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- Highly sensitive HPLC-MS/MS assay for the quantitation of ondansetron in rat plasma and rat brain tissue homogenate following administration of a very low subcutaneous dose. [Journal Article]
- JPJ Pharm Biomed Anal 2019 Jul 12; 175:112766
- Ondansetron is a highly selective 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist that is well tolerated in the clinic. Pre-clinical studies in rats have shown interesting effects of small dos…
Ondansetron is a highly selective 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist that is well tolerated in the clinic. Pre-clinical studies in rats have shown interesting effects of small doses of ondansetron on cognition, behavioural sensitisation and epilepsy. However, the pharmacokinetic profile at a very low dose has not been reported, possibly because currently, there are no published analytical methods capable of quantifying trace levels of ondansetron in plasma or brain. The objective of this study was to develop and validate a highly sensitive HPLC-MS/MS assay capable of quantifying ondansetron in rat plasma and rat brain homogenate following a low subcutaneous administration of 1.0 μg/kg. Ondansetron was extracted by protein precipitation with methanol containing labeled ondansetron. The chromatography was performed on a Thermo Scientific Aquasil C18 analytical column (100 x 2.1 mm I.D., 5 μm) operating at 40 °C. The mobile phase consisted of acetonitrile and 10 mM ammonium formate pH 3 at a ratio of 30:70, respectively. The flow rate was fixed at 300 μL/min and ondansetron and the internal standard were both eluted at 2.3 min. A linear (1/x) relationship was used to perform the calibration over an analytical range from 20.0 - 10,000 pg/mL in plasma and from 2.00 to 1000 pg/mL in rat brain homogenate. The inter-batch precision and accuracy ranged from 3.7 to 4.7% and from 0.7 to 10.9% in rat plasma, respectively. The inter-batch precision and accuracy observed in rat brain was 4.5 to 6.4% and -5.1 to 4.9% respectively. The method met all requirements and the assay was suitable for the determination of the pharmacokinetic profile following a subcutaneous dose of 1.0 μg/kg body weight (BW) in rats.
- The serotonin system in the hippocampus CA3 involves in effects of CSDS on social recognition in adult female mandarin voles (Microtus mandarinus). [Journal Article]
- PNProg Neuropsychopharmacol Biol Psychiatry 2019 Jul 19; :109704
- Chronic social defeat stress (CSDS) exacerbated the development of stress-related psychiatric disorders, and the social recognition dysfunction is the core feature of many psychiatric disorders. Howe…
Chronic social defeat stress (CSDS) exacerbated the development of stress-related psychiatric disorders, and the social recognition dysfunction is the core feature of many psychiatric disorders. However, the effects of CSDS on female social recognition and the underlying neural mechanisms remain unclear. Using highly aggressive adult female mandarin voles (Microtus mandarinus) as animal model, the aim of this work is to investigate the effects of CSDS on social recognition in adult female rodents and the neurobiological mechanisms underlying these effects. Our results indicate the CSDS disrupted the normal social recognition in adult female voles. Meanwhile, defeated voles exhibited increased neural activity in the DG, CA1 and CA3 of the hippocampus. Furthermore, CSDS reduced levels of serotonin (5-HT) and serotonin 1A receptors (5-HT1AR) in the CA3. We also discovered that microinjection of 8-OH-DPAT into the CA3 effectively reversed the social recognition deficits induced by CSDS, and an infusion of WAY-100635 into the CA3 of control female voles impaired social recognition. Moreover, targeted activation of the 5-HT neuron projection from the DRN to CA3 by long-term administration of CNO significantly prevented the CSDS induced social recognition deficits. Taken together, our study demonstrated that CSDS induced social recognition deficits in adult female voles, and these effects were mediated by the action of 5-HT on the 5-HT1AR in the hippocampus CA3. The projection from the DRN to CA3 may be involved in social recognition deficits induced by CSDS.
- Preclinical characterization of ACH-000029, a novel anxiolytic compound acting on serotonergic and alpha-adrenergic receptors. [Journal Article]
- PNProg Neuropsychopharmacol Biol Psychiatry 2019 Jul 19; :109707
- Anxiety disorders are serious and common mental diseases, yet there is still a need for the development of more effective anxiolytics with better safety profiles than benzodiazepines and serotonin re…
Anxiety disorders are serious and common mental diseases, yet there is still a need for the development of more effective anxiolytics with better safety profiles than benzodiazepines and serotonin reuptake inhibitors. The serotonergic and noradrenergic neurotransmission have reciprocal interactions and are intricately related to the pathogenesis of anxiety. In this study, the anxiolytic-like effects of a novel compound, ACH-000029, 3-(2-(4-(2-methoxyphenyl) piperazine-1-yl) ethyl) quinazoline-4(3H)-one, which modulates the activities of both serotonergic and α-adrenergic receptors, is reported. This compound acts at selected serotonergic (5-HT1A and 5-HT1D partial agonism and 5-HT2A antagonism) and α-adrenergic (α-1A, 1B and 1D antagonism) receptors, with good selectivity over other G-protein-coupled receptors. ACH-000029 exhibited high blood-brain barrier permeation and acute anxiolytic effects in the marble burying (MB) and light-dark box (LDB) models of anxiety over the dose ranges 8-32 mg/kg i.p. and 16-30 mg/kg p.o. The anxiolytic activity was comparable to that observed for serotonin reuptake inhibitors (paroxetine and fluoxetine) and benzodiazepines (alprazolam, diazepam and clobazam). The analysis of the whole-brain c-fos expression following oral dosing showed that ACH-000029 regulated regions highly associated with the processing of environmental stimuli and anxiety behavior, such as the amygdala, paraventricular nucleus of the thalamus, retrosplenial dorsal, pallidum, bed nuclei of the stria terminalis, and locus ceruleus. No safety concerns were identified for ACH-000029 in the functional observational battery up to 50 mg/kg i.p. and in the nonprecipitated withdrawal test up to 30 mg/kg p.o. twice daily for 20 days. This work supports the further development of ACH-000029 as a drug candidate for the treatment of anxiety disorders. The analysis of the in vitro pharmacology and brain regions regulated by this compound may also lead to the exploration of other indications within the psychiatry field.
- Managing Depression with Bupleurum chinense Herbal Formula: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. [Journal Article]
- JAJ Altern Complement Med 2019 Jul 19
- CONCLUSIONS: BC formula alone or given as integrative medicine with antidepressants reduced depression severity. However, the evidence is low quality and at risk of bias. Well-designed studies are needed to validate the results we identified in this review.
- Melatonin synthesis in the optic lobes and midbrain of the grasshopper Oedipoda caerulescens. [Journal Article]
- AIArch Insect Biochem Physiol 2019 Jul 22; :e21605
- The pathways of insect melatonin (MEL) biosynthesis apparently follow the same routes as those identified in vertebrates but information on MEL synthesis variations related with serotonin (5-HT), 5-h…
The pathways of insect melatonin (MEL) biosynthesis apparently follow the same routes as those identified in vertebrates but information on MEL synthesis variations related with serotonin (5-HT), 5-hydroxy-indole acetic acid (5HIAA), and N-acetylserotonin (NAS) levels, as well as 5-HT N-acetyltransferase (NAT) activity throughout the day, is very limited in the insect nervous system. In the present study, the levels of MEL, metabolites (5-HT, NAS, and 5-HIAA) and enzyme NAT were determined in the optic lobes and the midbrain of the grasshopper Oedipoda caerulescens, in conditions of light and darkness. In both tissues, a different pattern of MEL synthesis was observed over the light/dark cycle. Variations in the levels of 5-HT, NAS and NAT activity related to the synthesis of cerebral MEL follow a pattern very similar to that observed in the pineal of mammals, with a peak of synthesis in the first half of the scotophase. Also, we observed differences in the metabolism of 5-HT between the optic lobes and the midbrain light/dark-dependent.
- Alkaloids and phenylpropanoid from Rhizomes of Arundo donax L. [Journal Article]
- NPNat Prod Res 2019 Jul 22; :1-6
- A new bis-indole alkaloid, named arundaline (1), a new phenylpropanoid, named arundalcohol (2), and four known alkaloids, N-acetyltryptamine (3), trans-N-(p-coumaroyl)serotonin (4), trans-N-feruloyls…
A new bis-indole alkaloid, named arundaline (1), a new phenylpropanoid, named arundalcohol (2), and four known alkaloids, N-acetyltryptamine (3), trans-N-(p-coumaroyl)serotonin (4), trans-N-feruloylserotonin (5), and tuberosine B (6), were isolated from 70% aqueous ethanol extracts of the rhizomes of Arundo donax L. Their structures were elucidated by spectroscopic analysis and comparison of the data with literature values. Compounds 3-6 were isolated from the genus Arundo for the first time.
- Risk of Congenital Heart Disease in Newborns with Prenatal Exposure to Anti-depressant Medications. [Journal Article]
- CCureus 2019 May 15; 11(5):e4673
- Introduction It is uncertain whether the use of selective serotonin-reuptake inhibitors (SSRI) and other anti-depressants during pregnancy is associated with an increased risk of congenital heart dis…
Introduction It is uncertain whether the use of selective serotonin-reuptake inhibitors (SSRI) and other anti-depressants during pregnancy is associated with an increased risk of congenital heart disease (CHD) in newborn. There have been various studies showing a number of adverse outcomes, including gestational hypertension, reduced birth weight, altered neonatal pain responses and persistent pulmonary hypertension of the newborn with exposure to anti-depressant medications. There have been very few longitudinal studies showing CHD association with the use of anti-depressant medications. Our objective is to examine the risk for congenital heart disease of the newborn associated with prenatal exposure to antidepressant medication. Methods We reviewed charts of mothers who were referred for a fetal echocardiogram between January 1st, 2009 and December 31st, 2014. We identified mothers who were exposed to antidepressant medications prenatally. Fetal echocardiograms for these patients were reviewed by two fetal cardiologists and each was blinded to the others' findings. Results A total of 40 patients were identified with prenatal exposure to SSRI. Seven (18%) out of these 40 were found to have a form of CHD. Two fetuses whose mothers were exposed to fluoxetine during pregnancy had large posteriorly malaligned ventricular septal defect, sub-aortic stenosis and critical coarctation identified on fetal echocardiogram. Exposure to citalopram during pregnancy was found to be associated with a moderate size secundum atrial septal defect on one patient and a moderate size mid muscular ventricular septal defect seen on fetal echocardiogram in another patient. Exposure to venlafaxine during pregnancy showed two small muscular ventricular septal defects on fetal echocardiogram on one patient and ductal constriction with increased ductal velocity on another patient. One of the women on escitalopram had a fetus with a large membranous ventricular septal defect (VSD), secundum atrial septal defect (ASD) and left superior vena cava. None of the women on a combination of drugs had CHD. Conclusion There is a risk of congenital heart disease in patients who are prenatally exposed to anti-depressant medications as evident by the specific echocardiographic abnormalities noted in the study.
- A Rare Overlap of Serotonin Syndrome and Status Epilepticus Confirmed on Electroencephalogram. [Case Reports]
- CCureus 2019 May 15; 11(5):e4667
- Serotonin syndrome (SS) is a potentially fatal complication of treatment with various serotonergic agents. It is diagnosed clinically and consists of cognitive, autonomic, and neuromuscular dysfuncti…
Serotonin syndrome (SS) is a potentially fatal complication of treatment with various serotonergic agents. It is diagnosed clinically and consists of cognitive, autonomic, and neuromuscular dysfunction. Although serotonin syndrome has been known to induce seizures, there are no reported cases of electroencephalogram (EEG)-documented status epilepticus (SE) associated with serotonin syndrome. We report a case of serotonin syndrome and status epilepticus in a patient thought to have overdosed on both fluoxetine and bupropion in the setting of alcohol intoxication. Our patient required aggressive treatment with various anticonvulsant medications to control status epilepticus and was also treated with cyproheptadine for the serotonin syndrome. This paper will also discuss the contributing factors of fluoxetine and bupropion to this presentation in the context of alcohol intoxication.
- Inpatient management strategies in a severe case of heparin-induced thrombocytopenia. [Journal Article]
- TATransfus Apher Sci 2019 Jul 09
- We present important laboratory testing and clinical management strategies used to safely discharge home a 69-year old woman with heparin-induced thrombocytopenia (HIT) from the hospital. She was adm…
We present important laboratory testing and clinical management strategies used to safely discharge home a 69-year old woman with heparin-induced thrombocytopenia (HIT) from the hospital. She was admitted for a coronary artery bypass graft procedure for which she was anticoagulated with heparin. Shortly after the procedure she developed thrombocytopenia and was diagnosed with HIT using the 4Ts scoring system, a latex-enhanced immunoassay (LEI) screen and confirmatory serotonin release assay. Her anticoagulation was switched from heparin to argatroban, and response to treatment was monitored in the laboratory using LEI. Unfortunately, she also received platelet transfusions and subsequently developed multifocal deep vein thrombosis with worsening platelet counts with nadir less than 10 x 10^3/μL. After five therapeutic plasma exchange procedures we noted an improvement in platelet counts, which plateaued into the 50s x 10^3/μL. Furthermore, the LEI remained positive. At this juncture we decided to transition from argatroban to fondaparinux so that she could leave the hospital in stable condition. Upon follow-up with hematology she exhibited no worsening clinical signs or symptoms of disease, and platelet counts markedly improved to within normal limits of detection. In this report we examine the utility of LEI in monitoring patients with HIT, therapeutic plasma exchange in the management of severe HIT (with thrombosis), and the use of subcutaneous fondaparinux in managing HIT in the outpatient setting.
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- Novel electrochemical biosensor for serotonin detection based on gold nanorattles decorated reduced graphene oxide in biological fluids and in vitro model. [Journal Article]
- BBBiosens Bioelectron 2019 Jul 13; 142:111502
- Abnormal level of serotonin (ST) in body fluids is related to various clinical conditions including behavioral and psychotic disorders; hence its fast detection in clinically relevant ranges have tre…
Abnormal level of serotonin (ST) in body fluids is related to various clinical conditions including behavioral and psychotic disorders; hence its fast detection in clinically relevant ranges have tremendous importance in medical science. In view of this, we have developed a novel biosensor for ST detection using Au-nanorattles (AuNRTs)- reduced graphene oxide (rGO) nanocomposite coated on to the gold nanoparticles (AuNPs) deposited glassy carbon electrode (GCE). The nanocomposite/sensor probe was characterized using UV-Vis, TEM, SAED, EDX, AFM, and electrochemical techniques including LSV and EIS. Thereafter, the suitability of fabricated GCE/AuNPs/AuNRTs-rGO-Naf sensor probe was applied for ST determination which showed a linear dynamic range (LDR) of 3 × 10-6 - 1 × 10-3 M and the detection limit (DL) of 3.87 (±0.02) ×10-7 (RSD < 4.2%) M, which falls in the ranges of normal as well as various abnormal pathophysiological conditions. The designed sensor is successfully applied to detect ST in various real matrices viz. urine, blood serum, and in vitro model to show its direct clinical/practical applicability. Interferences due to the coexisting molecules were assessed and the long-term stability of the designed sensor was also examined which was found to be 8 weeks.