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Chemical Compound Review

Ebiratida     (4S)-4-[[(1R)-1-[[(1S)-1- [[(1R)-5-amino-1...

Synonyms: Ebiratide, Ebiratidum, AC1L2HGJ, UNII-CM5J1V7AUT, Ebiratidum [Latin], ...
 
 
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Psychiatry related information on Ebiratide

  • In an acute trial, three different dosages (60, 300, and 600 micrograms) of the endocrinologically inert but behaviorally active corticotropin 4-9 (ACTH4-9) fragment ebiratide were given to three patients with clinically probable Alzheimer's disease and five patients with a major depressive episode who were psychomotorly retarded [1].
  • With all five training and testing procedures (inhibitory avoidance test with ECS- or scopolamine-induced amnesia, up-hill avoidance, one-way shuttle box avoidance and eight-arm radial maze) ebiratide was most effective in a dose range of 1-10 micrograms/kg SC [2].
 

High impact information on Ebiratide

  • We investigated the permeability of the BBB in normal and injured states to two markers of permeability (albumin and sucrose), to a peptide (ebiratide), and to a cytokine [tumor necrosis factor-alpha(TNF)] [3].
  • The penetration of the alpha-MSH/ACTH analogue ebiratide and of TNF, substances that have saturable transport systems across the BBB and may be involved in regenerative processes in the CNS, followed a regional pattern of differential permeability comparable to that of albumin and sucrose [3].
  • Blood-brain barrier permeability to ebiratide and TNF in acute spinal cord injury [3].
  • Transport mechanism of a new behaviorally highly potent adrenocorticotropic hormone (ACTH) analog, ebiratide, through the blood-brain barrier [4].
  • The binding and internalization of a novel adrenocorticotropic hormone (ACTH) analog having a potent neuromodulating effect, ebiratide (H-Met(O2)-Glu-His-Phe-D-Lys-Phe-NH(CH2)8NH2), by isolated bovine brain capillaries, were examined [4].
 

Biological context of Ebiratide

 

Anatomical context of Ebiratide

 

Associations of Ebiratide with other chemical compounds

  • Metabolism of [5-125I-His]ebiratide occurred during a 30-min incubation with bovine brain capillaries at 37 degrees C. In the presence of 20 mM EDTA, added to inhibit this metabolism, the medium, after 30 min of incubation, contained 82.3 +/- 0.5% of the unchanged ebiratide [4].
  • Sodium glycocholate and sodium caprate had no significant enhancing effect on the permeability of the jejunal membrane, but significantly enhanced the permeation of ebiratide through the colonic membrane [5].
  • 2. Several studies were performed in normal male controls to investigate the effect of antidepressants (brofaromine, moclobemide, amitriptyline, clomipramine and trimipramine) and of neuropeptides (CRH and the ACTH (4-9) fragment analog ebiratide) on the sleep EEG and sleep-associated hormone secretion [10].
 

Analytical, diagnostic and therapeutic context of Ebiratide

References

  1. Behavioral effects of a synthetic corticotropin 4-9 analog in patients with depression and patients with Alzheimer's disease. Heuser, I., Heuser-Link, M., Gotthardt, U., Grasser, A., Holsboer, F. Journal of clinical psychopharmacology. (1993) [Pubmed]
  2. Learning and memory processes of an ACTH4-9 analog (ebiratide; Hoe 427) in mice and rats. Hock, F.J., Gerhards, H.J., Wiemer, G., Usinger, P., Geiger, R. Peptides (1988) [Pubmed]
  3. Blood-brain barrier permeability to ebiratide and TNF in acute spinal cord injury. Pan, W., Banks, W.A., Kastin, A.J. Exp. Neurol. (1997) [Pubmed]
  4. Transport mechanism of a new behaviorally highly potent adrenocorticotropic hormone (ACTH) analog, ebiratide, through the blood-brain barrier. Shimura, T., Tabata, S., Ohnishi, T., Terasaki, T., Tsuji, A. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  5. Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes. Yamamoto, A., Okagawa, T., Kotani, A., Uchiyama, T., Shimura, T., Tabata, S., Kondo, S., Muranishi, S. J. Pharm. Pharmacol. (1997) [Pubmed]
  6. The neurotrophic effects of ebiratide, an analog of ACTH4-9, on cultured septal cells and aged rats. Matsumoto, T., Tsuda, S., Nakamura, S. J. Neural Transm. Gen. Sect. (1995) [Pubmed]
  7. Percutaneous absorption of physiologically active peptides, ebiratide and elcatonin, in rats. Ogiso, T., Paku, T., Iwaki, M., Tanino, T., Nishioka, S. Biol. Pharm. Bull. (1994) [Pubmed]
  8. Brain transfer of a new neuromodulating ACTH analog, ebiratide, in rats. Shimura, T., Tabata, S., Hayashi, S. Peptides (1991) [Pubmed]
  9. Absorptive-mediated endocytosis of an adrenocorticotropic hormone (ACTH) analogue, ebiratide, into the blood-brain barrier: studies with monolayers of primary cultured bovine brain capillary endothelial cells. Terasaki, T., Takakuwa, S., Saheki, A., Moritani, S., Shimura, T., Tabata, S., Tsuji, A. Pharm. Res. (1992) [Pubmed]
  10. The sleep EEG and nocturnal hormonal secretion studies on changes during the course of depression and on effects of CNS-active drugs. Steiger, A., von Bardeleben, U., Guldner, J., Lauer, C., Rothe, B., Holsboer, F. Prog. Neuropsychopharmacol. Biol. Psychiatry (1993) [Pubmed]
  11. High-performance liquid chromatography with fluorescence detection of ebiratide using 4-(N,N-dimethylamino-sulphonyl)-7-fluoro-2,1,3-benzoxadiazole as a fluorogenic reagent. Hamachi, Y., Tsujiyama, T., Nakashima, K., Akiyama, S. Biomed. Chromatogr. (1995) [Pubmed]
  12. In-vivo blood-brain barrier transport of a novel adrenocorticotropic hormone analogue, ebiratide, demonstrated by brain microdialysis and capillary depletion methods. Shimura, T., Tabata, S., Terasaki, T., Deguchi, Y., Tsuji, A. J. Pharm. Pharmacol. (1992) [Pubmed]
  13. Susceptibility of ebiratide to proteolysis in rat intestinal fluid and homogenates and its protection by various protease inhibitors. Okagawa, T., Fujita, T., Murakami, M., Yamamoto, A., Shimura, T., Tabata, S., Kondo, S., Muranishi, S. Life Sci. (1994) [Pubmed]
 
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