BIM-23027

BIM-23027
Identifiers
  • (3S,6S,9S,12R,15S,18S)-9-(4-aminobutyl)-3,15-dibenzyl-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-1,18-dimethyl-1,4,7,10,13,16-hexazacyclooctadecane-2,5,8,11,14,17-hexone
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC43H54N8O7
Molar mass794.954 g·mol−1
3D model (JSmol)
  • C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1C)CC2=CC=CC=C2)[C@@H](C)O)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=CC=C5
  • InChI=1S/C43H54N8O7/c1-26-38(53)47-34(22-28-14-6-4-7-15-28)40(55)48-35(24-30-25-45-32-19-11-10-18-31(30)32)41(56)46-33(20-12-13-21-44)39(54)50-37(27(2)52)42(57)49-36(43(58)51(26)3)23-29-16-8-5-9-17-29/h4-11,14-19,25-27,33-37,45,52H,12-13,20-24,44H2,1-3H3,(H,46,56)(H,47,53)(H,48,55)(H,49,57)(H,50,54)/t26-,27+,33-,34-,35+,36-,37-/m0/s1
  • Key:XDLJZSJKUWEHIA-ZKVPYEFOSA-N

BIM-23027 is a cyclic hexapeptide which acts as a selective agonist at somatostatin receptor 2. It inhibits secretion of various hormones and increases dopamine release in brain tissue, however due to poor pharmacokinetic properties its use has mainly been restricted to basic research into the function of SSRT2 receptors and distinguishing their action from other somatostatin receptor subtypes.[1][2][3][4][5][6]

See also

References

  1. ↑ McKeen ES, Feniuk W, Humphrey PP (October 1995). "Somatostatin receptors mediating inhibition of basal and stimulated electrogenic ion transport in rat isolated distal colonic mucosa". Naunyn-Schmiedeberg's Archives of Pharmacology. 352 (4): 402–411. doi:10.1007/BF00172777. PMID 8532068.
  2. ↑ Dimech J, Feniuk W, Latimer RD, Humphrey PP (November 1995). "Somatostatin-induced contraction of human isolated saphenous vein involves sst2 receptor-mediated activation of L-type calcium channels". Journal of Cardiovascular Pharmacology. 26 (5): 721–728. doi:10.1097/00005344-199511000-00008. PMID 8637186.
  3. ↑ Hathway GJ, Humphrey PP, Kendrick KM (November 1999). "Evidence that somatostatin sst2 receptors mediate striatal dopamine release". British Journal of Pharmacology. 128 (6): 1346–1352. doi:10.1038/sj.bjp.0702934. PMC 1571763. PMID 10578151.
  4. ↑ Booth CE, Kirkup AJ, Hicks GA, Humphrey PP, Grundy D (August 2001). "Somatostatin sst(2) receptor-mediated inhibition of mesenteric afferent nerves of the jejunum in the anesthetized rat". Gastroenterology. 121 (2): 358–369. doi:10.1053/gast.2001.26335. PMID 11487545.
  5. ↑ Hannon JP, Nunn C, Stolz B, Bruns C, Weckbecker G, Lewis I, et al. (2002). "Drug design at peptide receptors: somatostatin receptor ligands". Journal of Molecular Neuroscience. 18 (1–2): 15–27. doi:10.1385/JMN:18:1-2:15. PMID 11931345.
  6. ↑ Connor M, Bagley EE, Mitchell VA, Ingram SL, Christie MJ, Humphrey PP, et al. (August 2004). "Cellular actions of somatostatin on rat periaqueductal grey neurons in vitro". British Journal of Pharmacology. 142 (8): 1273–1280. doi:10.1038/sj.bjp.0705894. PMC 1575200. PMID 15265812.
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