OBJECTIVE: To explore the therapeutic effects and underlying mechanisms of Dendrobium officinale (Tiepi Shihu) extract (DOE) on insomnia. METHODS: Forty-two male Sprague-Dawley rats were randomly divided into 6 groups (n=7 per group): normal control, model control, melatonin (MT, 40 mg/kg), and 3-dose DOE (0.25, 0.50, and 1.00 g/kg) groups. Rats were raised in a strong-light (10,000 LUX) and -noise (>80 db) environment (12 h/d) for 16 weeks to induce insomnia, and from week 10 to week 16, MT and DOE were correspondingly administered to rats. The behavior tests including sodium pentobarbital-induced sleep experiment, sucrose preference test, and autonomous activity test were used to evaluate changes in sleep and emotions of rats. The metabolic-related indicators such as blood pressure, blood viscosity, blood glucose, and uric acid in rats were measured. The pathological changes in the cornu ammonis 1 (CA1) region of rat brain were evaluated using hematoxylin and eosin staining and Nissl staining. Additionally, the sleep-related factors gamma-aminobutyric acid (GABA), glutamate (GA), 5-hydroxytryptamine (5-HT), and interleukin-6 (IL-6) were measured using enzyme linked immunosorbent assay. Finally, we screened potential sleep-improving receptors of DOE using polymerase chain reaction (PCR) array and validated the results with quantitative PCR and immunohistochemistry. RESULTS: DOE significantly improved rats' sleep and mood, increased the sodium pentobarbital-induced sleep time and sucrose preference index, and reduced autonomic activity times (P<0.05 or P<0.01). DOE also had a good effect on metabolic abnormalities, significantly reducing triglyceride, blood glucose, blood pressure, and blood viscosity indicators (P<0.05 or P<0.01). DOE significantly increased the GABA content in hippocampus and reduced the GA/GABA ratio and IL-6 level (P<0.05 or P<0.01). In addition, DOE improved the pathological changes such as the disorder of cell arrangement in the hippocampus and the decrease of Nissel bodies. Seven differential genes were screened by PCR array, and the GABA_A receptors (Gabra5, Gabra6, Gabrq) were selected for verification. The results showed that DOE could up-regulate their expressions (P<0.05 or P<0.01). CONCLUSION DOE demonstrated remarkable potential for improving insomnia, which may be through regulating GABA_A receptors expressions and GA/GABA ratio.
Animals ; Dendrobium/chemistry* ; Rats, Sprague-Dawley ; Male ; Sleep Initiation and Maintenance Disorders/blood* ; Plant Extracts/therapeutic use* ; Receptors, GABA-A/metabolism* ; Noise/adverse effects* ; Light/adverse effects* ; gamma-Aminobutyric Acid/metabolism* ; Sleep/drug effects* ; Rats ; Receptors, GABA/metabolism*

Objective:Aural fullness（AF） is one of the common symptoms in ENT outpatient department, the incidence is about 1.4%. Some patients have an unknown etiology and are diagnosed as idiopathic ear congestion. In this paper, the therapeutic effect of gabapentin on some patients with idiopathic ear congestion was studied. Methods:Forty-eight cases of patients with ear distress as the main complaint between January 2024 and September 2024 were examined by questionnaire, specialist physical examination, pure tone audiometry and acoustic impedance. Among them, 19 cases were diagnosed with definite etiology, 29 cases were diagnosed with idiopathic ear congestion, and 7 cases were lost to follow-up in the idiopathic ear congestion group. Twenty-two patients were divided into the administration group（12 cases receiving regular gabapentin treatment for 3-6 weeks） and the control group（10 cases receiving no medication） based on whether they received gabapentin to explore the effect of ear congestion and possible related factors. Results:Among the 12 patients in the medication group, 2 cases of aural fullness disappeared completely, 9 cases had different degrees of relief, and 1 case had no relief Among the 10 patients in the control group, 2 patients' aural fullness disappeared, 1 patient consciously relieved, and the remaining 7 patients had no significant change in ear boredom. According to the Wong-baker Facial expression Scale, the score of ear tightness decreased from 2.83 before medication to 1.51 after medication in the medication group. The remission rate of ear congestion in the medication group was significantly higher than that in the control group（P=0.004）. Conclusion:Gabapentin can be used to treat idiopathic aural fullness, which can reduce the symptoms effectively. This suggests that the occurrence of idiopathic aural fullness may be related to neuralgia and central sensitization.
Humans ; Gabapentin/therapeutic use* ; Amines/therapeutic use* ; gamma-Aminobutyric Acid/therapeutic use* ; Female ; Male ; Cyclohexanecarboxylic Acids/therapeutic use* ; Ear Diseases/drug therapy* ; Middle Aged ; Adult ; Aged

The visual system plays an important role in our daily life. In this study, we found that loss of dendritic cell factor 1 (DCF1) in the primary visual cortex (V1) caused a sight deficit in mice and induced an abnormal increase in glutamic acid decarboxylase 67, an enzyme that catalyzes the decarboxylation of glutamate to gamma aminobutyric acid and CO, particularly in layer 5. In vivo electrophysiological recordings confirmed a decrease in delta, theta, and beta oscillation power in DCF1-knockout mice. This study presents a previously unknown function of DCF1 in V1, suggests an unknown contact between DCF1 and GABA systems, and provides insight into the mechanism and treatment of visual deficits.
Animals ; Brain Waves ; genetics ; Disease Models, Animal ; Electroencephalography ; Gene Expression Regulation ; drug effects ; genetics ; Geniculate Bodies ; drug effects ; metabolism ; Ginkgolides ; therapeutic use ; Glutamate Decarboxylase ; metabolism ; Lactones ; therapeutic use ; Membrane Proteins ; deficiency ; genetics ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Nerve Tissue Proteins ; deficiency ; genetics ; Photic Stimulation ; Proto-Oncogene Proteins c-fos ; metabolism ; Vision Disorders ; drug therapy ; genetics ; pathology ; physiopathology ; Visual Cortex ; metabolism ; pathology ; gamma-Aminobutyric Acid ; metabolism

BACKGROUND: Although both pregabalin and gabapentin are known to be useful for treating lumbar radiating pain and reducing the incidence of surgery, the oral corticosteroids sometimes offer a dramatic effect on severe radiating pain despite the lack of scientific evidence. METHODS: A total of 54 patients were enrolled among 703 patients who complained of lumbar radiating pain. Twenty patients who received an oral corticosteroid was classified as group A and 20 patients who received the control drugs (pregabalin or gabapentin) as group B. Oswestry Disability Index (ODI), Revised Roland Morris disability questionnaire (RMDQ), Short Form 36 (SF-36) questionnaire, lumbar radiating pain, objective patient satisfaction, and objective improvement of patients or physicians were assessed at 2, 6, and 12 weeks after medication. RESULTS: No difference in the sex ratio and age was observed between the groups (p = 0.70 and p = 0.13, respectively). Group A showed greater improvement in radiating pain after 2, 6, and 12 weeks than group B (p < 0.001, p = 0.001, and p < 0.001, respectively). No differences were observed between the groups in satisfaction at the beginning and 12 weeks after taking the medication (p = 0.062 and p = 0.061, respectively) and in objective improvement of patients and physicians (p = 0.657 and p = 0.748, respectively). Group A was less disabled and had greater physical health scores than group B (p = 0.014 and p = 0.017, respectively). CONCLUSIONS: Oral corticosteroids for the treatment of lumbar radiating pain can be more effective in pain relief than gabapentin or pregabalin. The satisfaction of patients and physicians with the drug and objective improvement status were not inferior to that with gabapentin or pregabalin.
Adolescent ; Adrenal Cortex Hormones/*therapeutic use ; Adult ; Aged ; Amines/therapeutic use ; Analgesics/therapeutic use ; Cyclohexanecarboxylic Acids/therapeutic use ; Female ; Humans ; Low Back Pain/*drug therapy/*physiopathology ; Lumbosacral Region/physiopathology ; Male ; Middle Aged ; Patient Satisfaction/statistics & numerical data ; Pregabalin/therapeutic use ; Quality of Life ; Radiculopathy/drug therapy ; Surveys and Questionnaires ; Young Adult ; gamma-Aminobutyric Acid/therapeutic use

OBJECTIVETo explore the analgesia of oxymatrine (OMT) affecting high voltage-dependent calcium channels (HVDCCs) and GABA release under neuropathic pain condition.

METHODSTotally 66 C57BL/6 mice were randomly divided into the sham-operation group, the model group, and the OMT group, 22 in each group. Neuropathic pain models were established by partial sciatic nerve ligation (PSNL). Hind paw plantar mechanical response threshold (MWT) was measured by up-and-down method with Von-Frey filament. mRNA expression of HVDCCs in brains and spinal cords was detected with Real-time PCR and concentration of GABA was determined using ELISA kit.

RESULTSCompared with day 0, the left hind paw MWTwas decreased on day 7, 10, and 14 in the model group (P < 0.05). Compared with the sham-operation group, the left hind paw MWT was significantly reduced in the model group on day 7 (P < 0.05). The MWT of PSNL ipsilateral hind paw was decreased on day 7 before OMT administration, when compared with day 0 (P < 0.05), and increased after OMT administration (P < 0.05). Compared with the sham-operation group, mRNA levels of Cav1.2, Cav1.3, Cav2.1, and Cav2.3 in brain tissues were increased and those of Cav2.2 were decreased significantly in the model group (P < 0.05). In spinal cord tissues, mRNA levels of Cav1.2 and Cav1.3 were increased, but those of Cav2.1, Cav2.2, and Cav2. 3 were decreased significantly in the model group, when compared with those of the sham-operation group (P < 0.05). Compared with the model group, mRNA levels of Cavl.2, Cavl.3, Cav2.1, and Cav2. 3 in brain tissues were decreased, and those of Cav2.2 were increased significantly in the OMT group (P < 0.05). In spinal cord tissues of the OMT group, mRNA levels of Cav1.3 decreased and those of Cav2.1, Cav2.2, and Cav2.3 increased significantly with statistical difference, when compared with those of the model group (P < 0.05). Compared with the sham-operation group, GABA levels in brain tissues decreased in the model group (P < 0.05). Compared with the model group, GABA levels in brain tissues increased in the OMT group (P < 0.05). There was no statistical difference in GABA levels of spinal cord tissues among these groups (P > 0.05).

CONCLUSIONSOMT had analgesic effect on neuropathic pain, which might be probably related to HVDDCs. Cav2.2 might directly affect GABA release.

Alkaloids ; pharmacology ; therapeutic use ; Analgesia ; methods ; Animals ; Calcium ; Calcium Channels ; drug effects ; metabolism ; Disease Models, Animal ; Mice ; Mice, Inbred C57BL ; Neuralgia ; drug therapy ; Pain Management ; Quinolizines ; pharmacology ; therapeutic use ; Spinal Cord ; metabolism ; gamma-Aminobutyric Acid

OBJECTIVETo study the clinical effects of gabapentin on the treatment of pruritus of scar resulting from deep partial-thickness burn.

METHODSA total of fifty-eight patients suffering from pruritus of scar after deep partial-thickness burn were hospitalized from January 2013 to January 2014. Patients were divided into placebo group (n =18, treated with oral vitamin C in the dose of 100 mg for 4 weeks, twice per day) , cetirizine group (n = 20, treated with oral cetirizine in the dose of 10 mg for 4 weeks, twice per day) , and gabapentin group (n = 20, treated with oral gabapentin in the dose of 300 mg for 4 weeks, twice per day) . Before treatment and on post treatment day (PTD) 3 and 28, the Visual Analog Scale (VAS) was used to assess the itching degree, and the mean scores were recorded. The remission rates of pruritus on PTD 3 and 28 were calculated. The adverse effects were observed during treatment. Data were processed with analysis of variance, q test, and chi-square test.

RESULTSCompared with that before treatment, the itching degree of patients with light, moderate, and severe itching in placebo group was not relieved after treatment; the itching degree of patients with moderate or severe itching in cetirizine group was alleviated after treatment, but not in patients with light itching; itching degree of all patients in gabapentin group was significantly relieved after treatment. There were no obvious differences in VAS scores among the 3 groups before treatment (F = 2.78, P > 0.05). On PTD 3 and 28, the VAS scores of patients in both gabapentin group [(2.3 ± 0.8) and (0.6 ± 0.3) points] and cetirizine group [(4.2 ± 1.7) and (2.8 ± 1.2) points] were lower than those in placebo group [(5.7 ± 2.0) and (5.7 ± 1.9) points, with q values from 6.70 to 7.75, P values below 0.05]. The VAS scores of patients in gabapentin group on PTD 3 and 28 were lower than those in cetirizine group (with q values respectively 6.30 and 6.90, P values below 0.05). The remission rates of pruritus of patients in gabapentin group on PTD 3 and 28 were respectively (66 ± 20)% and (91 ± 17)%, and they were higher than those in cetirizine group [(33 ± 8)% and (56 ± 14)%, with q values respectively 4.70 and 3.82, P values below 0.05]. The remission rate of pruritus of patients in placebo group on PTD 3 and 28 was 0, which was lower than that of the other 2 groups each (with q values from 3.94 to 6.76, P values below 0.05). During the course of treatment, 5 patients in gabapentin group suffered from adverse effects including mild-to-moderate drowsiness and dizziness, but they disappeared one week later. No adverse effects were observed in patients of the other two groups.

CONCLUSIONSFor patients with deep partial-thickness burn, gabapentin can effectively alleviate scar itching after wound healing with safety.

Amines ; administration & dosage ; therapeutic use ; Analgesics ; therapeutic use ; Ascorbic Acid ; administration & dosage ; Burns ; complications ; Cetirizine ; administration & dosage ; Cicatrix ; Cyclohexanecarboxylic Acids ; administration & dosage ; therapeutic use ; Humans ; Pruritus ; drug therapy ; Skin Transplantation ; Treatment Outcome ; Visual Analog Scale ; Wound Healing ; gamma-Aminobutyric Acid ; administration & dosage ; therapeutic use

OBJECTIVETo study the changes in plasma substance P (SP) and calcitonin gene-related peptide (CGRP) levels in children with acute asthma before and after gamma-aminobutyric acid (GABA) treatment.

METHODSSeventy-five children with asthma were randomly assigned to GABA treatment (n=36) and control groups (n=39). Both groups were given conventional treatment for asthma. Besides the conventional treatment, the treatment group was administered with oral GABA (25-30 mg/kg•d). Plasma content of SP and CGRP was measured using ELISA before treatment and after remission.

RESULTSThere were no significant differences in plasma content of SP and CGRP between the GABA treatment and control groups (P＞0.05) before treatment. Plasma content of SP and CGRP in the GABA treatment group was significantly lower than the control group (SP: 57±15 pg/mL vs 127±12 pg/mL; CGRP: 23±10 pg/mL vs 42±8 pg/mL) after remission (P<0.01). Plasma content of SP and CGRP after remission was significantly lower than before treatment (P<0.01) in both groups. There was a significantly positive correlation between plasma SP and CGRP content in asthmatic children (r=0.792, P<0.01).

CONCLUSIONSGABA can significantly decrease plasma levels of SP and CGRP in children suffering from acute asthma.

Asthma ; blood ; drug therapy ; Calcitonin Gene-Related Peptide ; blood ; Child ; Child, Preschool ; Female ; Humans ; Male ; Substance P ; blood ; gamma-Aminobutyric Acid ; pharmacology ; therapeutic use

We examined the possible anti-inflammatory mechanisms of gabapentin in the attenuation of neuropathic pain and the interaction between the anti-allodynic effects of gabapentin and interleukin-10 (IL-10) expression in a rat model of neuropathic pain. The anti-allodynic effect of intrathecal gabapentin was examined over a 7-day period. The anti-allodynic effects of IL-10 was measured, and the effects of anti-IL-10 antibody on the gabapentin were assessed. On day 7, the concentrations of pro-inflammatory cytokines and IL-10 were measured. Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-alpha, 316.0 +/- 69.7 pg/mL vs 88.8 +/- 24.4 pg/mL; IL-1beta, 1,212.9 +/- 104.5 vs 577.4 +/- 97.1 pg/mL; IL-6, 254.0 +/- 64.8 pg/mL vs 125.5 +/- 44.1 pg/mL; IL-10, 532.1 +/- 78.7 pg/mL vs 918.9 +/- 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody. Expression of pro-inflammatory cytokines was significantly attenuated by daily injections of IL-10. The anti-allodynic effects of gabapentin may be caused by upregulation of IL-10 expression in the spinal cord, which leads to inhibition of the expression of pro-inflammatory cytokines in the spinal cords.
Amines/pharmacology/*therapeutic use ; Analgesics/pharmacology/*therapeutic use ; Animals ; Antibodies/immunology/pharmacology ; Behavior, Animal/drug effects ; Cyclohexanecarboxylic Acids/pharmacology/*therapeutic use ; Cytokines/*metabolism ; Disease Models, Animal ; Injections, Spinal ; Interleukin-10/genetics/immunology/*metabolism ; Male ; Neuralgia/*drug therapy/metabolism/pathology ; Rats ; Rats, Sprague-Dawley ; Recombinant Proteins/biosynthesis/genetics/pharmacology ; Spinal Cord/metabolism ; Up-Regulation ; gamma-Aminobutyric Acid/pharmacology/*therapeutic use

PURPOSE: Osteoarthritic pain is largely considered to be inflammatory pain. Sensory nerve fibers innervating the knee have been shown to be significantly damaged in rat models of knee osteoarthritis (OA) in which the subchondral bone junction is destroyed, and this induces neuropathic pain (NP). Pregabalin was developed as a pain killer for NP; however, there are no reports on pregabalin use in OA patients. The purpose of this study was to investigate the efficacy of pregabalin for pain in OA patients. MATERIALS AND METHODS: Eighty-nine knee OA patients were evaluated in this randomized prospective study. Patients were divided into meloxicam, pregabalin, and meloxicam+pregabalin groups. Pain scores were evaluated before and 4 weeks after drug application using a visual analogue scale (VAS), and Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC). Pain scales among groups were compared using a Kruskal-Wallis test. RESULTS: Before drug application, there was no significant difference in VAS and WOMAC scores among the three groups (p>0.05). Significant pain relief was seen in the meloxicam+pregabalin group in VAS at 1, 2, and 4 weeks, and WOMAC score at 4 weeks, compared with the other groups (p<0.05). No significant pain relief was seen in the meloxicam only group in VAS during 4 weeks and WOMAC score at 4 weeks compared with the pregabalin only group (p>0.05). CONCLUSION: Meloxicam+pregabalin was effective for pain in OA patients. This finding suggests that OA pain is a combination of inflammatory and NP.
Aged ; Aged, 80 and over ; Drug Therapy, Combination/adverse effects ; Female ; Humans ; Male ; Middle Aged ; Osteoarthritis, Knee/*drug therapy ; Pain Measurement ; Thiazines/administration & dosage/adverse effects/*therapeutic use ; Thiazoles/administration & dosage/adverse effects/*therapeutic use ; gamma-Aminobutyric Acid/administration & dosage/adverse effects/*analogs & derivatives/therapeutic use

To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.
4-Aminopyridine ; Amides ; chemical synthesis ; chemistry ; therapeutic use ; Animals ; Anticonvulsants ; chemical synthesis ; chemistry ; therapeutic use ; Epilepsy ; chemically induced ; drug therapy ; Female ; Male ; Mice ; Molecular Structure ; Random Allocation ; Structure-Activity Relationship ; gamma-Aminobutyric Acid ; chemistry