COMBINATION PRODUCT FOR THE INDUCTION AND/OR MAINTENANCE OF GENERAL ANESTHESIA
申请人:BLUMENTECH, S.L.
公开号:US20210186927A1
公开(公告)日:2021-06-24
The state of general anesthesia (GA) is essential to many surgical and medical procedures. This state is characterized by loss of consciousness, deep analgesia and suppression of movements. GA is rarely achieved with a single drug, usually requiring the combination of various pharmacological agents. Each drug can interact with one or more molecular targets affecting neuronal excitability and synaptic transmission in multiple regions of the CNS. Agonists of the μ-opioid receptor are commonly used in GA to cause analgesia, but not to induce or maintain loss of consciousness or movement suppression. Additionally, agonists of the μ-opioid receptor can cause serious unwanted side effects, e.g. respiratory depression. The present invention provides alternative combination products based on K-opioid receptor agonists. These combination products unexpectedly induced loss of consciousness, and were able to achieve and maintain GA. Furthermore, the combination products suppressed pain perception without the need of a μ-opioid receptor agonist. The combination of Salvinorin A, a selective κ-opioid receptor agonist, with Diazepam or Medetomidine surprisingly led to rapid consciousness, deep analgesia and movement suppression. This combination was found to effectively induce and maintain a state of general anesthesia.
A one-pot telescopic synthesis of benzo[<i>b</i>]carbazoles and exploration of their liquid crystalline properties
作者:Nirmal Malik、Ritobrata De、Santanu Kumar Pal、S. S. V. Ramasastry
DOI:10.1039/d4cc00721b
日期:2024.4.30
describe a diversity-oriented one-pot telescopic synthesis of various benzo[b]carbazoles with the naphthannulation of indoles as the key step, enabled by an intramolecular furan–olefin Diels–Alder reaction. This strategy is general and efficient across a wide range of substrates. We applied this method to synthesize and characterize the first benzo[b]carbazole-based liquid crystalline materials, where
我们描述了各种苯并[ b ]咔唑的多样性导向的一锅式伸缩合成,以吲哚的环烷化作为关键步骤,通过分子内呋喃-烯烃Diels-Alder反应实现。该策略在多种基材上都是通用且有效的。我们应用这种方法合成并表征了第一个苯并[ b ]咔唑基液晶材料,其中独特的分子设计导致在室温下形成罕见的向列相。