📜6-甲基吡嗪-3-甲腈置于pd-Baso4 盐酸,氢气体系中,用 溶剂黄146 用作溶剂,化学反应 5.0H,反应生成6-甲基-3哒嗪甲基胺
参考文献:High-Efficacy 5-Ht1A Agonists For Antidepressant Treatment: A Renewed Opportunity
标题:High-Efficacy 5-Ht1A Agonists For Antidepressant Treatment: A Renewed Opportunity
摘要:We Report The Discovery Of Novel 5-Ht1A Receptor Agonists And Describe The Process That Led To The Antidepressant Candidate 9 (F 15599). 9 Has Nanomolar Affinity For 5-Ht1A Binding Sites And Is Over 1000-Fold Selective With Respect To The Other 5-Ht1 Receptor Subtypes,5-Ht2-7 Receptor Families,And Also Numerous Gpcrs,Transporters,Ion Channels,And Enzymes. In A Cellular Model Of Signal Transduction,9 Activates H5-Ht1A Receptors With An Efficacy Superior To That Of The Prototypical 5-Ht1A Agonist (+/-)-8-Oh-Dpat And Comparators Undergoing Clinical Trials. After Acute Oral Administration In Rats,9 Totally Reverses Immobility In The Forced Swimming Test And Produces Behaviors Characteristic Of 5-Ht1A Receptor Activation. However,These Effects occurred At Widely Separated Doses,Suggesting That 9 Discriminates Between Distinct Populations Of 5-Ht1A Receptors. While The Clinical Relevance Of These Observations Is Still Unknown,This Opens New Perspectives For The Treatment Of Depressive Disorders.
Doi:10.1021/jm070714L