ABSTRACT
Aim To explore the effect of activated SK channels(small conductance Ca2+-activated K+ channels) on morphine-induced hyperalgesia in the spinal cord in mice.Methods Adult C57BL6/N male mice were chosen to establish the model of morphine-hyperalgesia.The changes of tail withdrawal latency(TWL), mechanical withdrawal threshold(MWT) and the threshold of visceral pain were observed after intrathecal 1-EBIO, the agonist of SK channels.Results Compared with the control group, TWL, MWT and the threshold of visceral pain were decreased after morphine injection.After intrathecal 1-EBIO, the TWL, MWT and visceral pain threshold were increased.The level of spinal membrane SK2 expression in morphine-treated mice was decreased compared with that of control group.After intrathecal 1-EBIO, the level of spinal membrane SK2 expression was increased.Conclusion SK channels in the spinal cord are involved in morphine-induced hyperalgesia in mice.
ABSTRACT
Objective To establish a simple and sensitive method for the determination of plasma drug concentration in rats after intragastrical and intravenous administration of paclitaxel loaded nanoparticles and to evaluate its pharmacokinetic characteristics .Methods AgilentTC-C18 column (250 mm × 4 .6 mm ,5 μm) was used for HPLC at the flow rate 1 ml/min with ketoconazole as internal standard and methanol acetonitrile water (45:20:35) as the mobile phase .The statistical mo-ment method was applied to calculate the pharmacokinetic parameters and to evaluate pharmacokinetic characteristics .Results There was a good liner relationship (r=0 .9997) when rat blood concentration of Paclitaxel ranged from 0 .5 to 20μg /ml .The accuracy and precision were in line with the requirements of biological sample analysis .The t1/2 were 3.86 ,3.76 ,3.35 and 2 .62 h after intravenous injection of three lab-made paclitaxel nanoparticles and paclitaxel solution via rat tail vein .The t1/2 were 5 .28 and 3 .72 h respectively after intragastrical administration of lab-made paclitaxel nanoparticles and paclitaxel suspen-sion .Conclusion This method can be used for the pharmacokinetic study of paclitaxel nanoparticles in rats .The paclitaxel loaded nanoparticles exhibited significantly longer in vivo retention time than paclitaxel injection and paclitaxel suspension .
ABSTRACT
Aim To investigate the effects and signifi-cance of 5-HT2A receptor antagonist MDL1 1 939 on a-mice.Methods Kunming male mice were suffered a-cute acetic acid visceral pain,acute incision pain and CCI neuropathic pain.After each animal model was es-tablished,MDL1 1 939 was injected intraperitoneally. The writhing reaction was used to assess acute acetic acid visceral pain,while the thermal withdrawal laten-cy (TWL)was used to evaluate the acute incision pain and CCI neuropathic pain.Results Compared with the control group,MDL1 1 939 (0.25,0.5,1 .0 mg· kg -1 ,i.p.)relieved acetic acid visceral pain signifi-cantly in a dose-dependent manner in mice,as re-vealed by the significant reduction of the number of twisting.In acute incision pain and CCI neuropathic pain,MDL1 1 939 (0.5 mg·kg -1 ,i.p.)significantly increased TWL level.Conclusion 5-HT2A receptor antagonist MDL1 1 939 has analgesic effects on visceral pain,acute pain and neuropathic pain,which might be a novel therapeutic target to treat different pain in clini-cal situations.
ABSTRACT
Objective Todiscusstheangiographicfeaturesofhepaticneuroendocrineneoplasm(NEN),and to analyze the survival time of patients.Methods The clinical data of 60 patients with hepatic NEN were retrospectively reviewed.Transcatheter arterial chemoembolization (TACE),used as main therapy,was employed in 17 patients,22 patients received palliative treatment with no use of TACE,and 21 didn't receive any related treatment.The angiographic features of hepatic NEN were analyzed.Kaplan-Meier method was used to calculate the survival rate,and the survival prognostic factors were evaluated by Cox multivariate analysis method.Results Angiography showed that most neuroendocrine tumors (NETs) were characterized by hypovascular lesion,while neuroendocrine carcinomas (NECs) were manifested as hypervascular mass.The median overall survival time of 60 patients was 13.8 months.The 6-month,one-,2-and 3-year cumulative survival rates were 85.0％,52.0％,40.0％ and 33.8％,respectively.Cox regression analysis indicated that pathological grade of tumor (P=0.001) and treatment mode (P＜0.001) were the independent prognostic factors.Conclusion The rich or poor vascularity of hepatic NEN is helpful for the judgment of tumor grading.Patients whose hepatic NENs belong to high pathological grade (grade Ⅲ) usually have a poor prognosis.TACE is an effective therapy for hepatic NEN.
ABSTRACT
Aim To explore the effect of pharmacolog-ical activation of serotonin 5-HT2C receptor (5-HT2C R) on naloxone-precipitated withdrawal in morphine-de-pendent mice. Method EthoVision Noldus video tracking system was used to record the effect of 5-HT2C R agonist WAY on locomotor activities and behavioral performances in mice.Results Selective 5-HT2C R ag-onist WAY (0.5,0.75 or 1 .0 mg·kg -1 ,i.p.)a-lone did not alter the locomotor activities as determined by distance traveled and velocity (all P values >0.05).Chronic morphine treatment induced depend-ence in mice as demonstrated by increases in distance traveled,velocity and jumping behavior.WAY (0.5, 0.75 or 1 .0 mg·kg -1 ,i.p.)and clonidine (0.2 mg ·kg -1 ,i.p.)significantly ameliorated naloxone-pre-cipitated withdrawal symptoms,including burrowing, jumping,body grooming,rearing,“wet dog”shakes, head shakes,face grooming,penile grooming,scratch (all P values <0.05).Conclusion Pharmacological activation of 5-HT2C R ameliorates naloxone-precipitated withdrawal symptoms in morphine-dependent mice.5-HT2C R may be a novel target to develop therapeutic ap-proach against morphine physical dependence,craving and relapsing.
ABSTRACT
Aim To examine subcellular localization of serotonin 5-HT2A receptor (5-HT2AR) and glutamate NMDA receptor in dorsal hippocampal CA1 area ( dCA1 ) and further explore the effect of systemic acti-vation of 5-HT2A R on hippocampal neuronal firing rate. Methods The distribution of 5-HT2A R and NMDA re-ceptor in the dCA1 region was detected with immune e-lectron microscopy after embedding. The effect of acti-vation of 5-HT2A R on the principal neuron and inter-neuron firing rates was examined with multichannel re-cording. Results 5-HT2A R immunoreactivity was ob-served in the dCA1 neurons, including rough endoplas-mic reticula and mitochondria, and the 5-HT2A R and glutamate NMDA receptors were colocalized in the syn-aptic membrane, vesicle and neurofilament of the hipp-ocampal neuron. 5-HT2A R activation increased princi-pal neuronal firing rate and the interneuronal firing rate was not changed. Conclusion The 5-HT2A R and NM-DA receptor are colocalized in dCA1 neurons, and acti-vation of 5-HT2A R increases hippocampal principal neuronal firing rate.
ABSTRACT
Objective To investigate the effects of bisphenol A(BPA)exposure to perinatal on learning and memory behaviour in F1 generation male rats.Methods From the 11th day of gestation to the 7th day of field test was used to detect the locomotion activity,the Morris water maze was employed to measure learning and memory ability and long-term potentiation(LTP)were recorded to detect the synaptic plasticity in hippocampus CA1 with extracellular recording.Results The crossing number of BPA group(70.35±13.56)was much more than control group((29.32±14.12),P＜0.05).The number of standing up and ornament of BPA group((38.52±6.52),(6.26±2.78))were both higher than control group((10.35±8.38),(2.67±1.46),P＜0.05).BPA rats had longer escape latencies to find platform((55.22±5.78)s)than control rats((21.22±2.65)s,P＜0.05).Conditional protocol with high-frequency stimulation evoked a stable LTP in hippocampus CA1 region in control rats((162.13±10.12)%),however the LTP could not be induced with the same conditional protocol in BPA-exposed rats((101.05±7.58)%,P＜0.05).Conclusion Perinatal BPA exposure impaires learning and memory ability in F1 generation male rats related to presynaptic dysfunction.
ABSTRACT
AIM To study the effect of bioactive compounds from entomogenous fungi (BCEF0083) on sleep-wakefulness cycle and behaviour in chronic unpredictable stress model of depression in rats. METHODS The effect of BCEF0083 on sleep-wakefulness cycle and behaviour was examined in the chronic unpredictable stress model of depression in rats. Stereotaxic and polysomnography were used to record the sleep-wakefulness cycle. The behaviour of rats was tested in the open field. RESULTS BCEF0083 increased ambulation and rearing score of chronic unpredictable stressed rats in the open field. BCEF0083 attenuated REMS percent and latency in chronic stressed rats obviously. CONCLUSION BCEF0083 can ameliate sleep-wakefulness cycle and behaviour in chronic unpredictable stress model of depression in rats.
ABSTRACT
AIM To study the role of serot on in (5-HT) in ventrolateral preoptic nucleus(VLPO) on sleep and wakefulness cycl e of rat by microinjection of 5-hydroxytryptaphan (5-HTP , precursor of 5-HT ) , non-special 5-HT receptor antagonist methysergide (MS) and 5-HT retake i nhibitor fluoxetine. METHODS Stereotaxic, microinjection and po lysomnography (PSG) were used in the experiment. RESULTS There was no significant effect by microinjection of 5-HTP(0 5 ?g,0 1 ?l) into VLPO,but microinjection of 5-HTP(1 ?g,0 1 ?l)and fluoxetine lead wake i ncreased and sleep decreased; while microinjection of non-selective serotonin receptor antagonist MS lead to the opposited effect. The chang of sleep-wakefu lness cycle caused by 5-HTP or MS were significantly assiociated with time. CONCLUSION 5-HT involved in the regulation of sleep-wake cycle a nd promoted wake in the VLPO and its role of promotion may involve the gene exp ression of post-synaptic neurons.
ABSTRACT
The frequencies of HLA-DR and DQ were investigated in Shanghai Crowd of Han Nationality with the whole typing serum of the first in- ternational red cross HLA workshop. The frequencies of HLA-DR split and HLA-DQ split were first described in Chinese. The result. the gene frequencies of HLA-DR. DR1 0.0054, DR4 0.0906, DR7 0.0847, DRw8 0.0499, DR9 0.1553, DRw10 0.0109,DRw11 0.0847,DRw12 0.1086,DRw13 0.0906,DRw14 0.0219,DRw15 0.1332,DRw16 0. 0191,DRw17 0.0556, DR blank 0.0895, the gene frequencies of HLA-D: DQw2 0.1426, DQw4 0.0527, DQw5 0.0642,DQw6 0.2393, DQw7 0.2324, DQw8 0.0219, DQw9 0.1521, DQ blank 0.0946.
ABSTRACT
AIM To investigate the role of serotonergic projection from dorsal raphe nuclei (DRN) to basolateral amygadaloid (BLA) in the regulation of sleep and waking state. METHODS stereotaxic microinjection and polysomnography were employed. RESULTS Microinjection of L Glu into the DRN caused an enhancement of wake (W) and a decrease of slow wave sleep (SWS) and paradoxical sleep (PS). However, microinjection of L Glu into the DRN plus bilateral microinjection of methysergide (MS) into the BLA reversed the effects of L Glu. Microinjection of PCPA into the DRN caused an enhancement of SWS and a decrease of W. Microinjection of PCPA into the DRN plus bilateral microinjection of 5 HTP into the BLA reversed the effects of PCPA. CONCLUSION These results suggest that the role of the DRN in the regulation of sleep and waking state is partly mediated by serotonergic projection from the DRN to the BLA.