MD-354: what is it good for?
MD-354 (meta-chlorophenylguanidine) has been identified as a member of a novel class of 5-HT(3) serotonin receptor agonists. MD-354 is a 5-HT(3) 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 alpha-adrenoceptors (ARs) and displays an affinity for alpha(2B)-ARs comparable to its affinity for 5-HT(3) 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.
Dukat
Malgorzata
M
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA. mdukat@vcu.edu
Glennon
Richard A
RA
Young
Shawquia
S
D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D003000:Clonidine / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D006146:Guanidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D051379:Mice; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D000700:Analgesics; D006146:Guanidines; D017366:Serotonin Receptor Agonists; C495409:m-chlorophenylguanidine; D003000:Clonidine