1401708-83-5/Dihexa

Description

Dihexa (developmental code name PNB-0408), also known as N-hexanoic-Tyr-Ile-(6) aminohexanoic amide, is an oligopeptide drug derived from angiotensin IV that binds with high affinity to hepatocyte growth factor (HGF) and potentiates its activity at its receptor, c-Met. The compound has been found to potently improve cognitive function in animal models of Alzheimer's disease-like mental impairment. In an assay of neurotrophic activity, Dihexa was found to be seven orders of magnitude more potent than brain-derived neurotrophic factor.

Uses

N-Hexanoic-Try-Ile-(6)-amino Hexanoic amide (Dihexa) is an angiotensin IV analog as a procognitive/antidementia agent.

benefits

As a new drug, Dihexa has been highly seen to help people experiencing Alzheimer's Disease.Thus, it's main function is to relieve and supplement people who are stricken by this Disease to slow down the progression of Alzheimer's.The best thing about Dihexa is its ability to be able to repair damages found in the synapse that is just between the neurons.Here are some of the benefits of Dihexa:Helps people having Alzheimer's Disease and those with Parkinson's DiseaseCan increase your mental staminaCan improve creative thinking skillsCan enhance conversational skillsCan improve one's ability to solve problemsCan help in managing depressionImproves memoryDihexa also helps one improve focus and learning. That's why this is good most, especially for people who study too.It can even improve heart health, and also boost medical endurance.People who use Dihexa have had testimonies of how this peptide has helped improve their creativity, thinking, and even problem-solving skills.Although you must keep in mind that despite the benefits of Dihexa, it still has some side effects that you must be aware of primarily when it is being regularly used.One who even stops using Dihexa can have severe withdrawal effects once they decide to discontinue using this peptide. Some side effects could be unexpected jitters or even irritability.

Biological Activity

Dihexa is an orally active, blood-brain barrier-permeable angiotensin IV analog; exhibits high affinity binding hepatocyte growth factor (HGF) with a Kd of 65 pM.Dihexa binds with high affinity to HGF and both dihexa and its parent compound Norleucine 1-AngIV induce c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering. Further, dihexa and Nle1-AngIV induce hippocampal spinogenesis and synaptogenesis similar to HGF itself. Dihexa effectively inhibits HGF dimerization at 1 μM. While dihexa at 1 nM and 10 pM alone does not activate c-Met, it markedly augments the capacity of HGF at 1.25 and 2.5 ng/mL to activate c-Met.Dihexa has a long circulating half-life. Dihexa exhibits procognitive activity. Dihexa reverses scopolamine-dependent spatial learning deficits. It improves spatial learning in aged rats. Dihexa induces spinogenesis in cultured hippocampal neurons.

Clinical Use

Dihexa is a peptide variant derived from angiotensin IV which has been found to potently improve cognitive function in animal models of disease such as Alzheimer’s. Angiotensin IV is a derivative of the potent vasoconstrictor angiotensin II and has been shown to enhance acquisition, consolidation, and recall of learning and memory in animal models when administered centrally or peripherally. In an essay of neurotrophic activity, Dihexa was found to be seven orders of magnitude more potent than BDNF. It could possibly help in the repair of the brain and nerves in neurological disease.

Mode of action

Being a first-class compound that is orally active, Dihexa works through penetrating the blood-brain barriers. This also works through facilitating one's memory consolidation and even memory retrieval.Researchers have seen how this peptide is very active. It also shows a very promising characteristic in terms of overcoming any memory and motor dysfunction.

Toxicity evaluation

According to a patent, "Short duration safety studies with Dihexa have uncovered no apparent toxicity. Of particular note is a lack of neoplastic induction, since c-Met is recognized as an oncogene. This is unsurprising since oncogenesis requires multiple mutations including both oncogene induction and tumor suppressor attenuation."

Who Evaluation

Evaluation year: 2010