Palmitic acid analogues exhibiting antinociceptive activity in mice.

Myrna Déciga-Campos, Rosa Mariana Montiel-Ruiz, Gabriel Navarrete-Vázquez, Francisco Javier López-Muñoz
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Abstract

Three palmitic acid derivatives were synthesized and evaluated as a potential platform for antinociceptive drug development. Female Swiss Webster mice were given N-(4-Methoxy-2-nitrophenyl)hexadecanamide (1), 2-amino-3-(palmitoylamino)benzoic acid (2) or 4-amino-3-(palmi-toylamino)benzoic acid (3) orally in doses of 10-100 mg/kg. The animals were tested for nociception using the hot plate and abdominal constriction response (writhing) tests. Compound 1 generated a dose-dependent antinociceptive effect, reflected by longer latencies (paw-lick and escape responses) and a decrease in writhing. Morphine (1.5-6 mg/kg, p.o.) and diclofenac (10-100 mg/kg, p.o.) were used as positive controls, respectively. Compounds 2 and 3 were less active in both nociceptive tests. The antinociception provoked by compound 1 was partially blocked by naloxone (1 mg/kg, i.p.) suggesting that this pharmacological effect could be due to the activation of micro-opioid receptors. N-(4-Methoxy-2-nitrophenyl)hexadecanamide showed antinociceptive effects in both nociceptive tests suggesting the possibility that this compound may define a new type of antinociceptive.

棕榈酸类似物在小鼠中表现出抗伤害性活性。
合成了三种棕榈酸衍生物,并对其作为抗痛感药物开发的潜在平台进行了评价。雌性瑞士韦氏小鼠口服N-(4-甲氧基-2-硝基苯基)十六烷酰胺(1)、2-氨基-3-(棕榈酰氨基)苯甲酸(2)或4-氨基-3-(棕榈酰氨基)苯甲酸(3),剂量为10-100 mg/kg。使用热板和腹部收缩反应(扭动)测试动物的伤害感受。化合物1产生了剂量依赖性的抗感觉作用,反映在更长的潜伏期(舔爪和逃跑反应)和扭动减少。分别以吗啡(1.5 ~ 6 mg/kg, p.o.)和双氯芬酸(10 ~ 100 mg/kg, p.o.)作为阳性对照。化合物2和3在两种伤害性测试中活性较低。化合物1的抗痛觉作用被纳洛酮(1mg /kg,口服)部分阻断,提示这种药理作用可能是由于微阿片受体的激活。N-(4-甲氧基-2-硝基苯基)十六烷酰胺在两项伤害性测试中均显示出抗伤害性作用,表明该化合物可能定义一种新型的抗伤害性感受剂。
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