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Chemical Compound Review

SureCN9485783     1-methyl-N-(8-methyl-8...

Synonyms: CCG-204826, BPBio1_000507, Lopac0_000741, AC1Q5GMX, AR-1C4727, ...
 
 
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High impact information on LY-278584

  • Control velocity ranged from 0.5 to 3.3 mm/s; mean +/- S.E.M., 1.3 +/- 0.1 mm/s. The 5-HT4 antagonist, GR 113808A, and the 5-HT3 antagonist, LY 278584, decreased the velocity of pellet propulsion in a concentration-dependent fashion (39 +/- 2% and 47 +/- 1% decrease at 10 microM, respectively) [1].
  • Maximal DA induced currents were 37 +/- 3% of maximal 5-HT responses and blocked the specific 5-HT3 antagonist LY-278584 (0.1 microM) [2].
  • MDL 72222 (1-a-H-3-a-5-aH-optropan-3yl-3,5-dichlorobenzoate) and LY 278584 (1-methyl-N-(8-methyl-8-azabicyclo[3.2.1.]oct-3-yl)-1H-indazole-3- carboxamide) inhibited [3H]flunitrazepam binding with Ki values of approximately 20 microM; ICS 205-930 (3 alpha-tropanyl-1H-indole-3-carboxylic acid ester) was more potent with a Ki of 0.8 microM [3].
  • The 5-HT3 antagonists zacopride and LY 278584 (ID50 = 0.02 micrograms/kg) antagonized the MDMA discriminative stimulus [4].

References

  1. Propulsion in guinea pig colon induced by 5-hydroxytryptamine (HT) via 5-HT4 and 5-HT3 receptors. Jin, J.G., Foxx-Orenstein, A.E., Grider, J.R. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  2. Direct activation by dopamine of recombinant human 5-HT1A receptors: comparison with human 5-HT2C and 5-HT3 receptors. Oz, M., Zhang, L., Rotondo, A., Sun, H., Morales, M. Synapse (2003) [Pubmed]
  3. Effects of 5-HT3 receptor antagonists on binding and function of mouse and human GABAA receptors. Klein, R.L., Sanna, E., McQuilkin, S.J., Whiting, P.J., Harris, R.A. Eur. J. Pharmacol. (1994) [Pubmed]
  4. Further studies on N-methyl-1(3,4-methylenedioxyphenyl)-2-aminopropane as a discriminative stimulus: antagonism by 5-hydroxytryptamine3 antagonists. Glennon, R.A., Higgs, R., Young, R., Issa, H. Pharmacol. Biochem. Behav. (1992) [Pubmed]
 
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