In this paper, duloxetine was chosen as the lead compound. The pharmacophores with 5-HT(1A) antagonism activity were used to replace the naphthyl of duloxetine. A series of duloxetine derivatives had been designed and synthesized and whose structures were confirmed with elemental analysis, MS and H NMR. All synthesized compounds were tested by tail suspension test and forced swimming test in vivo. The test results revealed that most of the compounds have shown better activity than duloxetine at the same dosage. Some of them are worth to be studied further.

Objective To explore the localization of epileptogenic focus and select the appropriate surgical procedures for post-traumatic epilepsy. Methods The clinical data of 21 patients with post-traumatic epilepsy were studied retrospectively. Epileptogenic focus was located by comprehensively analyzing data of electro-neurophysiology, neurological imaging and clinical manifestation. Surgical procedures were performed in all patients, including resection of lesion and peripheral cortex in 12 patients, epileptogenie focus resection plus low power bipolar coagulation in five, anterior temporal iobectomy plus amygdalohippocampectomy in three and corpus callosotomy in one. Results All patients were followed up from 6 months to 3 years, which showed satisfactory outcome in eight patients, marked improvement in six, improvement in five and slight improvement in two. The total effective rate was 90%. Conclusions Surgical procedure is important for intractable post-traumatic epilepsy. The good efficacy depends on precise localization of epileptogenic focus and combined application of various surgical procedures.

Objective To analyze the characteristics of dynamic contrast enhanced MR imaging (DCE-MRI)in prostate cancer (PCa)at 3.0T,and to evaluate the diagnostic value of DCE-MRI.Methods 85 patients with suepected PCa received conventional MRI and DCE-MRI.The signal intense-time (SI-T)curve was analyzed.Then the time to maximum (Tmax),the maximum degree of enhancement (STmax%),and the rate of enhancement (Rmax)were calculated.The differences of styles of SI-T curve and the parameters between the positive and negative group were compared respectively.Results 59 cases of PCa were proved by biopsy,and there was no evidence of tumor in 26 cases.507 zones had histopathological results with 250 zones in positive group and 257 zones in negative group .The most common style of SI-T curve in positive group was rapidly ascending followed with descending curve,the most common style of SI-T curve in negative group was persistent ascending curve and plateau curve.The mean values of Tmax,SImax%,Rmax were (69.49±22.53)s,1.74±0.43,7.83±3.80 in positive group respectively,while (175.61±52.64)s,1.05±0.35,1.86±1.10 in negative group respectively,there were statistically significant differences between the two groups(t =-24.24,1 6.34,1 7.75,P <0.01)respectively. The mean values of Tmax,SImax% ,Rmax were (8 9 .1 9 ± 3 1 .7 2 )s,1 .5 8 ± 0 .4 6 ,5 .2 1 ± 3 .3 4 in the low-risk group (Gleason score 2 - 6 )respectively,while (64.25±14.68)s,1.76±0.43,8.25±3.70 in the high-risk group (Gleason score 7-10)respectively, there were statistically significant differences between them(t = 7.09,-8.74,- 7.83,P <0.01).Conclusion 3.0T DCE-MRI has great value in the diagnosis of PCa.

Objective To evaluate the clinical benefits and safety of endoscopic thyroidectomy via bilat -eral-nipple approach and breast approach by comparison with conventional open thyroidectomy .Methods 59 pa-tients undergoing open thyroidectomy , 76 patients undergoing endoscopic thyroidectomy via breast approach , and 122 patients undergoing endoscopic thyroidectomy via bilateral-nipple approach were retrospectively analyzed . Patients'age, operation duration, intraoperative blood loss, the first day drainage volume after operation , postop-erative hospital stay , the incidence of complications , pain visual analogue score ( VAS) , postoperative satisfaction rate as well as the evaluation of cosmetic results were compared among different groups .Results No significant difference was observed in the intraoperative blood loss and the postoperative hospital stay among different groups . The operation duration and the first day drainage volume after operation in the endoscopic thyroidectomy groups ((103.5 ±26.2)min vs (108.1 ±23.9)min,(106.5 ±31.0)ml vs (117.4 ±38.8)ml)were significantly high-er than those in the open thyroidectomy group((65.3 ±22.4)min and (50.5 ±23.8)ml)(P<0.05, respective-ly).No significant difference was observed in the complication incidence among different groups .On the first day after operation, VAS of the endoscopic thyroidectomy groups (2.8 ±0.4 vs 2.9 ±0.4)was significantly lower than that of the open thyroidectomy group(3.8 ±0.6)(P<0.05, respectively), even though on the second and the third day no significant difference was observed among different groups .Besides, postoperative satisfaction rate and the evaluation of cosmetic results in endoscopic thyroidectomy groups were significantly higher than those in the open group(P<0.05, respectively).Furthermore, 90 days after operation, the satisfaction rate and the eval-uation of cosmetic results in the endoscopic thyroidectomy group through bilateral -nipple approach (96.7%,8.8 ± 0.9)were significantly higher than those in the endoscopic thyroidectomy group through breast approach (92.1%, 7.3 ±0.7)(P<0.05, respectively).Conclusions Endoscopic thyroidectomy is a feasible and safe procedure . Endoscopic thyroidectomy through bilateral-nipple approach has a higher long-term satisfaction rate as well as bet-ter cosmetic results , which is an ideal choice of thyroidectomy .

] AIM: To investigate the expression of the urotensin Ⅱ (UⅡ) receptor GPR14 in the aorta of apoE knockout mouse. METHODS: The expression of GPR14 in the aorta of apoE knockout C57BL/6J mice at various ages (18 weeks, 28 weeks, and 38 weeks old, respectively) was determined with competitive RT-PCR. A binding assay of [ 125 I]-UⅡ on the aortic tissue was also performed in 28 weeks group. RESULTS: We found significant upregulation of GPR14 mRNA at all three ages. Compared with wild type group at the same age, the GPR14 mRNA level in apoE knockout mice increased 54.2% in 18 week group (P

Objective To evaluate the safety and efficiency of robot assisted surgery guided by damage control orthopaedics(DCO) in polytraumatised patients with pelvic ring injuries.Methods A retrospective review of the pelvic fracture database was performed.Twenty-six patients who had sustained a pelvic fracture from September 2012 to December 2015 were suitable for robot-assisted minimally invasive internal fixation.They were 17 men and 9 women,aged from 23 to 58 years (average,42.6 years).Their Injury Severity Score(ISS) ranged from 20 to 31 points (average,21.3 years).According to Tile classification,6 cases were type B2,3 type B3,9 type C2 and 8 type C3.Guided by DCO,the vital signs were stabilized by all means and the fractures treated by simple and temporary external fixation before the pelvic and other fractures were managed by the robot-assisted minimally invasive internal fixation.Demographics,times to operating room (TOR),time from acute stabilization to late definitive internal fixation (TAL),time for bone union,type of robot-assisted surgery for major fractures,length of stay (LOS),postoperative complications and mortality were recorded.The outcomes of the pelvis were evaluated at the final follow-up according to the Matta criteria.Results Of the 26 patients,robot-navigated percutaneous screwing was conducted with 23 sacroiliac screws in 19,with 9 ramus pubicus screws in 9,with 6 supraacetabular screws in 4,and with 4 both-column screws in 2 cases.TOR averaged 2.7 times,TAL 5.9 days,LOS at ICU 2.1 days,ICU admission rate 46.2％ (12 of 26),hospital LOS 7.3 days,and time for pelvic bone union 79.0 days.None patients had postoperative complications related to the pelvic fracture and no one died.According to the Matta criteria at the final follow-ups,8 cases were excellent,11 good,5 fair and 2 poor,yielding an excellent and good rate of 73.1％.Conclusion Robot-navigated minimally invasive surgery plus DCO is effective,time saving and safe treatment for polytraumatised patients with pelvic ring injuries.

Objective To investigate the clinical value of 18 F?FDG PET/CT in staging multiple myeloma ( MM) and evaluating the glucose metabolic activity of MM. Methods A total of 25 MM patients ( 13 males, 12 females, age:39-67 years) from May 2010 to April 2015 were enrolled in this retrospective study. The SUVmax of each patient was recorded. D?S plus staging according to 18 F?FDG PET/CT was com?pared with the traditional D?S staging. The SUVmax and the percentage of plasmacytes of bone marrow of phase Ⅲ and non?phase Ⅲ ( phaseⅠand Ⅱ) according to D?S plus staging were compared. Two?sample t test and Wilcoxon rank sum test were used to analyze the data. Results In 25 MM patients, the range of SUVmax of lesions was 1.8-12?0 and the mean value was 5.15±2.74. According to D?S staging, the numbers of patients with phase Ⅰ,Ⅱ andⅢwere 7, 4 and 14, respectively. While the numbers were 3, 1 and 21 by D?S plus staging. Based on the D?S plus staging system, stages of 7 patients ( 28%, 7/25 ) were changed. According to the D?S plus staging system, the SUVmax between phaseⅢand non?phaseⅢpatients was significantly different (5.75±2.54 vs 3.00±0?70; t=2.12, P<0.05), while the percentage of plasma?cytes of bone marrow between the 2 groups had no significant difference ( 17. 50%( 4. 25%-41. 75%) vs 11?15%(10.25%-36.57%);z=0.05, P>0.05). Conclusion 18F?FDG PET/CT is of clinical importance for MM staging and metabolic activity assessment of MM.

Objective:To study the use of the Glissonean pedicle approach based on the triangular area among the right anterior pedicle, the right posterior pedicle and the right hepatic vein ( "APR triangle" ), followed by indocyanine green fluorescence negative staining in laparoscopic anatomical resection of right hepatic segments.Methods:The clinical data of 34 patients with liver tumors who underwent laparoscopic anatomical right hepatic segmentectomy at the Chinese Academy of Medical Sciences and Peking Union Medical College from September 2020 to September 2021 were analyzed retrospectively. Of the 34 patients, there were 24 males and 10 females, aged (58.3±10.3) years old. Data on completion of operation, operation time, intraoperative blood loss, intraoperative blood transfusion, postoperative complications and postoperative hospital stay were collected.Results:All the 34 patients had malignant liver tumors, and they were successfully operated using total laparoscopic surgery. There was no conversion to open surgery. Three patients underwent segment V resection, 3 patients segment VI resection, 5 patients segment VII resection, 2 patients segment V + segment VI resection, 9 patients segment VI + segment VII resection, 3 patients segment V + segment VII resection, 5 patients segment V dorsal segment + segment VI + segment VII resection, 3 patients right posterior section resection + anterior dorsal segment resection and 1 patient anterior dorsal section resection. The operation time was (275.58±82.28) min, the amount of intraoperative blood loss was 100(100, 300) ml, and there were no patients requiring blood transfusion during the operation. Liquid food was started on the first day after operation, and out-of bed activities were carried out on the second to third days after operation. The Clavien Dindo classification of postoperative complications was grade I in 32 patients and grade III in 2 patients. The postoperative hospital stay was (7.23±3.10) d. All tumor margins were negative for malignancy. All the 34 patients were followed-up for (8.94±2.94) months. By the end of follow-up, 34 patients had survived without tumor recurrence.Conclusion:The right Glisson pedicle approach based on the "APR triangle" and the anatomical resection of right hepatic segments with fluorescence negative staining were safe and feasible.

Objective:To investigate the efficacy of Qingruxiao granules combined with tamoxifen in the treatment of breast hyperplasia and its effect on serum hypoxia-inducible factor-alpha (HIF-α), angiopoietin-2 (Ang-2) and prolactin (PRL) levels. Methods:Ninety-eight patients with breast hyperplasia admitted to Xi'an No.3 Hospital from June 2020 to January 2022 were retrospectively included in this study. They were divided into control and observation groups ( n = 49/group) according to different treatments. The control group was treated with tamoxifen alone. The observation group was treated with Qingruxiao granules combined with tamoxifen. Clinical efficacy, symptom score, ultrasound parameters (glandular layer thickness, longest diameter of mass, maximum diameter of hypoechoic area, inner diameter of lactating tube), endocrine hormone levels (estradiol, progesterone, and prolactin), HIF-α, and Ang-2 pre- and post-treatment, as well as the incidence of adverse reactions were compared between the two groups. Results:Total response rate in the observation group was significantly higher than that in the control group [93.88% (4/49) vs. 77.55%, χ2 = 5.33, P < 0.05). After treatment, breast mass score, breast pain, systemic accompanying symptom, and nipple discharge in the observation group were (1.34 ± 0.29) points, (1.02 ± 0.36) points, (0.68 ± 0.17) points, (0.97 ± 0.15) points, respectively, which were significantly lower than (1.57 ± 0.23) points, (1.45 ± 0.41) points, (0.95 ± 0.26) points, and (1.28 ± 0.26) points, respectively, in the control group ( t = 4.35, 5.52, 6.08, 7.23, all P < 0.001). The glandular layer thickness, the longest diameter of mass, the maximum diameter of hypoechoic area, and the inner diameter of lactating duct in the observation group were (9.45 ± 1.67) mm, (11.46 ± 3.68) mm, (14.37 ± 4.22) mm, and (1.23 ± 0.39) mm, respectively, which were significantly lower than (11.26 ± 2.51) mm, (16.33 ± 4.01) mm, (19.87 ± 5.01) mm, (1.54 ± 0.48) mm in the control group ( t = 4.20, 2.26, 5.88, 3.51, all P < 0.001). Serum estradiol and prolactin levels in the observation group were (122.35 ± 29.76) ng/L and (205.64 ± 36.42) IU/L, respectively, which were significantly lower than (139.76 ± 30.48) ng/L and (251.49 ± 41.87) IU/L in the control group ( t = 2.86, 5.78, both P < 0.05). Serum progesterone level in the observation group was (9.22 ± 1.57) μg/L, which was significantly higher than (7.18 ± 1.21) μg/L in the control group ( t = -7.20, P < 0.05). Serum HIF-α and Ang-2 levels in the observation group were (0.15 ± 0.05) ng/L and (0.98 ± 0.11) ng/L, respectively, which were significantly lower than (0.24 ± 0.07) ng/L and (1.49 ± 0.22) ng/L in the control group ( t = 7.32, 14.51, both P < 0.001). There was no significant difference in the incidence of adverse reactions between the two groups ( P > 0.05). Conclusion:Qingruxiao granules combined with tamoxifen can effectively improve clinical symptoms, reduce tumor size, regulate endocrine hormone levels, decrease the expression of angiogenic factors in patients with breast hyperplasia, and is highly safe.

Objective Electrocardiographic (ECG) gated 4?dimensional CT angiography (4D?CTA) was performed to analyze the morphological characteristic differences between ruptured and unruptured intracranial aneurysms less than 5 mm to predict the rupture risk of small intracranial aneurysms. Methods A total of 118 patients with intracranial aneurysms less than 5 mm who underwent 4D?CTA examinations in our hospital from May 2014 to May 2017 were retrospectively analyzed. The whole study population was divided into ruptured group and unruptured group. Seventy?two patients were in the ruptured group and 46 patients were in the unruptured group. Original scanning data were reconstructed to produce 20 data sets of cardiac cycles with 5% time intervals. In addition, 20 groups of images and dynamic graphs were generated using three?dimensional software. We concluded the convex was point of impulse if small bubble or small pointed convex could be found in continuous three or more images at the same location. The morphological characteristics and clinical features of the two groups of aneurysms were firstly analyzed by univariate analysis, and then the meaningful indicators were analyzed by logistic regression, and the optimal diagnostic cutoff values were calculated using ROC curves. Results Univariate analysis showed that women, smoking history, location of aneurysm at the bifurcation, pulsation point, aspect ratio (AR) and size ratio (SR) were statistically significant different between the two groups of small aneurysms (P<0.05), but age, hypertension, type 2 diabetes, family history, history of multiple aneurysms, history of drinking, location, size, neck and tumor height had no significant differences between the two groups (P>0.05). Multivariate regression analysis showed that pulsation point (odds ratio=8.843, 95% confidence interval: 2.800—27.925) and large SR value (odds ratio=4.484, 95% confidence interval: 1.094—18.385) were independent risk factors for the aneurismal rupture. when the SR value was greater than 1.65, the area under the ROC curve was 0.832, the sensitivity to diagnose the risk of small aneurysm rupture was 76%, and the specificity is 70%. Conclusion The occurrence of pulsation point and SR value greater than 1.65 are independent predictors of the risk of intracranial aneurysm rupture less than 5 mm.