.Pharmacological Profile and Development

It exhibits significantly reduced toxicity (approximately 1,000-fold) compared to the venom peptide it mimics in binding to acetylcholine receptors.

It is a competitive antagonist of the acetylcholine receptor and functions by inhibiting neuromuscular transmission, leading to reduced muscle contraction.

Pentapeptide-3 is said to have a mode of action similar to that of tubocurarine, an extremely poisonous paralytic toxin obtained from many plants.

In contrast to direct extraction from snake venom, pentapeptide-3 sold commercially is synthesized by means of a chemical process.

This is to assure its purity and safety, preventing risks associated with other harmful agents found in natural venom.

2.Detailed Mechanism of Action

The primary mode of action for pentapeptide-3 is to block NMJ signaling.

Under normal functional conditions, nervous impulses that arrive at the motor nerve endings release a neurotransmitter known as acetylcholine.

Acetylcholine is released, crosses the synapse and binds to nicotinic acetylcholine receptors (nAChR) on muscle cell membrane (postsynaptic membrane).

This binding leads to the activation of receptor ion channels, which permits Na+ ions to enter.

This in turn results in depolarization of the muscle cell membrane and leads to biochemical changes that cause muscle fiber contraction.

Pentapeptide-3 is a competitive antagonist of the muscle nicotinic acetylcholine receptor (nAChR), preventing binding of acetylcholine to these receptors.

This action prevents the opening of voltage-gated sodium channels, in turn restricting depolarization of the postsynaptic membrane and resulting in decreases in frequency and intensity of muscle contraction.

3.In Vitro and Clinical Efficacy

In vitro tests have shown a reduction of muscle contraction by 71% after just one minute and an inhibition rate of 58 percent after two hours.

Given that facial wrinkles are developed by the repeated contraction of subcutaneous muscles, this method could relax subcutaneous muscles to reduce the depth of dynamic wrinkles, such as crow’s feet.

Pentapeptide-3 is mainly used in anti-aging skincare.

Its efficacy has been validated in numerous clinical trials.