Department of Pharmacology, University of Minnesota Medical School, Minneapolis, Minnesota 55455, United States.
Department of Veterinary Population Medicine, University of Minnesota Veterinary School, Minneapolis, Minnesota 55455, United States.
J Med Chem. 2020 Dec 10;63(23):14647-14667. doi: 10.1021/acs.jmedchem.0c01042. Epub 2020 Nov 20.
The incidence of fatal overdoses has increased worldwide due to the widespread access to illicit fentanyl and its potent analogues. Vaccines offer a promising strategy to reduce the prevalence of opioid use disorders (OUDs) and to prevent toxicity from accidental and deliberate exposure to fentanyl and its derivatives. This study describes the development and characterization of vaccine formulations consisting of novel fentanyl-based haptens conjugated to carrier proteins. Vaccine efficacy was tested against opioid-induced behavior and toxicity in mice and rats challenged with fentanyl and its analogues. Prophylactic vaccination reduced fentanyl- and sufentanil-induced antinociception, respiratory depression, and bradycardia in mice and rats. Therapeutic vaccination also reduced fentanyl intravenous self-administration in rats. Because of their selectivity, vaccines did not interfere with the pharmacological effects of commonly used anesthetics nor with methadone, naloxone, oxycodone, or heroin. These preclinical data support the translation of vaccines as a viable strategy to counteract fentanyl use disorders and toxicity.
由于非法芬太尼及其强效类似物的广泛获取,全球致命过量用药的发生率有所增加。疫苗为减少阿片类使用障碍(OUD)的流行和预防因意外和故意接触芬太尼及其衍生物而产生的毒性提供了一种有前途的策略。本研究描述了由新型基于芬太尼的半抗原与载体蛋白缀合而成的疫苗制剂的开发和表征。在接受芬太尼及其类似物挑战的小鼠和大鼠中,测试了疫苗的功效,以对抗阿片类药物引起的行为和毒性。预防性疫苗接种可减轻小鼠和大鼠中芬太尼和舒芬太尼引起的镇痛、呼吸抑制和心动过缓。治疗性疫苗接种也减少了大鼠中芬太尼的静脉自我给药。由于其选择性,疫苗不会干扰常用麻醉剂的药理学作用,也不会干扰美沙酮、纳洛酮、羟考酮或海洛因的作用。这些临床前数据支持将疫苗作为一种可行的策略来对抗芬太尼使用障碍和毒性。
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