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Chemical Compound Review

Seglitida     (2S)-6-amino-2-[[(2R)-2- [[(2S)-3-(4...

Synonyms: Seglitidum, AC1MHZC7, LS-186806, LS-187475, 81377-02-8, ...
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Disease relevance of seglitide


High impact information on seglitide

  • 3. In Ltk- cells expressing sst1 receptors, SRIF, SRIF-28, [D-Trp8]-SRIF and CGP 23996 all displaced [125I]-[Tyr11]-SRIF binding with high potency (IC50 values of 0.43 - 1.27 nM) whilst seglitide, BIM-23027, BIM-23056 and L-362855 were either weak inhibitors of binding or were ineffective [2].
  • In contrast to [125I]204-090 or [125I]LTT-SRIF-28 binding, [125I]CGP 23996 binding (in 5 mM MgCl2 buffer) in cerebellar membranes was heterogeneous as indicated by biphasic competition curves produced by sst2 receptor selective ligands such as seglitide or octreotide [3].
  • All somatostatin analogues reduced voltage-activated Ca2+ currents recorded in the whole-cell configuration of the patch-clamp technique, with somatostatin-14 being equipotent to somatostatin-28, but more potent than seglitide [4].
  • At hsst5 receptors Emax varied over a broad range, seglitide, CST17, SRIF28 displaying almost full agonism compared to SRIF14, whereas octreotide and BIM 23052 showed very low partial agonism [5].
  • Displacement of [125I]CGP 23996 (in Mg(2+)-buffer) with seglitide in the molecular layer of the cerebellum, deep layers of the entorhinal cortex, layers I, II and V of the insular cortex and frontal pole yielded complex competition curves suggesting the presence of two populations of SRIF receptors [6].

Anatomical context of seglitide


Associations of seglitide with other chemical compounds

  • In vitro, somatostatin and related peptides, including seglitide (MK-678), hyperpolarize subicular neurones of the burst firing type-a response, which may have functional consequences for their output [8].

Gene context of seglitide

  • SRIF-1 recognition sites were defined in binding studies performed with [125I]MK 678 (seglitide) [9].
  • The high potency of seglitide suggests that the SRIF receptor involved is of the SRIF1 type [7].
  • Thus, SRIF and SRIF28 competed for binding (IC50 values, 0.32 and 0.63 nM, respectively) with Hill slopes less than unity; while seglitide and BIM-23027 both maximally displaced only 30-40% of specific binding with apparent high affinity (respective pIC50 values, 10.1 nM and 10.0) [10].


  1. Somatostatin inhibits excitatory transmission at rat hippocampal synapses via presynaptic receptors. Boehm, S., Betz, H. J. Neurosci. (1997) [Pubmed]
  2. Differences in the operational characteristics of the human recombinant somatostatin receptor types, sst1 and sst2, in mouse fibroblast (Ltk-) cells. Castro, S.W., Buell, G., Feniuk, W., Humphrey, P.P. Br. J. Pharmacol. (1996) [Pubmed]
  3. Localization and pharmacological characterization of somatostatin recognition sites in the human cerebellum. Piwko, C., Thoss, V.S., Probst, A., Hoyer, D. Neuropharmacology (1996) [Pubmed]
  4. A somatostatin receptor inhibits noradrenaline release from chick sympathetic neurons through pertussis toxin-sensitive mechanisms: comparison with the action of alpha 2-adrenoceptors. Boehm, S., Huck, S. Neuroscience (1996) [Pubmed]
  5. Characterisation of human recombinant somatostatin receptors. 4. Modulation of phospholipase C activity. Siehler, S., Hoyer, D. Naunyn Schmiedebergs Arch. Pharmacol. (1999) [Pubmed]
  6. Somatostatin receptors in the rhesus monkey brain: localization and pharmacological characterization. Thoss, V.S., Piwko, C., Hoyer, D. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  7. Somatostatin-induced inhibition of neurotransmission in the mouse isolated vas deferens is resistant to pertussis toxin. Feniuk, W., Humphrey, P.P. Eur. J. Pharmacol. (1994) [Pubmed]
  8. Ventral subiculum administration of the somatostatin receptor agonist MK-678 increases dopamine levels in the nucleus accumbens. Mitchell, S.N., Sharrott, A., Cooper, J., Greenslade, R.G. Eur. J. Pharmacol. (2000) [Pubmed]
  9. Characterization and distribution of somatostatin SS-1 and SRIF-1 binding sites in rat brain: identity with SSTR-2 receptors. Schoeffter, P., Pérez, J., Langenegger, D., Schüpbach, E., Bobirnac, I., Lübbert, H., Bruns, C., Hoyer, D. Eur. J. Pharmacol. (1995) [Pubmed]
  10. Somatostatin receptors mediating inhibition of basal and stimulated electrogenic ion transport in rat isolated distal colonic mucosa. McKeen, E.S., Feniuk, W., Humphrey, P.P. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
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