NEUROPHYSIN I (NPI)
In combination with oxytocin, it inhibits steroid production.Steroids also have some negative effects on mental health.
* Severe mood swings,
* Paranoia and delusion,
* Common sense of disturbance, Invincibility feelings,
* Madness and anger known as “Sharp anger” that can cause violence.
The hormone estrogen stimulates the production of oxytocin and its carrier, neurophysin 1.
NEUROPHYSIN II (NPII)
The antidiuretic hormone (ADH or vasopressin) regulates the volume and osmolarity of urine through the kidneys, controls the water excretion and maintains the water balance without changing the homeostatic control and excretion of other substances.
It is synthesized in neuroendocrine cells located in the supraoptic and paraventricular nuclei of the hypothalamus. The synthesized hormone is carried along the hypothalamo-pituitary tract due to the carrier protein called neurophysin-II and stored at the nerve endings in the neurohypophysis. When the supraoptic and paraventricular nuclei are stimulated for osmolarity or other reasons, the impulses move downwards, reaching the nerve endings and increasing membrane permeability to calcium ions.
Stored in vesicles at the end of the nerve, ADH is released by exocytosis in response to an increase in calcium permeability. ADH and neurophysin are released together, but since they are loosely attached to each other, ADH is instantly separated from neurophysis. Neurophysis has no known function after leaving the nerve endings. The released ADH is carried to the systemic circulation by the neurohypophysis capillary circulation.
NEUROMEDIN U(NMU)
NMU exerts its biological effects via two G protein-coupled receptors, NMUR1 and NMUR2. NMUR1 is mostly found in the periphery whereas NMUR2, the receptor of our interest, is most abundant in the central nervous system. The purpose of this study is to develop new peptidergic selective NMUR2 antagonists which are enzymatically stable and blood-brain-barrier (BBB) permeable.
NMU-8, a natural occurring form of NMU, is taken as lead molecule for the synthesis of new analogues. The NMU-ligands are synthesized via solid phase peptide synthesis under classical conditions on rink amide polystyrene resin. A first batch of analogues is prepared on basis of the available structure-activity relationships. The in vitro characterization of these peptides is performed by an inositol phosphate accumulation assay.
The results of this in vitro characterization are generally in line with the available literature. EC50 values of a similar magnitude are found for NMU-8. Moreover our experiments revealed that acetylation of the N-terminus leads in general to an increase of the relative activity compared to the non-acetylated ligand. In conclusion, further research is needed to synthesize a NMUR2 selective, enzymatically stable and BBB permeable ligand.
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