Wrinkles are mainly caused by strong muscle contraction or keeping the muscle in a strong contraction position for a long time. In order to treat such expression lines and age-related wrinkles, Botox A (Botox A) is now commonly used.
Injecting Botox A into the muscles around the eyes or forehead paralyzes the muscles and can no longer move, making wrinkles impossible.
However, the use of subcutaneous Botox A must be administered by a doctor, and there are disadvantages of high cost and high risk. The effect of botulinum toxin type A (Botox A) can be maintained for 3-6 months, after which the treatment must be repeated.
The mechanism of action of Botox A is to selectively block the release of acetylcholine at neuromuscular synapses, resulting in muscle paralysis. This is achieved by the cleavage of a protein called SNAP-25.
The N-terminal amino acid sequence of SNAP-25 (H-Glu-Glu-Met-Gln-Arg-Arg-NH2) can also inhibit Ca+-dependent neurotransmitter release in synapses and cause muscle relaxation.
As a result, a topical anti-wrinkle polypeptide: Acetyl Hexapeptide-8 (Acetyl Hexapeptide-8) was developed. Akirelin is about 5000 times weaker than Botox A, so it can be dosed better and has almost no toxicity.
In addition to the inhibition of the release of the neurotransmitter acetylcholine by Botox A, there are two other types of inhibitors of acetylcholine activity at neuromuscular synapses: inhibitors of acetylcholine receptors and inhibitors of acetylcholinesterase.
The snake venom tripeptide (Dipeptide Diaminobutyroyl Benzylamide Diacetate) can reach its site of action (neuromuscular synapse) quickly and in sufficient concentration, block the neuromuscular synapse, and cause muscle relaxation.
Compared to Acetyl Hexapeptide-8 (Acetyl Hexapeptide-8), Dipeptide Diaminobutyroyl Benzylamide Diacetate has a significantly better spectrum of action characteristics and higher proteolytic stability in terms of muscle relaxation activity. And because of its relatively low molecular weight and suitable water/n-octanol partition coefficient, they can be applied topically.