(R)-N-(β-Trichlorogermyl propionyl)thiazolidine-2-thione-4-carboxylic methyl ether(1) and its sesquioxide(2) were synthesized. The crystal structure of 1 was determined by means of X-ray diffraction analysis, which s...(R)-N-(β-Trichlorogermyl propionyl)thiazolidine-2-thione-4-carboxylic methyl ether(1) and its sesquioxide(2) were synthesized. The crystal structure of 1 was determined by means of X-ray diffraction analysis, which shown that the >CO and >CS groups are located in the opposite sides of C(4)—N—C(3) bond with transconfiguration. The electronic structures and optimized configurations of compounds 1 and 2 were studied with MNDO method.展开更多
Background:The clinical efficacy of fentanyl for pain control differs greatly across individuals.The purpose of this study was to investigate the impact of CYP3A4*1G polymorphism including wild-type homozygote (CYP3A4...Background:The clinical efficacy of fentanyl for pain control differs greatly across individuals.The purpose of this study was to investigate the impact of CYP3A4*1G polymorphism including wild-type homozygote (CYP3A4*1/*1,GG),mutant heterozygote (CYP3A4*1/*1G,GA),and mutant homozygote (CYP3A4*1G/*1G,AA)on fentanyl analgesia in Chinese patients undergoing hysteroscopy by the assessment of analgesia nociception index (ANI). Methods:A total of 200 gynecologic patients scheduled for elective hysteroscopy under general anesthesia at Peking University People's Hospital from May to December in 2017 were enrolled in this study.Venous blood was withdrawn for genotyping of CYP3A4*1G before operation.Fentanyl 1μg/kg was administered preoperatively followed by target-controlled infusion of propofol for induction and maintenance.Intraoperative analgesic efficacy of fentanyl was assessed by ANI monitoring at T0(entering room),T1(cervical dilation), T2(start of cervical aspiration),and T3(end of cervical aspiration)time points.The duration of propofol infusion and total dosage of propofol were recorded as well. Results:The patients were divided into three groups according to CYP3A4*1G polymorphism,including 143 in GG group,47in GA group, and 10 in AA group.There was no significant difference in clinical demographics among three groups.The frequency of CYP3A4*1G variant alleles accounted for 16.8%and the distribution of variant alleles was consistent with Hardy-Weinberg equilibrium.Using a multilevel model,ANI values at T1(63.81±19.61),T2(63.63±17.82),and T3(65.68±17.79)were significantly lower than that at T0 (77.16±12.93)in the study population (F =23.50,P <0.001),suggesting that higher levels of pain at T 1,T2,and T3 than T0.Patients with GG genotype showed significantly lower ANI than those with GA or AA genotypes during hysteroscopy under the same dose of fentanyl. Conclusion:CYP3A4*1G polymorphism associated with the analgesic efficacy of intraoperative fentanyl in the patients undergoing hysteroscopy under general anesthesia.展开更多
文摘(R)-N-(β-Trichlorogermyl propionyl)thiazolidine-2-thione-4-carboxylic methyl ether(1) and its sesquioxide(2) were synthesized. The crystal structure of 1 was determined by means of X-ray diffraction analysis, which shown that the >CO and >CS groups are located in the opposite sides of C(4)—N—C(3) bond with transconfiguration. The electronic structures and optimized configurations of compounds 1 and 2 were studied with MNDO method.
文摘Background:The clinical efficacy of fentanyl for pain control differs greatly across individuals.The purpose of this study was to investigate the impact of CYP3A4*1G polymorphism including wild-type homozygote (CYP3A4*1/*1,GG),mutant heterozygote (CYP3A4*1/*1G,GA),and mutant homozygote (CYP3A4*1G/*1G,AA)on fentanyl analgesia in Chinese patients undergoing hysteroscopy by the assessment of analgesia nociception index (ANI). Methods:A total of 200 gynecologic patients scheduled for elective hysteroscopy under general anesthesia at Peking University People's Hospital from May to December in 2017 were enrolled in this study.Venous blood was withdrawn for genotyping of CYP3A4*1G before operation.Fentanyl 1μg/kg was administered preoperatively followed by target-controlled infusion of propofol for induction and maintenance.Intraoperative analgesic efficacy of fentanyl was assessed by ANI monitoring at T0(entering room),T1(cervical dilation), T2(start of cervical aspiration),and T3(end of cervical aspiration)time points.The duration of propofol infusion and total dosage of propofol were recorded as well. Results:The patients were divided into three groups according to CYP3A4*1G polymorphism,including 143 in GG group,47in GA group, and 10 in AA group.There was no significant difference in clinical demographics among three groups.The frequency of CYP3A4*1G variant alleles accounted for 16.8%and the distribution of variant alleles was consistent with Hardy-Weinberg equilibrium.Using a multilevel model,ANI values at T1(63.81±19.61),T2(63.63±17.82),and T3(65.68±17.79)were significantly lower than that at T0 (77.16±12.93)in the study population (F =23.50,P <0.001),suggesting that higher levels of pain at T 1,T2,and T3 than T0.Patients with GG genotype showed significantly lower ANI than those with GA or AA genotypes during hysteroscopy under the same dose of fentanyl. Conclusion:CYP3A4*1G polymorphism associated with the analgesic efficacy of intraoperative fentanyl in the patients undergoing hysteroscopy under general anesthesia.
