Atrioventricular Block ; complications ; Atrioventricular Node ; surgery ; Heart Neoplasms ; complications ; surgery ; Humans

Objective To studythe efficacy of levosimendan in treating refractory heart failure complicating severe renal in sufficiency.Methods Sixty-seven cases of refractory heart failure complicating severe renal insufficiency in the internal medicine department of our hospital were randomly divided into the levosimendan treatment group(L group,n=33)and dopamine treatment group(D group,n=34).The changes of N-terminal pro-B-type natriuretic peptide(NT-pro-BNP),left ventricular ejection fraction (LVEF)and glomerular filtration rate(GFR)before treatment and on 1,3,7,30 d after treatment were compared between the two groups and analyzed.Results Before the treatment,there were no statistically significant differences in the baseline indicators between the two groups(P＞0.05).The group L:the NT-pro-BNP level on 1,3,7 d after treatment was decreased significantly(P＜ 0.05),LVEF on 3,7 d was significantly increased compared with th baseline(P＜0.05)and GFR on 1,3,7,30 d was significantly increased compared with the baseline(P＜0.05).The group D:the NT-pro-BNP level on 7 d of treatment was significantly decreased(P＜0.05),LVEF on 7 d of treatment was significantly increased compared with the baseline(P＜0.05),and no statistically significant changes were observed in GFR on 1,3,7,30 d(P＞0.05).After treatment,NT-pro-BNP,LVEF and GFR significant level values in the group L were better than those in the group D.Conclusion Levosimendan is superior to dopamine in improving heart and renal function for the patients with refractory heart failure complicating severe renal insufficiency.

AIM: To investigate the effects of non-invasive ischemic preconditioning on nitric oxide (NO)/endothelin-1 (ET-1) imbalance and gas exchange impairment following limb ischemia reperfusion in patients undergoing unilateral lower extremity surgery with tourniquet. METHODS: Twenty-seven patients aged 25-65 years, whose tourniquets duration varied from 1 h to 1.5 h and matched American Society of Anesthesiologists Physical Status Ⅰ-Ⅱ, were randomized into two groups: a control group (n=14) and a ischemic preconditioning group (IPC group, n=13) in which patients received three cycles of 5 min of ischemia/5 min of reperfusion before tourniquet inflation. Radial arterial blood gas, plasma malondialdehyde (MDA) and NO, serum ET-1 and interleukin-6 (IL-6) were measured just before tourniquet inflation(T_0), 1 h after inflation(T_1), and 0.5 h(T_2), 2 h(T_3), 6 h(T_4), 24 h(T_5) after tourniquet deflation. Meanwhile NO/ET-1 ratio, alveolar-arterial oxygen gradient (P_(A-a)DO_2) and intrapulmonary shunt (Qs/Qt) were calculated. RESULTS: In control group, arterial partial pressure of oxygen (PaO_2) were decreased, while P_(A-a)DO_2 and Qs/Qt were increased significantly at T_4 compared to the baselines at T_0 (P<0.01). Plasma NO levels and NO/ET-1 ratios decreased gradually after tourniquets deflation and statistical significances were observed at T_3 (P<0.01) with a valley at T_4 (P<0.01) and recovered to baselines at T_5. Serum ET-1, IL-6 and plasma MDA began to increase remarkably after T_3 (P<0.05 or P<0.01), peaked at T_4 and dropped slightly at T_5. The changes above-mentioned could be well attenuated by the application of IPC (P<0.05 or P<0.01) except PaO_2 (P>0.05). CONCLUSION: Clinical application of unilateral tourniquet within safe time limit (1.5 h) may lead to limb ischemia reperfusion and further pulmonary gas exchange impairment, which could be partially attenuated by the application of IPC via alleviating NO/ET-1 imbalance.

OBJECTIVE: To investigate the effects of Enalapril maleate folic acid tablets on carotid atherosclerosis in H type hypertension patients with type 2 diabetes mellitus (T2DM) and its potential mechanism.METHODS: In prospective control study, 182 H type hypertension patients with T2DM were selected from Chongqing People's Hospital during Jan. 2014-Jan. 2016, and then randomly divided into observation group and control group, with 91 cases in each group. All patients received basic or hypoglycemic treatment of premixed insulin; observation group was additionally given Enalapril maleate folic acid tablets (containing enalapril maleate 10 mg, folic acid 0. 8 mg in each tablet) orally, one tablet, qd; control group was additionally given Enalapril maleate tablets (containing enalapril maleate 10 mg in each tablet) orally, one tablet, qd. Treatment course lasted for 12 months. The levels of blood pressure, plasma homocysteine (Hcy), fasting blood glucose (FBG), C-reactive protein (CRP) and carotid plaque score were detected in 2 groups before treatment, 12 months after treatment. RESULTS: Compared to before treatment, SBP and DBP of 2 groups were decreased significantly in 2 groups after 12 months of treatment (P<0. 05); there was no statistical significance between 2 groups (P>0. 05). The levels of plasma Hcy, FBG and CRP, carotid intima-media thickness and carotid plaque integral in observation group were significantly lower than control group (P<0. 05). CONCLUSIONS: Enalapril maleate folic acid tablets can relieve inflammation by reducing plasma Hcy, FBG and CRP so as to treat carotid atherosclerosis in H type hypertension patients with T2DM.

Dopamine D₃ receptor (D₃R) is implicated in multiple psychotic symptoms. Increasing the D₃R selectivity over dopamine D₂ receptor (D₂R) would facilitate the antipsychotic treatments. Herein, novel carbazole and tetrahydro-carboline derivatives were reported as D₃R selective ligands. Through a structure-based virtual screen, ZLG-25 (D₃R K_i = 685 nmol/L; D₂R K_i > 10,000 nmol/L) was identified as a novel D₃R selective bitopic ligand with a carbazole scaffold. Scaffolds hopping led to the discovery of novel D₃R-selective analogs with tetrahydro-β-carboline or tetrahydro-γ-carboline core. Further functional studies showed that most derivatives acted as hD₃R-selective antagonists. Several lead compounds could dose-dependently inhibit the MK-801-induced hyperactivity. Additional investigation revealed that 23j and 36b could decrease the apomorphine-induced climbing without cataleptic reaction. Furthermore, 36b demonstrated unusual antidepressant-like activity in the forced swimming tests and the tail suspension tests, and alleviated the MK-801-induced disruption of novel object recognition in mice. Additionally, preliminary studies confirmed the favorable PK/PD profiles, no weight gain and limited serum prolactin levels in mice. These results revealed that 36b provided potential opportunities to new antipsychotic drugs with the multiple antipsychotic-like properties.