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Chemical Compound Review

AC1Q5JOY     2-[[(2S,3S)-2-[[(2S)-2- [[(2S)-1-[(2S)-2...

Synonyms: AR-1K5634, AC1L3XA4, 60482-95-3, neurotensin (8-13), Arg-arg-pro-tyr-ile-leu
 
 
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Disease relevance of Arg-arg-pro-tyr-ile-leu

  • A series of novel analogs of neurotensin (8-13) was synthesized, and a structure-activity study was done comparing the abilities of these peptides to stimulate intracellular cyclic GMP production in intact neuroblastoma clone N1E-115 and to inhibit the binding of [3H]neurotensin to these cells and to membranal preparations from human brain [1].
 

High impact information on Arg-arg-pro-tyr-ile-leu

  • Pharmacological and biochemical profiles of unique neurotensin 8-13 analogs exhibiting species selectivity, stereoselectivity, and superagonism [2].
  • Silaproline was also substituted for proline in a neurotensin (8-13) analogue that retained biological activity and exhibited enhanced resistance to biodegradation [3].
  • The number of nigral cells expressing tyrosine hydroxylase mRNA was found to increase by 40% after injection of neurotensin or its active fragment (neurotensin 8-13) [4].
  • In this study, the residues that were important to the biochemical and binding activities of neurotensin (8-13) proved to be identical to the amino acids that are necessary for the functional integrity of native neurotensin (Gilbert JA et al., Biochem Pharmacol 35: 391-397, 1986 [1].
  • A sensitive and specific radioimmunoassay (RIA) for Lys8, Asn9, neurotensin 8-13 (LANT-6) has been developed which utilizes 125I-labeled LANT-6 and rabbit antisera raised towards conjugates of synthetic LANT-6 and bovine thyroglobulin [5].
 

Anatomical context of Arg-arg-pro-tyr-ile-leu

  • Potencies of the bovine neurotensin 8-13 fragment and its different coloured and penta-lysine derivatives were compared in isolated longitudinal muscle strips of guinea pig ileum [6].
 

Associations of Arg-arg-pro-tyr-ile-leu with other chemical compounds

 

Analytical, diagnostic and therapeutic context of Arg-arg-pro-tyr-ile-leu

References

  1. Neurotensin(8-13): comparison of novel analogs for stimulation of cyclic GMP formation in neuroblastoma clone N1E-115 and receptor binding to human brain and intact N1E-115 cells. Gilbert, J.A., McCormick, D.J., Pfenning, M.A., Kanba, K.S., Enloe, L.J., Moore, A., Richelson, E. Biochem. Pharmacol. (1989) [Pubmed]
  2. Pharmacological and biochemical profiles of unique neurotensin 8-13 analogs exhibiting species selectivity, stereoselectivity, and superagonism. Cusack, B., McCormick, D.J., Pang, Y.P., Souder, T., Garcia, R., Fauq, A., Richelson, E. J. Biol. Chem. (1995) [Pubmed]
  3. Influence of silaproline on peptide conformation and bioactivity. Cavelier, F., Vivet, B., Martinez, J., Aubry, A., Didierjean, C., Vicherat, A., Marraud, M. J. Am. Chem. Soc. (2002) [Pubmed]
  4. Neurotensin increases tyrosine hydroxylase messenger RNA-positive neurons in substantia nigra after retrograde axonal transport. Burgevin, M.C., Castel, M.N., Quarteronet, D., Chevet, T., Laduron, P.M. Neuroscience (1992) [Pubmed]
  5. Radioimmunoassay for Lys8, Asn9, neurotensin 8-13: tissue and subcellular distribution of immunoreactivity in chickens. Carraway, R.E., Ruane, S.E., Ritsema, R.S. Peptides (1983) [Pubmed]
  6. Coloured peptides: synthesis, properties and use in preparation of peptide sub-library kits. Sebestyén, F., Szendrei, G., Mák, M., Dóda, M., Illyés, E., Szókán, G., Kindla, K., Rapp, W., Szegö, P., Câmpian, E., Furka, A. J. Pept. Sci. (1998) [Pubmed]
  7. Electrophysiological effects of neurotensin on dopaminergic neurones of the ventral tegmental area of the rat in vitro. Seutin, V., Massotte, L., Dresse, A. Neuropharmacology (1989) [Pubmed]
  8. Specific binding of tritiated neurotensin to rat brain membranes: characterization and regional distribution. Goedert, M., Pittaway, K., Williams, B.J., Emson, P.C. Brain Res. (1984) [Pubmed]
 
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