3898-07-5Relevant articles and documents
Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia
Hammoud, Hassan,Elhabazi, Khadija,Quillet, Rapha?lle,Bertin, Isabelle,Utard, Valérie,Laboureyras, Emilie,Bourguignon, Jean-Jacques,Bihel, Frederic,Simonnet, Guy,Simonin, Frederic,Schmitt, Martine
, (2018/05/15)
Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's). Binding experiments and functional assays highlighted AGH 1n and its rigidified analog 2-amino-dihydropyrimidine 22e for in vivo experiments. As earlier shown with the prototypical dipeptide antagonist RF9, both 1n and 22e reduced significantly the long lasting fentanyl-induced hyperalgesia in rodents. Altogether these data indicate that AGH rigidification maintains nanomolar affinities for both NPFF receptors, while improving antagonist character towards NPFF1R.
Synthesis and Biological Activity of Some New 1-Aryl-2-S-methyl-5-(2-pyridyl/2-furfuryl)isodithiobiurets
Shridhar, D. R.,Gandhi, S. S.,Rao, K. Srinivasa,Rastogi, K.
, p. 716 - 717 (2007/10/02)
A number of 1-aryl-2-S-methyl-5-(2-pyridyl/2-furfuryl)isodithiobiurets (II and III) have been synthesized by the condensation of various N-aryl-S-methylisothioureas (V) with 2-pyridyl- and 2-furfurylisothiocyanates and tested for anthelmintic, antiamoebic, antitrichomonal, antileishmanial and antimicrobial activities.
A Convenient Synthesis of Mono-, N,N'-Di-, and Tri-substituted Selenoureas from Methyl Carbamimidothioates (S-Methylpseudothioureas)
Cohen, Victor Israel
, p. 60 - 63 (2007/10/02)
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