Effect of Thymol on the spontaneous contractile activity of the smooth muscles

Effects of Thymol on the spontaneous contractile activity (SCA) have been found in in vitro experiments with circular smooth-muscle strips (SMAs) from guinea pig stomach and vena portae. Thymol was found to possess an agonistic effect on the alpha(1)-, alpha(2)- and beta-adrenergic receptors. Its spasmolytic effect is registered at doses higher than 10(-6)M. Thymol in a dose of 10(-4)M inhibits 100% the SCA of the SMAs and reduces the excitatory effect of 10(-5)M ACH to 35%. It is assumed that Thymol has an analgesic effect through its action on the alpha(2)-adrenergic receptors of the nerve cells. By influencing the beta-adrenergic receptors in the adipose cells, it is possible to induce increased synthesis of fatty acids and glycerol, which is a prerequisite for increased heat release.     

Spatial summation of perceived pressure,sharpness and mechanically evoked cutaneous pain

Psychophysically, spatial summation can be demonstrated as a decrease in threshold accompanying an increased field of stimulation. The present study examined to what extent different mechanically evoked percepts (pressure, sharpness, and pain) show spatial summation. Various probes were used to apply prescribed forces to the dorsal surface of the digits of 19 healthy subjects. The threshold for three perceptual qualities showed differing degrees of spatial summation: sharpness showed no statistically significant spatial summation; pain demonstrated some significant summation (46% on average); pressure showed the greatest degree of spatial summation (76% on average). The lack of significant spatial summation for sharpness threshold is consistent with the theory that perceived sharpness can be evoked by near threshold activity of a single nociceptor. The modest amount of spatial summation for pain implies that distinctly suprathreshold activation of nociceptors is required for mechanically evoked pain perception, and such input summates centrally, but not completely. The greater spatial summation observed for pressure vs. pain thresholds implies a greater degree of central summation for slowly adapting mechanoreceptors vs. nociceptors.     

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.     

Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors

Replacement of the piperidine ring in the lead benzenesulfonamide Na_v1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Na_v1.7 inhibitory activity, but the activity was restored by shortening the linkage from methyleneoxy to oxygen. These efforts led to a series of morpholine-based aryl sulfonamides as isoform-selective Na_v1.7 inhibitors. This report describes the synthesis and SAR of these analogs.     

强电针穴位对背角神经元镇痛效应广泛性的中枢机制

实验用雄性大鼠,玻璃微电极细胞外记录Ｔ１２－Ｌ１脊髓背角会聚神经元对后爪伤害性刺激的反应,观察到低强度（２Ｖ）电针作用于与痛源接近的“足三里”穴对背角神经元的伤害性反应有明显的抑制作用,而远隔穴位“下关”穴则无效。而当采用超过Ｃ类纤维阈值１８Ｖ电针时,则远隔穴位“下关”也有明显的镇痛作用。表现为强电针穴位镇痛作用的广泛性。而损毁ＮＲＭ后,强电针（１８Ｖ）远节段“下关”穴的镇痛作用消失,而近节段“足     

脊髓背角痛觉传递和调制的一些化学解剖学观察

本实验研究了脊髓背角内Ｃ纤维末梢的分布和突触学特征及其一些神经递质化学构筑;定量观察了急性痛引起背角的递质变化;显示了初级传入Ｃ纤维,抑制性中间神经元和背角伤害性感受神经元三者之间的突触关系,并探讨它们在痛觉信息传递和调制中的作用。     

MIS-TLIF结合钉棒系统治疗极外侧型腰椎间盘突出症的临床研究

目的:观察和比较使用通道下经椎间孔腰椎融合术(Minimally Invasive Transforaminal Lumbar Interbody Fusion;MIS-TLIF)与常规开放手术治疗极外侧型腰椎间盘突出症的临床疗效。方法:回顾性分析2012.01至2016.01经纳入及排除标准筛选后的共计61例腰椎间盘突出症患者。根据不同的手术方法,将上述患者分别纳入实验组(MIS-TLIF组)与对照组(常规开放手术组)。对患者手术前后的疼痛程度(VAS),功能障碍程度(JOA)及各围手术期指标(出血量,手术时间,透视次数,卧床时间,花费,并发症)进行统计学比较。结果:MIS-TLIF组与对照组患者在术前的VAS评分及JOA评分的比较中无显著性差异,经外科手术后,都有显著性改善(P0.05)且两组间无显著统计学差异(P0.05)。但MIS-TLIF组在出血量,卧床时间,并发症等指标中都显著优于对照组(P0.05)。结论:通道下经椎间孔腰椎融合术作为一种微创术式,能够显著改善极外侧型腰椎间盘突出症患者的临床症状,并具有其独有的优势和长处,在临床工作中可以进行进一步的使用和推广。     

体液因素在一足致炎大鼠非致炎足伤害感受性变化中的作用

一足致炎大鼠对侧非致炎足的痛阈出现显著降低、不变和显著升高三种变化;分别结扎致炎与非致炎侧大隐静脉后,这三种变化均有所降低。结果提示,致炎足产生的体液因素参与健侧足出现的镇痛过程。     

Influence of centrally administered peptides on ear withdrawal from heat in the rabbit

Certain neuropeptides previously linked to stress and implicated in CNS control of analgesia/algesia were tested using a recently developed analgesiometric model, the rabbit ear-withdrawal test. The latency to ear withdrawal increased in a dose-related manner after β-endorphin was injected intracerebroventricularly (IVC). Intermediate doses (0.5 and 1.0 μg) of adrenocorticotropic hormone (ACTH) caused hyperalgesia as indicated by decreases in latency. Corticotropin-releasing factor (CRF, 0.5 and 1.0 μg) also caused significant hyperalgesia late in the testing period. -Melanocyte stimulating hormone (-MSH, 0.25–2.0 μg), a molecule that shares the first 13 amino acid sequence with ACTH, and somatostatin (0.25–2.0 μg), caused no significant change in latency. However, 1.0 μg doses of each peptide antagonized the analgesic effect of β-endorphin (1.0 μg) in the following order of potency: ACTH = -MSH > CRF > somatostatin. The results support the idea that CNS peptides that are released during stress can exert opposing actions on acute pain, even though they may cause little effect alone.