Anodic behavior of aripiprazole(ARP) was studied using electrochemical methods.Charge transfer,diffusion and surface coverage coefcients of adsorbed molecules and the number of electrons transferred in electrode mecha...Anodic behavior of aripiprazole(ARP) was studied using electrochemical methods.Charge transfer,diffusion and surface coverage coefcients of adsorbed molecules and the number of electrons transferred in electrode mechanisms were calculated for quasi-reversible and adsorp-tion-controlled electrochemical oxidation of ARP at 1.15 V versus Ag/AgCl at pH 4.0 in Britton-Robinson buffer(BR) on glassy carbon electrode.Voltammetric methods for direct determination of ARP in pharmaceutical dosage forms and biological samples were developed.Linearity range is found as from 11.4 μM(5.11 mg/L) to 157 μM(70.41 mg/L) without stripping mode and it is found as from 0.221 μM(0.10 mg/L) to 13.6 μM(6.10 mg/L) with stripping mode.Limit of detection(LOD) was found to be 0.11 μM(0.05 mg/L) in stripping voltammetry.Methods were successfully applied to assay the drug in tablets,human serum and human urine with good recoveries between 95.0% and 104.6% with relative standard deviation less than 10%.展开更多
Objectives: To elucidate the pharmacological profile of aripiprazole, we examined its ameliorating effect on the methamphetamine-induced disruption of latent inhibition (LI) in rats. Method: The effect was measured us...Objectives: To elucidate the pharmacological profile of aripiprazole, we examined its ameliorating effect on the methamphetamine-induced disruption of latent inhibition (LI) in rats. Method: The effect was measured using a conditioned emotional response procedure. The conditioned stimulus was a tone (2.8 kHz, 90 dB), and the unconditioned stimulus was a mild foot shock delivered through a floor grid. The conditioning procedure was repeated five times. Results: Methamphetamine-induced (1.0 mg/kg, i.p.) disruption of LI was ameliorated by the administration of haloperidol (0.2 mg/kg, i.p.) and by a moderate dose of aripiprazole (0.3 mg/kg, i.p.) but not by a lower or higher dose (0.1 or 3.0 mg/kg, i.p.) of aripiprazole. However, immunohistochemical examination showed increased levels of c-Fos expression in the shell of the nucleus accumbens after the administration of haloperidol (0.2 mg/kg, i.p.) but not of aripiprazole (0.3 mg/kg, i.p.). Conclusions: It is suggested that aripiprazole has an ameliorating effect on methamphetamine-induced disruption of latent inhibition within only a marginal therapeutic window.展开更多
Objective:To observe the effect of aripiprazole and olanzapine on the cognitive function in patients with schizophrenia in order to provide a reference evidence for the clinical medication.Methods:A total of 60 patien...Objective:To observe the effect of aripiprazole and olanzapine on the cognitive function in patients with schizophrenia in order to provide a reference evidence for the clinical medication.Methods:A total of 60 patients with schizophrenia who were admitted in our hospital were included in the study and randomized into the treatment 1 group and treatment 2 group.The patients in the two groups were given aripiprazole and olanzapine,respectively.PANSS,WCST,DS,IGT,and EIRT were used to evaluate the disease condition and cognitive function before and after treatment in the two groups.Results:Comparision of PANSS scores and other various scores before treatment between the two groups was not significantly different(P>0.05);however,PANSS scores and other various scores after treatment were significantly reduced(P<0.05).Comparision of PANSS scores and other various scores after treatment between the two groups was not significantly different(P>0.05).DS,WCST,and IGT scores before treatment between the two groups was comparable(P>0.05),and those scores after treatment were significantly elevated(P<0.05).DS score after treatment in the treatment 2 group was significantly higher than that in the treatment 1 group(P<0.05).Comparison of WCST and IGT scores after treatment between the two groups was not significantly different(P>0.05).The four cognition scores of happiness,fear,anger,and disgust after treatment in the treatment 1 group were significantly elevated(P<0.05),while the cognition of happiness and sadness after treatment in the treatment 2 group was significantly elevated when compared with before treatment(P<0.05).The comparison of various scores before and after treatment between the two groups was not significantly different(P>0.05).Conclusions:Aripiprazole and olanzapine can improve the clinical symptoms and partial cognitive function in patients with schizophrenia,while aripiprazole can make a better effect on the work and memory.展开更多
Aripiprazole, a third-generation antipsychotic, has been considered to have a high safety profile and rare withdrawal symptoms. We reported the case of a schizophrenic patient with a significant obsession, who was tre...Aripiprazole, a third-generation antipsychotic, has been considered to have a high safety profile and rare withdrawal symptoms. We reported the case of a schizophrenic patient with a significant obsession, who was treated with a high dosage of aripiprazole and fluoxetine. Generalized tonic-clonic seizure occurred two days after abruptly stopping these two medications. Gradually tapering aripiprazole is suggested in clinical practice, especially when using a high dosage.展开更多
The aim of this study was to consider the characteristics of intramuscular diffusion status of risperidone and aripiprazole long acting injectable (LAI) by ultrasonography. Subjects were 40 adult subjects diagnosed wi...The aim of this study was to consider the characteristics of intramuscular diffusion status of risperidone and aripiprazole long acting injectable (LAI) by ultrasonography. Subjects were 40 adult subjects diagnosed with schizophrenia and treated with LAI [32 patients were risperidone LAI (RLAI) and 8 patients were aripiprazole LAI (ALAI)]. However, in this paper, only three cases (one RLAI case and 2 ALAI cases) were selected to illustrate the diffusion effects of both LAI. Dorsogluteal intramuscular (IM) injection sites were measured at prone position using the “double cross” method. Before LAI injection, the distance from the epidermis to the under-fascia (DEUF), and distance from the epidermis to the iliac bone (DEI) at the IM injection site were assessed by using ultrasonography: 1) the injection needle was inserted to the gluteus medius, and 2) observed the diffusion status within the muscle injected RLAI and ALAI were confirmed using the B-mode ultrasonography. Both RLAI and ALAI were depicted as high echogenicity with acoustic shadowing. It was considered that the diffusion states of LAIs by ultrasonography were important time course evaluations providing objective evidence.展开更多
Colorectal cancer(CRC)is a type of malignant tumor that seriously threatens human health and life,and its treatment has always been a difficulty and hotspot in research.Herein,this study for the first time reports tha...Colorectal cancer(CRC)is a type of malignant tumor that seriously threatens human health and life,and its treatment has always been a difficulty and hotspot in research.Herein,this study for the first time reports that antipsychotic aripiprazole(Ari)against the proliferation of CRC cells both in vitro and in vivo,but with less damage in normal colon cells.Mechanistically,the results showed that5-hydroxytryptamine 2B receptor(HTR2B)and its coupling protein G protein subunit alpha q(Gaq)were highly distributed in CRC cells.Ari had a strong affinity with HTR2B and inhibited HTR2B downstream signaling.Blockade of HTR2B signaling suppressed the growth of CRC cells,but HTR2B was not found to have independent anticancer activity.Interestingly,the binding of Gaq to HTR2B was decreased after Ari treatment.Knockdown of Gaq not only restricted CRC cell growth,but also directly affected the antiCRC efficacy of Ari.Moreover,an interaction between Ari and Gaq was found in that the mutation at amino acid 190 of Gaq reduced the efficacy of Ari.Thus,these results confirm that Gaq coupled to HTR2B was a potential target of Ari in mediating CRC proliferation.Collectively,this study provides a novel effective strategy for CRC therapy and favorable evidence for promoting Ari as an anticancer agent.展开更多
基金Scientific Research Unit of Ankara University forfinancial support with Grant number:11B4240005
文摘Anodic behavior of aripiprazole(ARP) was studied using electrochemical methods.Charge transfer,diffusion and surface coverage coefcients of adsorbed molecules and the number of electrons transferred in electrode mechanisms were calculated for quasi-reversible and adsorp-tion-controlled electrochemical oxidation of ARP at 1.15 V versus Ag/AgCl at pH 4.0 in Britton-Robinson buffer(BR) on glassy carbon electrode.Voltammetric methods for direct determination of ARP in pharmaceutical dosage forms and biological samples were developed.Linearity range is found as from 11.4 μM(5.11 mg/L) to 157 μM(70.41 mg/L) without stripping mode and it is found as from 0.221 μM(0.10 mg/L) to 13.6 μM(6.10 mg/L) with stripping mode.Limit of detection(LOD) was found to be 0.11 μM(0.05 mg/L) in stripping voltammetry.Methods were successfully applied to assay the drug in tablets,human serum and human urine with good recoveries between 95.0% and 104.6% with relative standard deviation less than 10%.
文摘Objectives: To elucidate the pharmacological profile of aripiprazole, we examined its ameliorating effect on the methamphetamine-induced disruption of latent inhibition (LI) in rats. Method: The effect was measured using a conditioned emotional response procedure. The conditioned stimulus was a tone (2.8 kHz, 90 dB), and the unconditioned stimulus was a mild foot shock delivered through a floor grid. The conditioning procedure was repeated five times. Results: Methamphetamine-induced (1.0 mg/kg, i.p.) disruption of LI was ameliorated by the administration of haloperidol (0.2 mg/kg, i.p.) and by a moderate dose of aripiprazole (0.3 mg/kg, i.p.) but not by a lower or higher dose (0.1 or 3.0 mg/kg, i.p.) of aripiprazole. However, immunohistochemical examination showed increased levels of c-Fos expression in the shell of the nucleus accumbens after the administration of haloperidol (0.2 mg/kg, i.p.) but not of aripiprazole (0.3 mg/kg, i.p.). Conclusions: It is suggested that aripiprazole has an ameliorating effect on methamphetamine-induced disruption of latent inhibition within only a marginal therapeutic window.
基金Science and technology research and development program of Hebei province(No.1221068D).
文摘Objective:To observe the effect of aripiprazole and olanzapine on the cognitive function in patients with schizophrenia in order to provide a reference evidence for the clinical medication.Methods:A total of 60 patients with schizophrenia who were admitted in our hospital were included in the study and randomized into the treatment 1 group and treatment 2 group.The patients in the two groups were given aripiprazole and olanzapine,respectively.PANSS,WCST,DS,IGT,and EIRT were used to evaluate the disease condition and cognitive function before and after treatment in the two groups.Results:Comparision of PANSS scores and other various scores before treatment between the two groups was not significantly different(P>0.05);however,PANSS scores and other various scores after treatment were significantly reduced(P<0.05).Comparision of PANSS scores and other various scores after treatment between the two groups was not significantly different(P>0.05).DS,WCST,and IGT scores before treatment between the two groups was comparable(P>0.05),and those scores after treatment were significantly elevated(P<0.05).DS score after treatment in the treatment 2 group was significantly higher than that in the treatment 1 group(P<0.05).Comparison of WCST and IGT scores after treatment between the two groups was not significantly different(P>0.05).The four cognition scores of happiness,fear,anger,and disgust after treatment in the treatment 1 group were significantly elevated(P<0.05),while the cognition of happiness and sadness after treatment in the treatment 2 group was significantly elevated when compared with before treatment(P<0.05).The comparison of various scores before and after treatment between the two groups was not significantly different(P>0.05).Conclusions:Aripiprazole and olanzapine can improve the clinical symptoms and partial cognitive function in patients with schizophrenia,while aripiprazole can make a better effect on the work and memory.
文摘Aripiprazole, a third-generation antipsychotic, has been considered to have a high safety profile and rare withdrawal symptoms. We reported the case of a schizophrenic patient with a significant obsession, who was treated with a high dosage of aripiprazole and fluoxetine. Generalized tonic-clonic seizure occurred two days after abruptly stopping these two medications. Gradually tapering aripiprazole is suggested in clinical practice, especially when using a high dosage.
文摘The aim of this study was to consider the characteristics of intramuscular diffusion status of risperidone and aripiprazole long acting injectable (LAI) by ultrasonography. Subjects were 40 adult subjects diagnosed with schizophrenia and treated with LAI [32 patients were risperidone LAI (RLAI) and 8 patients were aripiprazole LAI (ALAI)]. However, in this paper, only three cases (one RLAI case and 2 ALAI cases) were selected to illustrate the diffusion effects of both LAI. Dorsogluteal intramuscular (IM) injection sites were measured at prone position using the “double cross” method. Before LAI injection, the distance from the epidermis to the under-fascia (DEUF), and distance from the epidermis to the iliac bone (DEI) at the IM injection site were assessed by using ultrasonography: 1) the injection needle was inserted to the gluteus medius, and 2) observed the diffusion status within the muscle injected RLAI and ALAI were confirmed using the B-mode ultrasonography. Both RLAI and ALAI were depicted as high echogenicity with acoustic shadowing. It was considered that the diffusion states of LAIs by ultrasonography were important time course evaluations providing objective evidence.
基金supported by Chongqing basic research and frontier exploration project(cstc2022ycjh-bgzxm0119,China)。
文摘Colorectal cancer(CRC)is a type of malignant tumor that seriously threatens human health and life,and its treatment has always been a difficulty and hotspot in research.Herein,this study for the first time reports that antipsychotic aripiprazole(Ari)against the proliferation of CRC cells both in vitro and in vivo,but with less damage in normal colon cells.Mechanistically,the results showed that5-hydroxytryptamine 2B receptor(HTR2B)and its coupling protein G protein subunit alpha q(Gaq)were highly distributed in CRC cells.Ari had a strong affinity with HTR2B and inhibited HTR2B downstream signaling.Blockade of HTR2B signaling suppressed the growth of CRC cells,but HTR2B was not found to have independent anticancer activity.Interestingly,the binding of Gaq to HTR2B was decreased after Ari treatment.Knockdown of Gaq not only restricted CRC cell growth,but also directly affected the antiCRC efficacy of Ari.Moreover,an interaction between Ari and Gaq was found in that the mutation at amino acid 190 of Gaq reduced the efficacy of Ari.Thus,these results confirm that Gaq coupled to HTR2B was a potential target of Ari in mediating CRC proliferation.Collectively,this study provides a novel effective strategy for CRC therapy and favorable evidence for promoting Ari as an anticancer agent.
