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. 2007 Apr 24;13(1):1–20. doi: 10.1111/j.1527-3458.2007.00002.x

MD‐354: What is It Good For?

Małgorzata Dukat 1, Richard A Glennon 1, Shawquia Young 1
PMCID: PMC6494146  PMID: 17461887

ABSTRACT

MD‐354 (meta‐chlorophenylguanidine) has been identified as a member of a novel class of 5‐HT3 serotonin receptor agonists. MD‐354 is a 5‐HT3 receptor partial agonist that has been shown to behave as an agonist in some assays, and as an antagonist in others. MD‐354 also binds at α‐adrenoceptors (ARs) and displays an affinity for α2B‐ARs comparable to its affinity for 5‐HT3 receptors. Although devoid of antinociceptive actions following systemic administration alone, MD‐354 markedly enhances the antinociceptive actions of clonidine in the mouse tail‐flick assay without potentiating the sedative side effects of clonidine. Although studies with MD‐354 are still in progress, some pharmacological findings are described here. MD‐354‐related agents may represent drug adjuvants for the relief of severe pain.

Keywords: α2‐Adrenoceptors, Antinociception, Clonidine, Drugs of abuse, 5‐HT3 receptors, MD‐354, Pain

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Acknowledgments

Acknowledgments We wish to acknowledge the NIMH Psychoactive Drug Screening Program for providing the binding profile on arylguanidines and clonidine. This study was supported in part by IRG‐73‐001‐28 from the American Cancer Society (MD) and J‐778 from the Jeffress Foundation (MD).

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