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Timothy T. Soncrant - One of the best experts on this subject based on the ideXlab platform.

  • chronic treatment with meta chlorophenylpiperazine m cpp alters behavioral and cerebral metabolic responses to the serotonin agonists m cpp and quipazine but not 8 hydroxy 2 di n propylamino tetralin
    Psychopharmacology, 1992
    Co-Authors: Ulderico Freo, Harold W. Holloway, Nigel H Greig, Timothy T. Soncrant
    Abstract:

    The effects of the serotonin (5-HT) agonists Meta-Chlorophenylpiperazine (m-CPP), quipazine and 8-hydroxy-2(di-n-propylamino)tetralin (DPAT) on behavior and on regional cerebral metabolic rates for glucose (rCMRglc) were measured in control rats or in rats pretreated for 2 weeks with continuous infusion of saline or m-CPP (2.5 mg/kg/day, subcutaneously). rCMRglc was measured in 71 brain regions, using the quantitative autoradiographic [14C]2-deoxy-D-glucose technique, at 15 min after acute administration of m-CPP 2.5 mg/kg, 60 min after quipazine 20 mg/kg, or 10 min after DPAT 1 mg/kg. Behavioral effects were assessed for m-CPP with an activity monitor, for quipazine by counting head shakes and for DPAT by scoring the serotonin syndrome. Chronic m-CPP pretreatment produced tolerance to hypolocomotion induced by acute m-CPP and to head shakes caused by acute quipazine, but did not alter the serotonin syndrome produced by DPAT. m-CPP 2.5 mg/kg IP produced widespread rCMRglc reductions in control rats but failed to modify rCMRglc in any region after chronic m-CPP pretreatment. Quipazine increased rCMRglc in 4 regions in control rats, but reduced rCMRglc in 14 brain areas of chronically m-CPP-pretreated animals. DPAT altered rCMRglc to the same degree in control (25 regions affected) and in chronically m-CPP-pretreated rats (28 regions affected). Reduced behavioral and metabolic effects of acute m-CPP in chronically m-CPP-pretreated rats were not due to pharmacokinetic alterations. These results demonstrate that chronic administration of m-CPP produces behavioral and metabolic tolerance to acute administration of m-CPP, but not of DPAT. They suggest that hypolocomotion and the serotonin syndrome are mediated by different 5-HT receptor subtypes, and that chronic m-CPP administration produces functional down-regulation of 5-HT1B/1C but not of 5-HT1A-coupled mechanisms.

Negrin Negrev - One of the best experts on this subject based on the ideXlab platform.

  • isoteoline a putative serotonin antagonist inhibits meta chlorophenylpiperazine but not 1 2 5 dimethoxy 4 iodphenyl 2 aminopropane and 8 hydroxy 2 di n propylamino tetraline induced increase of serum prolactin levels
    Pharmacological Research, 2000
    Co-Authors: Maria Zhelyazkovasavova, Negrin Negrev
    Abstract:

    Abstract Serotonin, in addition to dopamine and other factors, is known to participate in the control of prolactin (PRL) and gonadotropins secretion. Isoteoline (IST), a putative serotonin antagonist and dopamine agonist, was studied for its neuroendocrine effects on PRL, follicle-stimulating hormone (FSH) and luteinizing hormone (LH). IST was given intraperitoneally to adult male rats at doses of 0.25, 1 and 4 mg kg −1 alone and 30 min prior to the injection of three 5-HT agonists with preferential affinity for various receptor subtypes: meta -chlorophenylpiperazine ( m CPP) for 5-HT2C; 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) for 5-HT2A and 8-hydroxy-2-(di- n -propylamino)tetralin (8-OH-DPAT) for 5-HT1A. m CPP (2.5 mg kg −1 ), DOI (2.5 mg kg −1 ) and 8-OH-DPAT (1 mg kg −1 ) increased the serum PRL levels to a similar value, without affecting FSH and LH concentrations. IST by itself modified neither PRL nor gonadotropins serum levels. IST antagonized the m CPP-induced elevation in serum PRL, the lowest dose being the most effective. It had no effect on DOI and 8-OH-DPAT-induced increases of PRL levels and produced no significant changes in the gonadotropins levels when used as an antagonist. The results are discussed in terms of the likely involvement of serotonin vs dopamine mechanism in the effect of IST. It is concluded that the inhibition of the m CPP-induced rise of PRL levels by IST confirmed the serotonin antagonistic activity, previously demonstrated for this compound in other studies. The present results are also suggestive of possible selectivity of this antagonism of IST for the 5-HT2C vs 5-HT2A and 5-HT1A receptors, all of which are involved in the control of PRL secretion.

Pim De Voogt - One of the best experts on this subject based on the ideXlab platform.

  • Qualitative screening for new psychoactive substances in wastewater collected during a city festival using liquid chromatography coupled to high-resolution mass spectrometry.
    Chemosphere, 2017
    Co-Authors: Ana Causanilles, Juliet Kinyua, Christoph Ruttkies, Alexander L.n. Van Nuijs, Erik Emke, Adrian Covaci, Pim De Voogt
    Abstract:

    The inclusion of new psychoactive substances (NPS) in the wastewater-based epidemiology approach presents challenges, such as the reduced number of users that translates into low concentrations of residues and the limited pharmacokinetics information available, which renders the choice of target biomarker difficult. The sampling during special social settings, the analysis with improved analytical techniques, and data processing with specific workflow to narrow the search, are required approaches for a successful monitoring. This work presents the application of a qualitative screening technique to wastewater samples collected during a city festival, where likely users of recreational substances gather and consequently higher residual concentrations of used NPS are expected. The analysis was performed using liquid chromatography coupled to high-resolution mass spectrometry. Data were processed using an algorithm that involves the extraction of accurate masses (calculated based on molecular formula) of expected m/z from an in-house database containing about 2,000 entries, including NPS and transformation products. We positively identified eight NPS belonging to the classes of synthetic cathinones, phenethylamines and opioids. In addition, the presence of benzodiazepine analogues, classical drugs and other licit substances with potential for abuse was confirmed. The screening workflow based on a database search was useful in the identification of NPS biomarkers in wastewater. The findings highlight the specific classical drugs and low NPS use in the Netherlands. Additionally, Meta-Chlorophenylpiperazine (mCPP), 2,5-dimethoxy-4-bromophenethylamine (2C-B), and 4-fluoroamphetamine (FA) were identified in wastewater for the first time.

  • performance of the linear ion trap orbitrap mass analyzer for qualitative and quantitative analysis of drugs of abuse and relevant metabolites in sewage water
    Analytica Chimica Acta, 2013
    Co-Authors: Lubertus Bijlsma, Erik Emke, Felix Hernandez, Pim De Voogt
    Abstract:

    This work illustrates the potential of liquid chromatography coupled to a hybrid linear ion trap Fourier Transform Orbitrap mass spectrometer for the simultaneous identification and quantification of 24 drugs of abuse and relevant metabolites in sewage water. The developed methodology consisted of automatic solid-phase extraction using Oasis HLB cartridges, chromatographic separation of the targeted drugs, full-scan accurate mass data acquisition under positive electrospray ionization mode over an m/z range of 50-600 Da at a resolution of 30,000 FWHM and simultaneous MSn measurements to obtain information of fragment ions generated in the linear ion trap. Accurate mass of the protonated molecule, together with at least one nominal mass product ion and retention time allowed the confident identification of the compounds detected in these complex matrices. In addition to the highly reliable qualitative analysis, Orbitrap analyzer also proved to have satisfactory potential for quantification at sub-ppb analyte levels, a possibility that has been very little explored in the literature until now. The limits of quantification ranged from 4 to 68 ng L−1 in influent sewage water, and from 2 to 35 ng L−1 in effluent, with the exception of MDA, morphine and THC that presented higher values as a consequence of the high ionization suppression in this type of samples. Satisfactory recoveries (70-120%) and precision (<30%) for the overall procedure were obtained for all compounds with the exception of Meta-Chlorophenylpiperazine, methylphenidate and ketamine. Isotope-labelled internal standards were added to sewage samples as surrogates in order to correct for matrix effects and also for possible losses during sample treatment. The methodology developed was applied to sewage water samples from the Netherlands (influent and effluent), and the results were compared with those obtained by LC-MS/MS with triple quadrupole. Several drugs of abuse could be identified and quantified, mainly MDMA, benzoylecgonine, codeine, oxazepam and temazepam. Orbitrap also showed potential for retrospective investigation of ketamine metabolites in the samples without the need of additional analysis.

Romeu J Daroda - One of the best experts on this subject based on the ideXlab platform.

  • chemical profile of meta chlorophenylpiperazine m cpp in ecstasy tablets by easy ambient sonic spray ionization x ray fluorescence ion mobility mass spectrometry and nmr
    Analytical and Bioanalytical Chemistry, 2011
    Co-Authors: Wanderson Romao, Priscila M Lalli, Marcos Fernando Franco, Gustavo B Sanvido, Nicolas V Schwab, Rafael Lanaro, Jose Luiz Costa, Bruno D Sabino, Maria Izabel M S Bueno, Romeu J Daroda
    Abstract:

    Meta-Chlorophenylpiperazine (m-CPP) is a new illicit drug that has been sold as ecstasy tablets. Easy ambient sonic-spray ionization mass spectrometry (EASI-MS) and X-ray fluorescence spectrometry (XRF) are shown to provide relatively simple and selective screening tools to distinguish m-CPP tablets from tablets containing amphetamines (mainly 3,4-methylenedioxymethamphetamine (MDMA)). EASI-MS detects the active ingredients in their protonated forms: [m-CPP + H]+ of m/z 197, [MDMA + H]+ of m/z 194, and [2MDMA + HCl + H]+ of m/z 423 and other ions from excipients directly on the tablet surface, providing distinct chemical fingerprints. XRF identifies Cl, K, Ca, Fe, and Cu as inorganic ingredients present in the m-CPP tablets. In contrast, higher Cl concentrations and a more diverse set of elements (P, Cl, Ca, Fe, Cu, Zn, Pt, V, Hf, Ti, Pt, and Zr) were found in MDMA tablets. Principal component analysis applied to XRF data arranged samples in three groups: m-CPP tablets (four samples), MDMA tablets (twenty three samples), and tablets with no active ingredients (three samples). The EASI-MS and XRF techniques were also evaluated to quantify m-CPP in ecstasy tablets, with concentrations ranging from 4 to 40 mg of m-CPP per tablets. The m-CPP could only be differentiated from its isomers (o-CPP and for the three isomers p-CPP) by traveling wave ion mobility mass spectrometry and NMR measurements.

Ulderico Freo - One of the best experts on this subject based on the ideXlab platform.

  • chronic treatment with meta chlorophenylpiperazine m cpp alters behavioral and cerebral metabolic responses to the serotonin agonists m cpp and quipazine but not 8 hydroxy 2 di n propylamino tetralin
    Psychopharmacology, 1992
    Co-Authors: Ulderico Freo, Harold W. Holloway, Nigel H Greig, Timothy T. Soncrant
    Abstract:

    The effects of the serotonin (5-HT) agonists Meta-Chlorophenylpiperazine (m-CPP), quipazine and 8-hydroxy-2(di-n-propylamino)tetralin (DPAT) on behavior and on regional cerebral metabolic rates for glucose (rCMRglc) were measured in control rats or in rats pretreated for 2 weeks with continuous infusion of saline or m-CPP (2.5 mg/kg/day, subcutaneously). rCMRglc was measured in 71 brain regions, using the quantitative autoradiographic [14C]2-deoxy-D-glucose technique, at 15 min after acute administration of m-CPP 2.5 mg/kg, 60 min after quipazine 20 mg/kg, or 10 min after DPAT 1 mg/kg. Behavioral effects were assessed for m-CPP with an activity monitor, for quipazine by counting head shakes and for DPAT by scoring the serotonin syndrome. Chronic m-CPP pretreatment produced tolerance to hypolocomotion induced by acute m-CPP and to head shakes caused by acute quipazine, but did not alter the serotonin syndrome produced by DPAT. m-CPP 2.5 mg/kg IP produced widespread rCMRglc reductions in control rats but failed to modify rCMRglc in any region after chronic m-CPP pretreatment. Quipazine increased rCMRglc in 4 regions in control rats, but reduced rCMRglc in 14 brain areas of chronically m-CPP-pretreated animals. DPAT altered rCMRglc to the same degree in control (25 regions affected) and in chronically m-CPP-pretreated rats (28 regions affected). Reduced behavioral and metabolic effects of acute m-CPP in chronically m-CPP-pretreated rats were not due to pharmacokinetic alterations. These results demonstrate that chronic administration of m-CPP produces behavioral and metabolic tolerance to acute administration of m-CPP, but not of DPAT. They suggest that hypolocomotion and the serotonin syndrome are mediated by different 5-HT receptor subtypes, and that chronic m-CPP administration produces functional down-regulation of 5-HT1B/1C but not of 5-HT1A-coupled mechanisms.