Tesamorelin

DESCRIPTION

Tesamorelin is a growth hormone releasing hormone analog that has been shown to
increase IGF-1 levels in men by an average of 181 micrograms/liter. It binds and
stimulates GHRH receptors with similar potency as endogenous GHRH. It has a host
of other benefits including nootropic effects and reducing triglycerides.

Tesamorelin has subsequently been shown to decrease carotid intima-media
thickness (cIMT), Visceral adipose tissue (VAT), and C-reactive protein (CRP) in a
recent study. It has not been shown to significantly affect other pituitary hormones
and their respective mechanisms in the body. Additionally, it has been shown to
improve cognitive function for healthy older adults and also for people with mild
cognitive

PROTOCOL

Content & Potency: 24 1mg lyophilized vials, 10ml vial of sterile water for
reconstitution
Suggested dosage: 1 mg injected subcutaneously before bed about 90 minutes
after last food intake

CLINICAL RESEARCH

The Procognitive and Synaptogenic Effects of Angiotensin IV–Derived
Peptides Are Dependent on Activation of the Hepatocyte Growth Factor/c-Met
System

A subset of angiotensin IV (AngIV)–related molecules are known to possess
procognitive/antidementia properties and have been considered as templates for
potential therapeutics. However, this potential has not been realized because of
two factors: 1) a lack of blood-brain barrier–penetrant analogs, and 2) the absence
of a validated mechanism of action. The pharmacokinetic barrier has recently been
overcome with the synthesis of the orally active, blood-brain barrier–permeable
analog N-hexanoic-tyrosine-isoleucine-(6) aminohexanoic amide (dihexa).
Therefore, the goal of this study was to elucidate the mechanism that underlies
dihexa’s procognitive activity. Here, we demonstrate that dihexa binds with high
affinity to hepatocyte growth factor (HGF) and both dihexa and its parent
compound Norleucine 1-AngIV (Nle1-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. These actions were inhibited by an HGF
antagonist and a short hairpin RNA directed at c-Met. Most importantly, the
procognitive/antidementia capacity of orally delivered dihexa was blocked by an
HGF antagonist delivered intracerebroventricularly as measured using the Morris
water maze task of spatial learning.

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