Srikiatkhachorn A, Anthony M
Institute of Neurological Sciences, Prince Henry and Prince of Wales Hospitals and School of Medicine, University of New South Wales, Sydney, Australia.
Cephalalgia. 1996 Oct;16(6):419-22. doi: 10.1046/j.1468-2982.1996.1606419.x.
Analgesic abuse has recently been recognized as a cause of deterioration in primary headache patients. Although the pathogenesis of this headache transformation is still obscure, alteration of serotonin receptor function is one possible mechanism. To assess the plasticity of 5HT2 serotonin receptors in this condition, we investigated receptor binding by the platelet membrane in patients with analgesic-induced headache (AIH), migraine and non-headache controls. The technique involved radioligand binding with (phenyl-4-3H)spiperone and ketanserin. A greater density of receptor numbers (Bmax) was found in patients with AIH and in non-headache controls (96.47 +/- 10.21 and 92.01 +/- 13.15 fmol/mg protein), as compared to migraine patients (49.52 +/- 5.14 fmol/mg protein). The value of dissociation equilibrium constant (KD) remained unchanged (3.07 +/- 0.49, 2.24 +/- 0.24 and 2.91 +/- 0.42 nM for patients with AIH, migraine and non-headache controls, respectively). Based on these findings, we suggest that up-regulation of 5HT2 serotonin receptors may be a possible mechanism of headache transformation in patients with AIH.
镇痛药滥用最近被认为是原发性头痛患者病情恶化的一个原因。尽管这种头痛转变的发病机制仍不清楚，但血清素受体功能改变是一种可能的机制。为了评估这种情况下5HT2血清素受体的可塑性，我们研究了镇痛药诱发头痛（AIH）患者、偏头痛患者和非头痛对照者血小板膜上的受体结合情况。该技术涉及用（苯基-4-3H）螺哌隆和酮色林进行放射性配体结合。与偏头痛患者（49.52±5.14 fmol/mg蛋白质）相比，AIH患者和非头痛对照者（分别为96.47±10.21和92.01±13.15 fmol/mg蛋白质）的受体数量（Bmax）密度更高。解离平衡常数（KD）的值保持不变（AIH患者、偏头痛患者和非头痛对照者分别为3.07±0.49、2.24±0.24和2.91±0.42 nM）。基于这些发现，我们认为5HT2血清素受体上调可能是AIH患者头痛转变的一种可能机制。
