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Chemical Compound Review

Seglitide acetate     (3S,6S,9S,12S,15S,18S)-9-(4- aminobutyl)-3...

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Disease relevance of Seglitide acetate

  • The effects of MK 678 were reversible and blocked by pertussis toxin pretreatment, suggesting that SSTR2 couples to the L-type Ca2+ channels via G proteins [1].

Psychiatry related information on Seglitide acetate


High impact information on Seglitide acetate

  • In contrast, the somatostatin analogs SMS 201-995, IM 4-28, and MK-678 failed to displace specific binding in transfected cells [3].
  • Binding of the SST analogue MK 678 to the solubilized receptor was completely inhibited by guanosine 5'-O-thiotriphosphate (IC50 = 100 nM), reflecting decreased receptor affinity for agonist following uncoupling of the receptor and G protein(s) [4].
  • Treatment of AtT-20 cells in culture with neuraminidase (V. cholera) greatly reduces high affinity [125I] MK 678 binding sites, but did not alter the maximal ability of SRIF to inhibit forskolin-stimulated cAMP accumulation in intact AtT-20 cells [5].
  • The two receptors exhibited similar affinities for a number of SSTR2-selective agonists such as MK-678 [6].
  • In contrast, the SSTR2 receptor was insensitive to CGP 23996-like compounds but bound MK 678 with high affinity [7].

Biological context of Seglitide acetate


Anatomical context of Seglitide acetate


Associations of Seglitide acetate with other chemical compounds

  • Treatment of the receptor with endoglycosidase D did not affect the specific binding of [125I] MK 678 to the solubilized SRIF receptors, consistent with the finding from lectin affinity chromatography that high mannose-type carbohydrate structures were not associated with SRIF receptors [5].
  • The binding of 125I-MK-678 to SRIF1 receptors was monophasically inhibited by SRIF, the octapeptides (such as SMS-201-995), and the hexapeptides (such as MK-678), consistent with the highly selective labeling of a subtype of SRIF receptor [13].
  • Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria [14].
  • The sst(1) agonist L-797,591 (10(-5) M) mimicked the effect of CH-275, while MK-678 and L-803,087 at the same concentration were unable to influence somatostatin levels [15].
  • In addition to SRIF-14 and SRIF-28, the most potent SRIF peptides were the cyclic octapeptides, BIM-23014C, BIM-23023, SMS 201-995, and the cyclic hexapeptides, MK-678 and BIM-23027 [16].

Gene context of Seglitide acetate

  • The SSTR1 receptor could also bind CGP 23996-like compounds but not MK 678 [7].
  • The inhibition by MK-678 was incomplete, indicating this peptide is highly selective for a subtype of SRIF receptor that we have termed the SRIF1 receptor [13].
  • In experiments using in-gel kinase assays, MK-678 also inhibited EGF-stimulated ERK activity via a pertussis toxin sensitive pathway, and this effect resulted in inhibition of Elk-1 transcriptional activity [17].
  • SRIF1 receptors have high affinity for MK 678, whereas SRIF2 receptors have no affinity for MK 678 but selectively bind peptides with structures similar to that of CGP 23996 [7].
  • Subtypes of SRIF receptors are found in the CNS that are distinguished by their sensitivities to the cyclic hexapeptide MK-678, such that SRIF1 receptors are sensitive to MK-678 and SRIF2 receptors are insensitive to MK-678 [13].


  1. Somatostatin receptor subtypes SSTR2 and SSTR5 couple negatively to an L-type Ca2+ current in the pituitary cell line AtT-20. Tallent, M., Liapakis, G., O'Carroll, A.M., Lolait, S.J., Dichter, M., Reisine, T. Neuroscience (1996) [Pubmed]
  2. Somatostatin receptors. Raynor, K., Reisine, T. Critical reviews in neurobiology. (1992) [Pubmed]
  3. Molecular cloning and functional expression of a brain-specific somatostatin receptor. Bruno, J.F., Xu, Y., Song, J., Berelowitz, M. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  4. Brain somatostatin receptor-G protein interaction. G alpha C-terminal antibodies demonstrate coupling of the soluble receptor with Gi(1-3) but not with Go. Murray-Whelan, R., Schlegel, W. J. Biol. Chem. (1992) [Pubmed]
  5. Structural analysis and functional role of the carbohydrate component of somatostatin receptors. Rens-Domiano, S., Reisine, T. J. Biol. Chem. (1991) [Pubmed]
  6. Splice variant of the somatostatin receptor 2 subtype, somatostatin receptor 2B, couples to adenylyl cyclase. Reisine, T., Kong, H., Raynor, K., Yano, H., Takeda, J., Yasuda, K., Bell, G.I. Mol. Pharmacol. (1993) [Pubmed]
  7. Pharmacological properties of two cloned somatostatin receptors. Rens-Domiano, S., Law, S.F., Yamada, Y., Seino, S., Bell, G.I., Reisine, T. Mol. Pharmacol. (1992) [Pubmed]
  8. Blood pressure reduction in hypertensive-diabetic rats by the somatostatin analog MK-678. Hartmann, J., Szemplinski, M., Chen, S.L., Slater, E. Life Sci. (1989) [Pubmed]
  9. Transient expression of somatostatin receptors in the brain during development. Leroux, P., Bodenant, C., Bologna, E., Gonzalez, B., Vaudry, H. Ciba Found. Symp. (1995) [Pubmed]
  10. Subtypes of brain somatostatin receptors couple to multiple cellular effector systems. Raynor, K., Wang, H.L., Dichter, M., Reisine, T. Mol. Pharmacol. (1991) [Pubmed]
  11. Differential coupling of somatostatin1 receptors to adenylyl cyclase in the rat striatum vs. the pituitary and other regions of the rat brain. Raynor, K., Reisine, T. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  12. Differential agonist activity of somatostatin and L-362855 at human recombinant sst4 receptors. Smalley, K.S., Feniuk, W., Humphrey, P.P. Br. J. Pharmacol. (1998) [Pubmed]
  13. Analogues of somatostatin bind selectively to brain somatostatin receptor subtypes. Raynor, K., Coy, D.C., Reisine, T. J. Neurochem. (1992) [Pubmed]
  14. Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria. Dimech, J., Feniuk, W., Humphrey, P.P. Br. J. Pharmacol. (1993) [Pubmed]
  15. The somatostatin receptor (sst1) modulates the release of somatostatin in the nucleus accumbens of the rat. Vasilaki, A., Papasava, D., Hoyer, D., Thermos, K. Neuropharmacology (2004) [Pubmed]
  16. Somatostatin (SSTR2) receptors mediate phospholipase C-independent Ca2+ mobilization in rat AR42J pancreas cells. Taylor, J.E. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
  17. Molecular mechanisms for somatostatin inhibition of c-fos gene expression. Todisco, A., Takeuchi, Y., Yamada, J., Sadoshima, J.I., Yamada, T. Am. J. Physiol. (1997) [Pubmed]
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