Synthesis and biological activity of indoline compounds as α_1-AR antagonist / 中国药科大学学报

Aim: To search for novel α_1-adrenoceptor(α_1-AR) antagonists. Methods: On the basis of hybridization principle with silodosin as the lead compound, twelve 5-[2-[4-[ ( substituted phenoxy) alkyl] piperazin-1-yl] propyl] indoline compounds were designed and synthesized by maintaining indoline while incorporating the 1-[(substituted phenoxy) alkyl] piperazine group. Results: The structures of synthesized target compounds were confirmed by the elemental analysis, IR, ESI-MS and ~1H NMR. Preliminary pharmacological test showed that pA_2 values of six target compounds were greater than 7. 50, which suggested that the compounds possessed considerable α_1-AR antagonic activity. Conclusion: 5-[2-[4-[ ( substituted phenoxy) alkyl] piperazin-1-yl] propyl] indoline compounds is potentially a new candidate for α_1-AR antagonist.

Microvascular decompression in treating cranial nerve diseases / 中国综合临床

Objective To study the efficacy of microvascular decompression in treating cranial nerve diseases. Methods 156 patients were treated with microvaseular decompression,of whom 119 were with trigeminal neuralgia,34 with hemifacial spasm and three with glossopharyngeal neuralgia.Rusults The overall effective rate was 96.8%(151/156) and the corresponding effective rate for the above three conditions were 94.2%,97.1% and 66.7%. Conlusions Mierovaseular decompression iS an effective treatment for cranial nerve diseases.