Berger V, Alloui A, Kemeny J L, Dubray C, Eschalier A, Lavarenne J
Equipe NPPUA, Laboratoire de Pharmacologie Médicale, Faculté de Médecine, Clermont-Ferrand, France.
Fundam Clin Pharmacol. 1998;12(2):200-4. doi: 10.1111/j.1472-8206.1998.tb00942.x.
Numerous neurotransmitters are involved in nociceptive transmission or regulation. Several reports have shown the analgesic effects of somatostatin and its analogues. Somatostatin, when given intrathecally, markedly reduced pain in cancer patients. Somatostatin analogues that possess a longer half-life time are more convenient for therapeutic use. Vapreotide, a somatostatin analogue, was shown to induce a long-lasting antinociceptive effect in rats. We studied the site and the mechanism of action of vapreotide in rats using the paw pressure test. Intrathecal administration of vapreotide induced no antinociception. Systemically administered vapreotide-induced antinociception was inhibited by several intrathecal (i.t.) administered antagonists (yohimbine, naloxone and to a lesser degree tropisetron). These results show a lack of spinal effect and suggest a supraspinal site of action with an involvement of noradrenergic and to a lesser degree serotonergic bulbospinal pathways. In addition, spinal opioid receptors also seen to be involved.
许多神经递质都参与伤害性感受的传递或调节。有几份报告显示了生长抑素及其类似物的镇痛作用。鞘内注射生长抑素可显著减轻癌症患者的疼痛。半衰期较长的生长抑素类似物在治疗应用上更为方便。生长抑素类似物伐普肽在大鼠中显示出持久的抗伤害感受作用。我们使用 paw 压力试验研究了伐普肽在大鼠中的作用部位和作用机制。鞘内注射伐普肽未诱导出抗伤害感受作用。全身给药的伐普肽诱导的抗伤害感受作用被几种鞘内注射的拮抗剂（育亨宾、纳洛酮以及程度较轻的托烷司琼）所抑制。这些结果表明缺乏脊髓效应，并提示作用部位在脊髓以上，涉及去甲肾上腺素能以及程度较轻的血清素能延髓脊髓通路。此外，脊髓阿片受体似乎也参与其中。
