1-(2-fluorophenyl)ethyl N-(1-azabicyclo[2.2.2]octan-3-yl)carbamate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(2-fluorophenyl)ethyl N-(1-azabicyclo[2.2.2]octan-3-yl)carbamate
• 化学式: C₁₆H₂₁FN₂O₂
• 分子量: 292.35
• InChiKey: HQYLURGLNKLOQJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists
  申请人：——

  公开号：US20030166654A1

  公开（公告）日：2003-09-04

  The invention provides compounds of formula (I) wherein n, A, R 1 , R 2 and R 3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

  该发明提供了式（I）中的化合物，其中n，A，R1，R2和R3如描述中定义，并提供其制备方法。式（I）中的化合物可用作药物。
• Inhibition of inflammation using alpha 7 receptor-binding cholinergic agonists
  申请人：The Feinstein Institute for Medical Research

  公开号：EP1949901A2

  公开（公告）日：2008-07-30

  Methods of inhibiting release of a proinflammatory cytokine from a macrophage are provided. The methods comprise treating the macrophage with a cholinergic agonist in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from the macrophage, wherein the cholinergic agonist is selective for an α7 nicotinic receptor. Methods for inhibiting an inflammatory cytokine cascade in a patient are also provided. The methods comprise treating the patient with a cholinergic agonist in an amount sufficient to inhibit the inflammatory cytokine cascade, wherein the cholinergic agonist is selective for an α7 nicotinic receptor. Methods for determining whether a compound is a cholinergic agonist reactive with an α7 nicotinic receptor are also provided. The methods comprise determining whether the compound inhibits release of a proinflammatory cytokine from a mammalian cell. Additionally, methods for determining whether a compound is a cholinergic antagonist reactive with an α7 nicotinic receptor are provided. These methods comprise determining whether the compound reduces the ability of a cholinergic agonist to inhibit the release of a proinflammatory cytokine from a mammalian cell. Oligonucleotides or mimetics capable of inhibiting attenuation of lipopolysaccharide-induced TNF release from a mammalian macrophage upon exposure of the macrophage to a cholinergic agonist are also provided. The oligonucleotides or mimetics consist essentially of a sequence greater than 5 nucleotides long that is complementary to an mRNA of an α7 receptor. Additionally, methods of inhibiting attenuation of TNF release from a mammalian macrophage upon exposure of the macrophage to a cholinergic agonist are provided. These methods comprise treating the macrophage with the above-described oligonucleotide or mimetic.

  提供了抑制巨噬细胞释放促炎细胞因子的方法。这些方法包括用胆碱能激动剂处理巨噬细胞，其用量足以减少从巨噬细胞释放的促炎细胞因子的量，其中胆碱能激动剂对α7烟碱受体具有选择性。还提供了抑制患者炎症细胞因子级联的方法。这些方法包括用足以抑制炎症细胞因子级联的胆碱能激动剂治疗患者，其中胆碱能激动剂对α7烟碱受体具有选择性。还提供了确定化合物是否是与 α7 尼古丁受体反应的胆碱能激动剂的方法。这些方法包括确定化合物是否抑制哺乳动物细胞释放促炎细胞因子。此外，还提供了确定化合物是否是与α7烟碱受体反应的胆碱能拮抗剂的方法。这些方法包括确定化合物是否降低了胆碱能激动剂抑制哺乳动物细胞释放促炎细胞因子的能力。还提供了能够在哺乳动物巨噬细胞暴露于胆碱能激动剂时抑制减弱脂多糖诱导的TNF从该巨噬细胞释放的寡核苷酸或模拟物。寡核苷酸或模拟物基本上由长度大于 5 个核苷酸的序列组成，该序列与 α7 受体的 mRNA 互补。此外，还提供了在哺乳动物巨噬细胞暴露于胆碱能激动剂时抑制其 TNF 释放的方法。这些方法包括用上述寡核苷酸或模拟物处理巨噬细胞。
• Treatment of bleeding by non-invasive stimulation
  申请人：The Feinstein Institutes for Medical Research

  公开号：US10912712B2

  公开（公告）日：2021-02-09

  Devices, systems and methods for stimulating (e.g., noninvasively) a subject's inflammatory reflex are provided to reduce bleed time. The method may include the step of non-invasively stimulating the inflammatory reflex (e.g., the vagus nerve, the splenic nerve, the hepatic nerve, the facial nerve, and the trigeminal nerve) of a subject, such as by mechanical stimulation, in a manner which significantly reduces bleed time in the subject. Devices for non-invasively stimulating the inflammatory reflex may include a movable tip or actuator that is controlled to mechanically stimulate the ear. The devices may be hand-held or wearable, and may stimulate the cymba conchae region of the subject's ear.

  提供了用于刺激（例如非侵入式）受试者炎症反射的设备、系统和方法，以缩短出血时间。该方法可包括非侵入性刺激受试者炎症反射（如迷走神经、脾神经、肝神经、面神经和三叉神经）的步骤，例如通过机械刺激，以显著缩短受试者的出血时间。用于非侵入性刺激炎症反射的设备可包括一个可移动的尖端或致动器，控制其对耳朵进行机械刺激。这些装置可以是手持式的，也可以是可穿戴式的，可以刺激受试者耳朵的钹状海螺区。
• Treatment of pancreatitis using alpha 7 receptor-binding cholinergic agonists
  申请人：Tracey J. Kevin

  公开号：US20050137218A1

  公开（公告）日：2005-06-23

  A method of treating a patient suffering from pancreatitis comprising treating said patient with a therapeutically effective amount of a cholinergic agonist selective for an α7 nicotinic receptor in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from a macrophage wherein said condition is acute pancreatitis. The compounds of the present invention include a quaternary analog of cocaine; (1-aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid 1-(2-fluorophenyl)-ethyl ester; a compound of formula (I), a compound of formula (II), a compound of formula (III), a compound of formula (IV), and an oligonucleotide or mimetic capable of attenuating the symptoms of acute pancreatitis wherein the oligonucleotide or mimetic consists essentially of a sequence greater than 5 nucleotides long that is complementary to an mRNA of an α7 cholinergic receptor. The variables of formulae (I), (II), (III) and (IV) are described herein.

  一种治疗胰腺炎患者的方法，包括用治疗有效量的选择性α7烟碱受体的胆碱能激动剂治疗所述患者，其量足以减少从巨噬细胞释放的促炎细胞因子的量，其中所述病症为急性胰腺炎。本发明的化合物包括可卡因的季类似物；(1-氮杂双环[2.2.2]辛-3-基)-氨基甲酸 1-(2-氟苯基)-乙基酯；式(I)化合物、式(II)化合物、式(III)化合物、式(IV)化合物和能减轻急性胰腺炎症状的寡核苷酸或模拟物，其中寡核苷酸或模拟物基本上由长度大于5个核苷酸的序列组成，该序列与α7胆碱能受体的mRNA互补。式(I)、(II)、(III)和(IV)的变量已在此描述。
• Neural tourniquet
  申请人：Tracey J. Kevin

  公开号：US20050282906A1

  公开（公告）日：2005-12-22

  Disclosed is a method of reducing bleed time in a subject by activation of the cholinergic anti-inflammatory pathway in said subject. The cholinergic anti-inflammatory pathway can be activated by direct or indirect stimulation of the vagus nerve. The cholinergic anti-inflammatory pathway can also be activated by administering an effective amount of cholinergic agonist or acetylcholinesterase inhibitor to the subject.

  本发明公开了一种通过激活受试者体内的胆碱能抗炎通路来缩短出血时间的方法。胆碱能抗炎通路可通过直接或间接刺激迷走神经来激活。胆碱能抗炎通路还可通过向受试者施用有效量的胆碱能激动剂或乙酰胆碱酯酶抑制剂来激活。