Agomelatine
Background
Agomelatine is anagonist of melatonin receptors uye anopikisa serotonin 5-HT2C receptor ine Ki values ye0.062nM uye 0.268nM uye IC50 kukosha kwe0.27μM, zvakateerana kune MT1, MT2 uye 5-HT2C [1].
Agomelatine yakasarudzika antidepressant uye inogadzirwa kurapa hombe depressive disorder (MDD). Agomelatine inosarudza kupikisa 5-HT2C. Iyo inoratidza yakaderera affinities kune akaumbwa vanhu 5-HT2A uye 5-HT1A. Kune melatonin receptors, agomelatine inoratidza zvakafanana affinities kune akaumbwa munhu MT1 uye MT2 ine Ki values dze0.09nM uye 0.263nM, zvichiteerana. Mune in vivo zvidzidzo, agomelatine inokonzera kuwedzera kwe dopamine uye noradrenaline mazinga kuburikidza nekuvhara iyo inhibitory yekupinda ye5-HT2C. Uyezve, hutongi hweagomelatine hunopesana nekudzikira-kunokonzera kuderera mukushandiswa kwe sucrose mune rat modhi yekuora mwoyo. Kunze kweizvozvo, agomelatine inoderedza kusagadzikana kwekuita mune yerodent modhi yekushushikana [1].
References:
[1] Zupancic M, Guilleminault C. Agomelatine. CNS mishonga, 2006, 20 (12): 981-992.
Chimiro chemakemikari





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