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Literature DB >> 20965726

5-benzyloxytryptamine as an antagonist of TRPM8.

Jeff DeFalco¹, Daniel Steiger, Michelle Dourado, Daniel Emerling, Matthew A J Duncton.

Abstract

5-Benzyloxytryptamine 19 was found to act as an antagonist of the TRPM8 ion-channel. For example, 19 had an IC(50) of 0.34 μM when menthol was used as the stimulating agonist. Related commercially-available tryptamine derivatives showed diminished, or no antagonist activity at TRPM8. The structural similarity of 5-benzyloxytryptamine to other literature TRPM8 antagonists was noted.

Entities: Chemical Gene

Mesh：

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Year: 2010 PMID： 20965726 DOI： 10.1016/j.bmcl.2010.09.099

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

11 in total

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Journal: Pflugers Arch Date: 2014-06-18 Impact factor: 3.657

5-benzyloxytryptamine as an antagonist of TRPM8.

Review 1. Transient receptor potential (TRP) channels: a clinical perspective.

2. Strategies for therapeutic hypometabothermia.

3. Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.

4. Odontoblasts as sensory receptors: transient receptor potential channels, pannexin-1, and ionotropic ATP receptors mediate intercellular odontoblast-neuron signal transduction.

Review 5. Modulation of thermoreceptor TRPM8 by cooling compounds.

6. Pharmacological blockade of TRPM8 ion channels alters cold and cold pain responses in mice.

7. Comparing structural fingerprints using a literature-based similarity benchmark.

8. A high throughput screening method for the nano-crystallization of salts of organic cations.

9. Activation of host transient receptor potential (TRP) channels by praziquantel stereoisomers.

10. Selenium and Neurological Diseases: Focus on Peripheral Pain and TRP Channels.