220652-02-8Relevant articles and documents
A convenient synthesis of disubstituted guanidines via the Mitsunobu protocol
Kim, Hwa-Ok,Mathew, Felix,Ogbu, Cyprian
, p. 193 - 194 (1999)
An efficient synthetic method for the preparation of disubstituted guanidines is described. Primary and secondary alcohols were treated with guanylating agents under Mitsunobu conditions and their subsequent reactions with amines provided disubstituted guanidines.
Design, synthesis, and: In vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H3 receptor antagonists
Staszewski, Marek,Stasiak, Anna,Karcz, Tadeusz,McNaught Flores, Daniel,Fogel, Wies?awa Agnieszka,Kie?-Kononowicz, Katarzyna,Leurs, Rob,Walczyński, Krzysztof
supporting information, p. 234 - 251 (2019/03/02)
Previously, we have shown that 1-substituted-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine with electron withdrawing substituents at position 4 in the benzyl moiety exhibits high in vitro affinities toward the guinea pig jejunal histamine H3/sub
Development of a peptidomimetic antagonist of neuropeptide FF receptors for the prevention of opioid-induced hyperalgesia
Bihel, Frédéric,Humbert, Jean-Paul,Schneider, Séverine,Bertin, Isabelle,Wagner, Patrick,Schmitt, Martine,Laboureyras, Emilie,Petit-Demouliere, Beno?t,Schneider, Elodie,Mollereau, Catherine,Simonnet, Guy,Simonin, Frédéric,Bourguignon, Jean-Jacques
, p. 438 - 445 (2015/03/30)
Through the development of a new class of unnatural ornithine derivatives as bioisosteres of arginine, we have designed an orally active peptidomimetic antagonist of neuropeptide FF receptors (NPFFR). Systemic low-dose administration of this compound to rats blocked opioid-induced hyperalgesia, without any apparent side-effects. Interestingly, we also observed that this compound potentiated opioid-induced analgesia. This unnatural ornithine derivative provides a novel therapeutic approach for both improving analgesia and reducing hyperalgesia induced by opioids in patients being treated for chronic pain.