4800-58-2Relevant articles and documents
Evaluation of the antidepressant therapeutic potential of isocyanine and pseudoisocyanine analogues of the organic cation decynium-22
Krause-Heuer, Anwen M.,Fraser-Spears, Rheaclare,Dobrowolski, Jeremy C.,Ashford, Mark E.,Wyatt, Naomi A.,Roberts, Maxine P.,Gould, Georgianna G.,Cheah, Wai-Ching,Ng, Clarissa K.L.,Bhadbhade, Mohan,Zhang, Bo,Greguric, Ivan,Wheate, Nial J.,Kumar, Naresh,Koek, Wouter,Callaghan, Paul D.,Daws, Lynette C.,Fraser, Benjamin H.
, p. 476 - 487 (2017/06/20)
Herein we describe the synthesis and evaluation of antidepressant properties of seven analogues (1–7) of the low affinity/high capacity transporter blocker decynium-22 (D-22). All analogues (1–7) were synthesized via base promoted coupling reactions between N-alkylated-2-methylquinolinium iodides or N-alkylated-4-methylquinolinium iodides and electrophilic N-alkylated-2-iodoquinolinium iodides. All final compounds were purified by re-crystallization or preparative HPLC and initial evaluation studies included; 1) screening for in vitro α1-adrenoceptor activity (a property that can lead to unwanted side-effects), 2) measuring antidepressant-like activity in a mouse tail suspension test (TST), and 3) measuring effects upon mouse locomotion. The results showed some analogues have lower affinities at α1-adrenoceptors compared to D-22 and showed antidepressant-like activity without the need for co-administration of SSRIs. Additionally, many analogues did not affect mouse locomotion to the same extent as D-22. Plans for additional evaluations of these promising analogues, including measurement of antidepressant-like activity with co-administration of selective serotonin re-uptake inhibitors (SSRIs), are outlined.
