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Chemical Compound Review

SureCN2678917     1-[6-[[(8S,9S,13S,14S,17S)-3- methoxy-13...

Synonyms: U6881_SIGMA, u-73343, AC1L3G0Q, U 73343
 
 
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Psychiatry related information on u-73343

 

High impact information on u-73343

  • U-73122 (1 microM) completely inhibited the effect of ETA-mediated ET-1 stimulation of IP production, whereas U-73343 was inactive [2].
  • The PLC inhibitor U-73122 blocked both agonist- and cell swelling-induced I(Cl, swell), while its inactive analogue U-73343 had no effect [3].
  • In contrast, U-73343 (with Ca2+ channel blockers) did not inhibit the TRH effect on PRL (control: 24.3 +/- 2.1; TRH: 51.0 +/- 6.3 ng/well).(ABSTRACT TRUNCATED AT 400 WORDS)[4]
  • LPG-stimulated [Ca(2+)](i) increase was inhibited by U-73122 but not by U-73343, suggesting that LPG stimulates calcium signaling via phospholipase C activation [5].
  • Moreover, the phospholipase C (PLC) inhibitor U-73122, but not its inactive stereoisomer U-73343 (5 microM), significantly reduced the ATP-evoked [Ca2+]i rise [6].
 

Biological context of u-73343

  • The succinimido analogue, U-73343, also inhibited the binding of [3H]mepyramine (estimated IC50 24+/-1 microM), but NEM was only a weak inhibitor, even at 10 mM [7].
  • Similarly, when the effects of U-73122 and U-73343 were measured on [3H]phosphatidylinositol hydrolysis of islets, both compounds caused a slight, non-specific inhibition of phospholipase C activity [8].
 

Anatomical context of u-73343

 

Associations of u-73343 with other chemical compounds

 

Gene context of u-73343

  • The phospholipase C inhibitor, U-73122 inhibited INSC and the sustained Ca2+ plateau during agonist stimulation whereas the inactive analogue, U-73343 had no effect [11].
  • The inactive analog, U-73343, had no effect on the secretory response to NT [12].

References

  1. H1-receptor stimulation induces hyperalgesia through activation of the phospholipase C-PKC pathway. Galeotti, N., Malmberg-Aiello, P., Bartolini, A., Schunack, W., Ghelardini, C. Neuropharmacology (2004) [Pubmed]
  2. Dual control of seminiferous tubule contractility mediated by ETA and ETB endothelin receptor subtypes. Tripiciano, A., Palombi, F., Ziparo, E., Filippini, A. FASEB J. (1997) [Pubmed]
  3. Ca(2+)- and volume-sensitive chloride currents are differentially regulated by agonists and store-operated Ca2+ entry. Zholos, A., Beck, B., Sydorenko, V., Lemonnier, L., Bordat, P., Prevarskaya, N., Skryma, R. J. Gen. Physiol. (2005) [Pubmed]
  4. U-73122, an aminosteroid phospholipase C antagonist, noncompetitively inhibits thyrotropin-releasing hormone effects in GH3 rat pituitary cells. Smallridge, R.C., Kiang, J.G., Gist, I.D., Fein, H.G., Galloway, R.J. Endocrinology (1992) [Pubmed]
  5. Effect of lysophosphatidylglycerol on several signaling molecules in OVCAR-3 human ovarian cancer cells: Involvement of pertussis toxin-sensitive G-protein coupled receptor. Park, K.S., Kim, M.K., Im, D.S., Bae, Y.S. Biochem. Pharmacol. (2007) [Pubmed]
  6. Characterization of the Ca2+ responses evoked by ATP and other nucleotides in mammalian brain astrocytes. Centemeri, C., Bolego, C., Abbracchio, M.P., Cattabeni, F., Puglisi, L., Burnstock, G., Nicosia, S. Br. J. Pharmacol. (1997) [Pubmed]
  7. The interaction of U-73122 with the histamine H1 receptor: implications for the use of U-73122 in defining H1 receptor-coupled signalling pathways. Hughes, S.A., Gibson, W.J., Young, J.M. Naunyn Schmiedebergs Arch. Pharmacol. (2000) [Pubmed]
  8. U-73122 does not specifically inhibit phospholipase C in rat pancreatic islets and insulin-secreting beta-cell lines. Alter, C.A., Amagasu, M., Shah, K., Jolly, Y.C., Major, C., Wolf, B.A. Life Sci. (1994) [Pubmed]
  9. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. Bleasdale, J.E., Thakur, N.R., Gremban, R.S., Bundy, G.L., Fitzpatrick, F.A., Smith, R.J., Bunting, S. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  10. U-73122, a phospholipase C antagonist, inhibits effects of endothelin-1 and parathyroid hormone on signal transduction in UMR-106 osteoblastic cells. Tatrai, A., Lee, S.K., Stern, P.H. Biochim. Biophys. Acta (1994) [Pubmed]
  11. Nonselective cation channels in endothelial cells derived from human umbilical vein. Kamouchi, M., Mamin, A., Droogmans, G., Nilius, B. J. Membr. Biol. (1999) [Pubmed]
  12. Neurotensin stimulation of mast cell secretion is receptor-mediated, pertussis-toxin sensitive and requires activation of phospholipase C. Barrocas, A.M., Cochrane, D.E., Carraway, R.E., Feldberg, R.S. Immunopharmacology (1999) [Pubmed]
 
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