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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Contribution of peripheral vanilloid receptor to the nociception induced by injection of spermine in mice.
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Contribution of peripheral vanilloid receptor to the nociception induced by injection of spermine in mice.

机译：外周香草受体对小鼠注射精胺诱导的伤害感受的贡献。

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摘要

Polyamines (putrescine, spermidine and spermine) are important endogenous regulators of ion channels, such as vanilloid (TRPV1), glutamatergic (NMDA or AMPA/kainate) and acid-sensitive (ASIC) receptors. In the present study, we have investigated the possible nociceptive effect induced by polyamines and the mechanisms involved in this nociception in vivo. The subcutaneous (s.c.) injection of capsaicin (as positive control), spermine, spermidine or putrescine produced nociception with ED(50) of 0.16 (0.07-0.39)nmol/paw, 0.4 (0.2-0.7) mumol/paw, 0.3 (0.1-0.9) mumol/paw and 3.2 (0.9-11.5) mumol/paw, respectively. The antagonists of NMDA (MK801, 1 nmol/paw), AMPA/kainate (DNQX, 1 nmol/paw) or ASIC receptors (amiloride, 100 nmol/paw) failed to reduce the spermine-trigged nociception. However, the TRPV1 antagonists capsazepine or SB366791 (1 nmol/paw) reduced spermine-induced nociception, with inhibition of 81 +/- 10 and 68 +/- 9%, respectively. The previous desensitization with resiniferatoxin (RTX) largely reduced the spermine-induced nociception and TRPV1 expression in the sciatic nerve, with reductions of 82 +/- 9% and 67 +/- 11%, respectively. Furthermore, the combination of spermine (100 nmol/paw) and RTX (0.005 fmol/paw), in doses which alone were not capable of inducing nociception, produced nociceptive behaviors. Moreover, different concentrations of spermine (3-300 muM) enhanced the specific binding of [(3)H]-RTX to TRPV1 receptor. Altogether, polyamines produce spontaneous nociceptive effect through the stimulation of TRPV1, but not of ionotropic glutamate or ASIC receptors.
机译：多胺（腐胺，亚精胺和亚精胺）是离子通道的重要内源性调节剂，例如香草酸（TRPV1），谷氨酸能（NMDA或AMPA /海藻酸酯）和酸敏感（ASIC）受体。在本研究中，我们研究了由多胺引起的可能的伤害作用以及体内这种伤害感受的机制。皮下注射皮下注射辣椒素（作为阳性对照），精胺，亚精胺或腐胺产生伤害感受，ED（50）为0.16（0.07-0.39）nmol / paw，0.4（0.2-0.7）mumol / paw，0.3（0.1 -0.9）摩尔/爪和3.2（0.9-11.5）摩尔/爪。 NMDA（MK801，1 nmol / paw），AMPA /海藻酸酯（DNQX，1 nmol / paw）或ASIC受体（阿米洛利，100 nmol / paw）的拮抗剂未能减少精胺触发的伤害感受。但是，TRPV1拮抗剂卡塞平或SB366791（1 nmol /爪）可减少精胺诱导的伤害感受，抑制率分别为81 +/- 10和68 +/- 9％。先前用树脂毒素（RTX）脱敏大大降低了精胺诱导的坐骨神经痛和TRPV1表达，分别降低了82 +/- 9％和67 +/- 11％。此外，精胺（100nmol /爪）和RTX（0.005fmol /爪）的组合，单独不能诱导伤害感受的剂量产生伤害感受行为。此外，不同浓度的精胺（3-300μM）增强[（3）H] -RTX与TRPV1受体的特异性结合。总而言之，多胺通过刺激TRPV1产生自发的伤害作用，而对离子型谷氨酸或ASIC受体则没有。

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