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Chemical Compound Review

SureCN10599789     (8R,9R,10S,11S,13S,14S,17S)- 11,17...

Synonyms: AC1L3XAP, AR-1H7323, RU 362, RU28362, RU 28362, ...
 
 
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Disease relevance of RU 362

  • 3. Hyperaldosteronism secondary to dietary Na+ depletion for 10-14 days, dexamethasone (600 micrograms 100 g-1 day-1 for 3 days), and RU 28362 (600 micrograms 100 g-1 day-1 for 3 days) induced amiloride-sensitive electrogenic Na+ transport, with the potency of aldosterone greater than dexamethasone greater than RU 28362 [1].
  • In primary cortical neurons, hypoxia increased Bnip3 mRNA expression and this was exacerbated with RU28362 treatment [2].
  • The aldosterone-induced increase in body weight gain and carcass water were attenuated by RU-28362 (type II receptor agonist) infusion, suggesting that type II receptor stimulation can antagonize the effect of type I receptor stimulation [3].
 

Psychiatry related information on RU 362

  • Because we found previously that RU 28362 infused into the hippocampus does not affect water maze acquisition or immediate recall, the findings suggest that the GR agonist-induced retention impairment was attributable to a selective influence on long-term memory retrieval [4].
 

High impact information on RU 362

  • Furthermore, atenolol (0.5 microg) blocked the memory-enhancing effects of the specific glucocorticoid receptor (GR or type II) agonist RU 28362 infused concurrently into the BLA immediately posttraining [5].
  • Both Ca2+ action potentials and voltage-activated Ca2+ currents (N- and L-like) were increased by 2-hr exposure to the synthetic GC receptor agonist, RU 28362 [6].
  • In contrast, acute administration of CORT (the endogenous type I and type II receptor agonist), or RU28362 (a specific type II receptor agonist), to adrenalectomized animals produced changes in leukocyte distribution that were similar to those observed in intact animals during stress [7].
  • The type II receptor agonist RU 28362 had an effect similar to that of dex; at both 10(-6) and 10(-8) M, RU 28362 inhibited CRF-induced increases in POMC hnRNA in p1 NIL and p1 and p10 AL.(ABSTRACT TRUNCATED AT 400 WORDS)[8]
  • Such an effect is mediated via glucocorticoid receptors (GRs), since it is mimicked by the glucocorticoid analogue RU28362 (100 nm) and prevented by the GR antagonist RU38486 (1 micro m) [9].
 

Biological context of RU 362

 

Anatomical context of RU 362

  • Receptor binding, measured using [3H]RU 28362, was stable in all regions (pituitary, hypothalamus, amygdala, and frontal cortex) except the hippocampus, where there was about a 40% decrease in binding capacity, with no change in the affinity of the receptor for RU 28362 [15].
  • Cortisol-21-sulfate (FS) is a specific ligand for intracellular transcortin: demonstration of three types of high affinity corticosteroid binders in bovine aortic cytosol by a combined use of FS and RU 28362 [16].
  • The majority of the well characterized effects of adrenal steroids on peripheral blood immune cells (increased neutrophils and decreased lymphocytes and monocytes) were reproduced by the type II receptor agonist, RU28362 [17].
  • In contrast to RU28362, however, aldosterone significantly decreased the number of neutrophils [17].
  • Administration of synthetic glucocorticoids (RU 28362 or dexamethasone) induced a robust increase in the intensity of immunostaining in cell nuclei of neurosecretory cells [18].
 

Associations of RU 362 with other chemical compounds

  • Injections of the type II glucocorticoid (GR) receptor agonist, RU 28362, into adrenalectomized rats differentially stimulates the synthesis of the 35,000 Mr protein compared with the mineralocorticoid aldosterone, which has a higher affinity for the type I (CR) receptor.(ABSTRACT TRUNCATED AT 250 WORDS)[19]
  • When rat splenocytes were preincubated with high concentrations (0.1-1 microM) of corticosterone (CORT) or with the specific glucocorticoid agonist RU 28362 (0.1 microM) for 1-6 h, washed, and then exposed to the T-cell mitogen Concanavalin-A, a time- and dose-dependent inhibition of lymphocyte mitogenesis over the next 3 days of culture was found [20].
  • Additionally, GR and MR mRNA levels were measured after ip injection of adrenalectomized rats with pharmacological doses of either the pure glucocorticoid agonist RU 28362 or the mineralocorticoid agonist aldosterone in combination with the glucocorticoid antagonist RU 38486 (blocks aldosterone binding to the GR) [21].
  • The specific glucocorticoid receptor (GR or type II) agonist RU 28362 (1.0, 3.0 or 10 ng) was infused into the BLA either alone or together with atropine immediately after training [22].
  • The current studies evaluated the effects of the synthetic glucocorticoid receptor (GR) agonist, RU 28362, and the endogenous, non-selective receptor ligand, corticosterone (Cort), on pituitary luteinizing hormone (LH) secretion in male rats [23].
 

Gene context of RU 362

  • Using in situ hybridization, we have examined the regulation of the messenger RNAs (mRNAs) encoding the glucocorticoid and mineralocorticoid receptors, by aldosterone, which acts selectively through MR, and by RU28362, which acts selectively through GR [24].
  • In order to discriminate the mineralocorticoid from the glucocorticoid actions exerted by corticosterone, F344 and Brown Norway adrenalectomized rats were treated with increasing doses (1, 5 and 25 microg/ml of drinking water) of deoxycorticosterone (DOC, MR-specific ligand) or RU 28362 (GR-specific ligand) [25].
  • Treatment of the cells with 0.01-10 micrograms/ml bacterial lipopolysaccharides (LPS) caused a dose-dependent increase (up to 10-fold) in FS mRNA steady state level in AEC, whereas 1-1000 nM RU 28362, a synthetic glucocorticoid, inhibited FS mRNA steady state levels in a dose-dependent manner [26].
  • Hippocampal GFAP mRNA (2.9 kb) decreases in a dose-dependent manner in response to CORT by RNA blot hybridization using a mouse GFAP cRNA probe; a similar decrease in response to the glucocorticoid agonist, RU 28362, is consistent with a type II glucocorticoid receptor-mediated effect [27].
  • The selective glucocorticoid RU 28362 associated rapidly with hippocampal GR, attaining maximum binding within 4 h, and dissociated with a t1/2 of 34.8 h [28].
 

Analytical, diagnostic and therapeutic context of RU 362

References

  1. Effects of corticosteroid hormones on the electrophysiology of rat distal colon: implications for Na+ and K+ transport. Binder, H.J., McGlone, F., Sandle, G.I. J. Physiol. (Lond.) (1989) [Pubmed]
  2. Glucocorticoids exacerbate hypoxia-induced expression of the pro-apoptotic gene Bnip3 in the developing cortex. Sandau, U.S., Handa, R.J. Neuroscience (2007) [Pubmed]
  3. Interaction of type I and type II corticosteroid receptor stimulation on carcass energy and carcass water. White, B.D., Edwards, G.L., Martin, R.J. Am. J. Physiol. (1996) [Pubmed]
  4. Glucocorticoid effects on memory retrieval require concurrent noradrenergic activity in the hippocampus and basolateral amygdala. Roozendaal, B., Hahn, E.L., Nathan, S.V., de Quervain, D.J., McGaugh, J.L. J. Neurosci. (2004) [Pubmed]
  5. Glucocorticoid enhancement of memory storage involves noradrenergic activation in the basolateral amygdala. Quirarte, G.L., Roozendaal, B., McGaugh, J.L. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  6. Hippocampal glucocorticoid receptor activation enhances voltage-dependent Ca2+ conductances: relevance to brain aging. Kerr, D.S., Campbell, L.W., Thibault, O., Landfield, P.W. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  7. Stress-induced changes in blood leukocyte distribution. Role of adrenal steroid hormones. Dhabhar, F.S., Miller, A.H., McEwen, B.S., Spencer, R.L. J. Immunol. (1996) [Pubmed]
  8. Developmental regulation of proopiomelanocortin gene expression in the fetal and neonatal rat pituitary. Scott, R.E., Pintar, J.E. Mol. Endocrinol. (1993) [Pubmed]
  9. Glucocorticoids modulate neurotransmitter-induced glycogen metabolism in cultured cortical astrocytes. Allaman, I., Pellerin, L., Magistretti, P.J. J. Neurochem. (2004) [Pubmed]
  10. Hippocampal homosynaptic long-term depression/depotentiation induced by adrenal steroids. Pavlides, C., Kimura, A., Magariños, A.M., McEwen, B.S. Neuroscience (1995) [Pubmed]
  11. Effects of the glucocorticoid agonist, RU28362, and the antagonist RU486 on lung phosphatidylcholine and antioxidant enzyme development in the genetically obese Zucker rat. Langley, S.C., Rickett, G.W., Hunt, A., Kelly, F.J., Postle, A.D., York, D.A. Biochem. Pharmacol. (1993) [Pubmed]
  12. Further studies of brain aldosterone binding sites employing new mineralocorticoid and glucocorticoid receptor markers in vitro. Coirini, H., Magariños, A.M., De Nicola, A.F., Rainbow, T.C., McEwen, B.S. Brain Res. (1985) [Pubmed]
  13. Effects of aldosterone or RU28362 treatment on adrenalectomy-induced cell death in the dentate gyrus of the adult rat. Woolley, C.S., Gould, E., Sakai, R.R., Spencer, R.L., McEwen, B.S. Brain Res. (1991) [Pubmed]
  14. Acute glucocorticoid pretreatment suppresses stress-induced hypothalamic-pituitary-adrenal axis hormone secretion and expression of corticotropin-releasing hormone hnRNA but does not affect c-fos mRNA or fos protein expression in the paraventricular nucleus of the hypothalamus. Ginsberg, A.B., Campeau, S., Day, H.E., Spencer, R.L. J. Neuroendocrinol. (2003) [Pubmed]
  15. Age-related changes in glucocorticoid receptor binding and mRNA levels in the rat brain and pituitary. Peiffer, A., Barden, N., Meaney, M.J. Neurobiol. Aging (1991) [Pubmed]
  16. Cortisol-21-sulfate (FS) is a specific ligand for intracellular transcortin: demonstration of three types of high affinity corticosteroid binders in bovine aortic cytosol by a combined use of FS and RU 28362. Hayashi, T., Kornel, L. Endocrinology (1990) [Pubmed]
  17. Effects of selective type I and II adrenal steroid agonists on immune cell distribution. Miller, A.H., Spencer, R.L., hassett, J., Kim, C., Rhee, R., Ciurea, D., Dhabhar, F., McEwen, B., Stein, M. Endocrinology (1994) [Pubmed]
  18. Glucocorticoid receptor in magnocellular neurosecretory cells. Kiss, J.Z., Van Eekelen, J.A., Reul, J.M., Westphal, H.M., De Kloet, E.R. Endocrinology (1988) [Pubmed]
  19. Receptor specificity of a glucocorticoid- and stress-induced hippocampal protein. Schlatter, L.K., Dokas, L.A. J. Neurosci. (1989) [Pubmed]
  20. Enhancement of rat splenic lymphocyte mitogenesis after short term preexposure to corticosteroids in vitro. Wiegers, G.J., Reul, J.M., Holsboer, F., de Kloet, E.R. Endocrinology (1994) [Pubmed]
  21. In contrast to glucocorticoid receptors, mineralocorticoid receptors are not autoregulated in rat distal colon epithelia. Meyer, A.S., Schmidt, T.J. Endocrinology (1994) [Pubmed]
  22. Glucocorticoid enhancement of memory consolidation in the rat is blocked by muscarinic receptor antagonism in the basolateral amygdala. Power, A.E., Roozendaal, B., McGaugh, J.L. Eur. J. Neurosci. (2000) [Pubmed]
  23. Effects of peripheral versus central administration of the endogenous glucocorticoid, corticosterone, and the glucocorticoid receptor agonist, RU 28362, on LH release in male rats. Briski, K.P. Brain Res. (1995) [Pubmed]
  24. Regulation of glucocorticoid receptor and mineralocorticoid receptor messenger ribonucleic acids by selective agonists in the rat hippocampus. Chao, H.M., Ma, L.Y., McEwen, B.S., Sakai, R.R. Endocrinology (1998) [Pubmed]
  25. Is the mineralocorticoid receptor in Brown Norway rats constitutively active? Marissal-Arvy, N., Ribot, E., Sarrieau, A., Mormède, P. J. Neuroendocrinol. (2000) [Pubmed]
  26. Production of follistatin in porcine endothelial cells: differential regulation by bacterial compounds and the synthetic glucocorticoid RU 28362. Michel, U., Schneider, O., Kirchhof, C., Meisel, S., Smirnov, A., Wiltfang, J., Rieckmann, P. Endocrinology (1996) [Pubmed]
  27. Messenger RNA for glial fibrillary acidic protein is decreased in rat brain following acute and chronic corticosterone treatment. Nichols, N.R., Osterburg, H.H., Masters, J.N., Millar, S.L., Finch, C.E. Brain Res. Mol. Brain Res. (1990) [Pubmed]
  28. Binding characteristics of mineralocorticoid and glucocorticoid receptors in dog brain and pituitary. Reul, J.M., de Kloet, E.R., van Sluijs, F.J., Rijnberk, A., Rothuizen, J. Endocrinology (1990) [Pubmed]
  29. Corticosteroid effects on morphine-induced antinociception as a function of two types of corticosteroid receptors in brain. Ratka, A., Veldhuis, H.D., De Kloet, E.R. Neuropharmacology (1988) [Pubmed]
  30. Effects of adrenalectomy and corticosterone replacement on glucocorticoid receptor levels in rat brain tissue: a comparison between western blotting and receptor binding assays. O'Donnell, D., Francis, D., Weaver, S., Meaney, M.J. Brain Res. (1995) [Pubmed]
  31. Aldosterone modulates glucocorticoid receptor binding in hippocampal cell cultures via the mineralocorticoid receptor. O'Donnell, D., Meaney, M.J. Brain Res. (1994) [Pubmed]
  32. Activation of the type 2 adrenal steroid receptor can rescue granule cells from death during development. Gould, E., Tanapat, P., McEwen, B.S. Brain Res. Dev. Brain Res. (1997) [Pubmed]
 
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