Coruzzi Gabriella, Adami Maristella, Guaita Elena, de Esch Iwan J P, Leurs Rob
Department of Human Anatomy, Pharmacology and Forensic Medicine, Section of Pharmacology, University of Parma, via Volturno 39, 43100 Parma, Italy.
Eur J Pharmacol. 2007 Jun 1;563(1-3):240-4. doi: 10.1016/j.ejphar.2007.02.026. Epub 2007 Feb 23.
The effects of the highly selective histamine H4 receptor antagonists JNJ7777120 and VUF6002 were investigated on the carrageenan-induced inflammation and thermal hyperalgesia in rats. JNJ7777120 (10 and 30 mg/kg, s.c.) and VUF6002 (10 mg/kg, s.c.) significantly reduced paw edema and hyperalgesia provoked by subplantar injection of carrageenan; the effect was evident against the early (2 h) phase of inflammation. An inactive analog of VUF6002, VUF6007 (10 mg/kg, s.c.) slightly aggravated paw edema, while leaving unaltered carrageenan-induced nociception. These findings indicate that histamine H4 receptors participate in the early phase of acute inflammation induced by carrageenan in rats, influencing both edema and thermal hyperalgesia.
研究了高选择性组胺H4受体拮抗剂JNJ7777120和VUF6002对大鼠角叉菜胶诱导的炎症和热痛觉过敏的影响。JNJ7777120(10和30毫克/千克,皮下注射)和VUF6002(10毫克/千克,皮下注射)显著减轻了足底注射角叉菜胶引起的爪部水肿和痛觉过敏;该作用在炎症早期(2小时)阶段明显。VUF6002的无活性类似物VUF6007(10毫克/千克,皮下注射)轻微加重了爪部水肿,而对角叉菜胶诱导的伤害感受没有影响。这些发现表明,组胺H4受体参与了大鼠角叉菜胶诱导的急性炎症的早期阶段,影响水肿和热痛觉过敏。