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Chemical Compound Review

SIB-1508Y     but-2-enedioic acid; 3-ethynyl-5-(1...

Synonyms: AC1O5WWQ, DNC001325, LS-173698, SIB 1765F, 179120-52-6, ...
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Disease relevance of SIB-1508Y


Psychiatry related information on SIB-1508Y

  • Finally, in an attempt to determine whether the psychostimulant profile of nicotinic agonists could be dissociated from their effects on attention, we compared the (R)- and (S)-enantiomers of SIB 1765F in the 5-CSRTT, and in their ability to increase locomotor activity [2].
  • The effect of SIB-1508Y on learned helplessness was still apparent 1 week following drug administration and was also maintained after 4 weeks of daily administration [3].
  • Preclinical studies suggest that SIB-1508Y is a candidate for the treatment of the motor and cognitive deficits of Parkinson's disease, whereas SIB-1553A appears to have potential as a candidate for the treatment of Alzheimer's disease [4].

High impact information on SIB-1508Y

  • RESULTS: Similarly to imipramine and fluoxetine, subchronic treatment (5 days) with SIB-1508Y reversed the escape deficit in the learned helplessness model in a dose dependent manner [3].
  • Thus, SIB-1508Y may be useful in the treatment of the cognitive deficits in Parkinson's disease [5].
  • SIB-1765F mimicked (-)-nicotine in stimulating [3H]-DA release from rat striatal and olfactory tubercle slices, with EC50 values of 99.6 and 39.6 microM, respectively [6].
  • SIB-1765F is a subtype selective NAChR agonist that displaces [3H]-nicotine binding with an IC50 of 4.6 nM and [3H]-cytisine binding with an IC50 of 12.2 nM which is 2000- to 6000-fold lower than its displacement of [3H]-QNB or [125I]-alpha-bungarotoxin [6].

Chemical compound and disease context of SIB-1508Y


  1. Interactions between a novel cholinergic ion channel agonist, SIB-1765F and L-DOPA in the reserpine model of Parkinson's disease in rats. Menzaghi, F., Whelan, K.T., Risbrough, V.B., Rao, T.S., Lloyd, G.K. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  2. Reversal of a vigilance decrement in the aged rat by subtype-selective nicotinic ligands. Grottick, A.J., Haman, M., Wyler, R., Higgins, G.A. Neuropsychopharmacology (2003) [Pubmed]
  3. Antidepressant-like effects of the subtype-selective nicotinic acetylcholine receptor agonist, SIB-1508Y, in the learned helplessness rat model of depression. Ferguson, S.M., Brodkin, J.D., Lloyd, G.K., Menzaghi, F. Psychopharmacology (Berl.) (2000) [Pubmed]
  4. The potential of subtype-selective neuronal nicotinic acetylcholine receptor agonists as therapeutic agents. Lloyd, G.K., Menzaghi, F., Bontempi, B., Suto, C., Siegel, R., Akong, M., Stauderman, K., Velicelebi, G., Johnson, E., Harpold, M.M., Rao, T.S., Sacaan, A.I., Chavez-Noriega, L.E., Washburn, M.S., Vernier, J.M., Cosford, N.D., McDonald, L.A. Life Sci. (1998) [Pubmed]
  5. Nicotinic acetylcholine receptor agonist SIB-1508Y improves cognitive functioning in chronic low-dose MPTP-treated monkeys. Schneider, J.S., Tinker, J.P., Van Velson, M., Menzaghi, F., Lloyd, G.K. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  6. Pharmacological characterization of SIB-1765F: a novel cholinergic ion channel agonist. Sacaan, A.I., Reid, R.T., Santori, E.M., Adams, P., Correa, L.D., Mahaffy, L.S., Bleicher, L., Cosford, N.D., Stauderman, K.A., McDonald, I.A., Rao, T.S., Lloyd, G.K. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
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