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Chemical Compound Review

Lopac-L-110     1-methyl-N-[(1R,5S)-8-methyl- 8...

Synonyms: AC1NSKB5, CHEMBL291046, LS-81435, DCL000728, DNC000902, ...
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High impact information on LY278584

  • The selective 5-HT3 receptor antagonist, LY278584 maleate, (1.0 mg/kg i.v.) caused no detectable reduction in the response to 100 micrograms/kg of 5-HT [1].
  • The binding had the pharmacological properties of a 5HT3 receptor, being potently inhibited by a variety of 5HT3 agonists and antagonists including (S)-zacopride (Ki = 0.032 nM), Quipazine (Ki = 0.45 nM), LY278584 (Ki = 0.5 nM), (1-m-chlorophenyl)-biguanide (Ki = 0.6 nM) and ICS 205-930 (Ki = 1.0 nM) [2].
  • In these oocytes, 5-HT, the selective 5-HT3 receptor agonists, 2-methyl-5-HT and m-chlorophenylbiguanide activated an inward current which was sensitive to the specific 5-HT3 receptor antagonist LY278584 [3].

Anatomical context of LY278584


  1. Serotonin-induced pulmonary responses are mediated by the 5-HT2 receptor in the mouse. Martin, T.R., Cohen, M.L., Drazen, J.M. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  2. Synthesis and evaluation of [125I]-(S)-iodozacopride, a high affinity radioligand for 5HT3 receptors. Gehlert, D.R., Schober, D.A., Gackenheimer, S.L., Mais, D.E., Ladouceur, G., Robertson, D.W. Neurochem. Int. (1993) [Pubmed]
  3. Effect of cocaine on the 5-HT3 receptor-mediated ion current in Xenopus oocytes. Fan, P., Oz, M., Zhang, L., Weight, F.F. Brain Res. (1995) [Pubmed]
  4. Identification and distribution of 5-HT3 recognition sites in the rat gastrointestinal tract. Champaneria, S., Costall, B., Naylor, R.J., Robertson, D.W. Br. J. Pharmacol. (1992) [Pubmed]
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