31408-47-6Relevant 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.
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl] piperidine series of histamine H3 receptor antagonists
Berlin, Michael,Ting, Pauline C.,Vaccaro, Wayne D.,Aslanian, Robert,McCormick, Kevin D.,Lee, Joe F.,Albanese, Margaret M.,Mutahi, Mwangi W.,Piwinski, John J.,Shih, Neng-Yang,Duguma, Luli,Solomon, Daniel M.,Zhou, Wei,Sher, Rosy,Favreau, Leonard,Bryant, Matthew,Korfmacher, Walter A.,Nardo, Cymbelene,West Jr., Robert E.,Anthes, John C.,Williams, Shirley M.,Wu, Ren-Long,Susan She,Rivelli, Maria A.,Corboz, Michel R.,Hey, John A.
, p. 989 - 994 (2007/10/03)
A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.