Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Editor

Personal info

View

About

Terms

Javascript disabled

Please enable Javascript support in your browser to use this application.

Instructions on how to enable JavaScript on different browsers can be found here: http://www.google.com/support/bin/answer.py?answer=23852.

[edit this page]

Chemical Compound Review:

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

Synonyms: AC1NSKB5, CHEMBL291046, LS-81435, DCL000728, DNC000902, ...

Gehlert, D.R. et al., Fan, P. et al., Champaneria, S. et al., Martin, T.R. et al.

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

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. Tritiated derivatives of the potent and selective 5-HT3 receptor antagonists GR65630 and LY278584 were used to identify 5-HT3 recognition sites in the rat gastrointestinal tract [4].

References

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]
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]
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]
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]

Contributions to this collaborative article are from individual authors of WikiGenes or mined by the WikiGenes Data Mining Engine from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use apsburg

The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

Editor

Share