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* Respected Journal Articles on Piperazines!!

Discussion in 'Piperazines' started by stjbm06, May 7, 2007.

  1. stjbm06

    stjbm06 Newbie

    Reputation Points:
    Feb 7, 2007
    from U.S.A.
    SWIM wanted to exploit his college's academic journal resource hookup, and hence he went on a little research binge on Piperazines. Did not find too much about the euphoric/beneficial/recreational use other than the common articles sourced on this forum. I didn't search the whole message board forum whether these were posted already, but I'm sure at least a couple are new.

    Enjoy!! And any pharmacological/chemistry/neurology experts feel free to post your comments and ideas!

    Chemistry, pharmacology, toxicology, and hepatic metabolism of designer drugs of the amphetamine (ecstasy), piperazine, and pyrrolidinophenone types - A synopsis
    Author(s): Maurer HH, Kraemer T, Springer D, Staack RF
    Source: THERAPEUTIC DRUG MONITORING 26 (2): 127-131 APR 2004
    Document Type: Article
    Language: English
    Cited References: 42 Times Cited: 16 [​IMG] [​IMG]
    Abstract: Designer drugs of the amphetamine type (eg, MDMA, MDEA, MDA), of the new benzyl or phenyl piperazine type (eg, BZP, MDBP, mCPP, TFMPP, MeOPP), or of the pyrrolidinophenone type (eg, PPP, MOPPP, MDPPP, MPPP, MPHP) have gained popularity and notoriety as rave drugs. These drugs produce feelings of euphoria and energy and a desire to socialize. Although in the corresponding drug scene designer drugs have the reputation of being safe, studies in rats and primates in combination with human epidemiologic investigations indicate potential risks to humans. Thus, a variety of adverse effects have been associated with the use/abuse of this class of drugs in humans, including a life-threatening serotonin syndrome, hepatotoxicity, neurotoxicity, and psychopathology. Metabolites were suspected to contribute to some of the toxic effects. Therefore, knowledge of the metabolism is a prerequisite for toxicologic risk assessment. The metabolic pathways, the involvement of cytochrome P450 isoenzymes in the main pathways, and their roles in hepatic clearance are described for designer drugs of different groups. In summary, polymorphically expressed CYP2D6 was the major enzyme catalyzing the major metabolic steps of the studied piperazineand pyrrolidinophenone-derived designer drugs. However, it cannot be concluded at the moment whether this genetic polymorphism is of clinical relevance.

    Author Keywords: designer drug; ecstasy; piperazine; pyrrolidinophenone; metabolism


    Addresses: Maurer HH (reprint author), Univ Saarland, Inst Expt & Clin Pharmacol & Toxicol, Dept Expt & Clin Toxicol, D-66421 Homburg, Germany
    Univ Saarland, Inst Expt & Clin Pharmacol & Toxicol, Dept Expt & Clin Toxicol, D-66421 Homburg, Germany

    E-mail Addresses: hans.maurer@uniklinik-saarland.de
    Subject Category: Medical Laboratory Technology; Pharmacology & Pharmacy; Toxicology
    IDS Number: 844GW

    ISSN: 0163-4356


    Behavioral responses to intravenous meta-chlorophenyl- piperazine awww.sciencedirect.com_scidirimg_sci_dir_nextterm.gif in patients with seasonal affective disorder and control subjects before and after phototherapy
    Frederick M. Jacobsen M.D. awww.sciencedirect.com_scidirimg_entities_REcor.gif
    Edward A. Mueller M.D.
    Norman E. Rosenthal M.D., Chief
    Susan Rogers R.N., M.S.N.
    James L. Hill Ph.D.
    Dennis L. Murphy M.D., Chief
    Laboratory of Clinical Sceince, National Institute of Mental Health (NIMH), Methesda, MD, USA
    George Washington University School of Medicine and Feorgetown University School of Medicine, Washington, DC, USA
    Rutland Mental Health Center, Rutland, VT, USA
    Section on Environmental Psychiatry, Clinical Psychobiology Branch, NIMH, USA
    Outpatient Studies, Clinical Psychobiology Branch, NIMH, USA
    Biometrics Branch National Institute on Drug Abuse, Bethesda, MD, USA
    Laboratory of Clinical Science, NIMH, USA
    Received 10 June 1993; revised 22 February 1994; accepted 28 March 1994. Available online 24 May 2002.

    A comparison of the baseline and post-infusion effects of the serotonin agonist meta-chlorophenylpiperazine (m-CPP) in 10 patients with seasonal affective disorder (SAD) and 11 healthy control subjects revealed significantly different subjective response profiles between the groups. Several baseline and m-CPP- stimulated responses in symptoms putatively related to serotonergic function changed significantly after a week's exposure to phototherapy in the SAD patients but not the control subjects. Before phototherapy, depressed patients with SAD reported activation- awww.sciencedirect.com_scidirimg_sci_dir_prevterm.gif euphoria awww.sciencedirect.com_scidirimg_sci_dir_nextterm.gif responses to m-CPP and significant decreases in carbohydrate hunger, but insignificant changes in feeling slowed or sleepy, while control subjects reported no mood or appetite changes but significant increases in feeling slowed down following m-CPP. After phototherapy, which led to a significant reduction in baseline depressive symptom ratings to near-euthymic levels in the SAD patients, almost all of the patients' responses to m-CPP were normalized and no longer differed from the control subjects' responses. These results provide evidence of a possible dysregulation in serotonergic neurotransmission in depressed SAD patients that normalizes following treatment with phototherapy.
    Author Keywords: Affective disorder; serotonin; light treatment

    awww.sciencedirect.com_scidirimg_entities_REcor.gif Reprint requests to Dr. F.M. Jacobsen, Laboratory of Clinical Science, NIMH, NIH Clinical Center, 10-3D41, 9000 Rockville Pike, Bethesda, MD 20892, USA.

    Psychiatry Research
    Volume 52, Issue 2, May 1994, Pages 181-197


    PubMed ID: 16669944 PubMed Related Articles Publication Type: Journal Article
    Title: Prevalence of use, epidemiology and toxicity of 'herbal party pills' among those presenting to the emergency department.
    Author(s): Nicholson, Tonia C
    Source: Emerg Med Australas 18 (2) : 180-4 2006 Apr
    Language: English
    Abstract: The aim of the present study was to establish the prevalence of use, epidemiology and toxicity of 'herbal party pills' in ED presenters. This was an analytical cross-sectional survey of patients and relatives presenting to a large tertiary ED. Consenting participants completed a specifically designed questionnaire. A total of 1043 people completed the questionnaire (participation rate of 97.2%). One hundred and twenty-five (11.9%) had taken herbal party pills and subgroup analysis showed that use was most prevalent in those aged 14-25 years (30%). The majority had taken pills between two and five times (56%). Eighty-three (66.4%) had been drinking alcohol when they first took party pills. Only 80 (64%) had read the product directions, and 48 (38.4%) had, at some stage, taken more pills than recommended. One hundred and six (84.8%) had felt effects from party pills, but only 63 (59% of those feeling effects or 50.4% of total) described these as 'good'. Six (5.7% of those with effects or 4.8% of total) had sought medical attention for effects. Seventy-four (59.2%) would take herbal party pills again. In conclusion, the use of herbal party pills is common in presenters to the ED, particularly in those aged 14-25 years. These people are at risk for toxicity from the pills because there is a tendency for them not to read the instructions before ingestion, to take more pills than recommended and to coingest alcohol. Emergency physicians need to be aware of the use and potential adverse effects of herbal party pills to enable them to recognize signs of toxicity in ED presenters and thus provide appropriate supportive care.

    Address: Department of Emergency Medicine, Waikato Hospital, Hamilton, New Zealand. nicholst@waikatodhb.govt.nz


    ==The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.== Department of Environmental Health and Toxicology, Tokyo Metropolitan Institute of Public Health, 24-1 Hyakunin-cho 3-chome, Shinjuku-ku, Tokyo, 169-0073 Japan. Fumiko_Nagai@member.metro.tokyo.jp

    We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. Alpha-metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-alpha-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines. N,N-dipropyltryptamine (DPT), 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-N,N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.

    PMID: 17223101 [PubMed - in process]


    ==Methylone and mCPP, two new drugs of abuse?== Drugs Information and Monitoring System (DIMS), Trimbos Institute for Mental Health and Addiction, Utrecht, the Netherlands. mbossong@trimbos.nl

    Recently, two new ecstasy-like substances, methylone and mCPP, were found in street drugs in the Netherlands by the Drugs Information and Monitoring System (DIMS). Methylone (3,4-methylenedioxymethcathinone) is the main ingredient of a new liquid designer drug that appeared on the Dutch drug market, called 'Explosion'. mCPP (meta-chlorophenylpiperazine) is a substance often used as a probe for the serotonin function in psychiatric research, and has now been found in street drugs, both in tablets and powders. Methylone as well as mCPP act on monoaminergic systems, resembling MDMA (3,4-methylenedioxymethamphetamine), with mCPP mainly affecting the serotonin system. The subjective effects of both new substances exhibit subtle differences with those of MDMA. Only little is known about the harmfulness of both methylone and mCPP. However, because of similarities between these substances and MDMA, risks common to MDMA cannot be excluded.


    The role of neurotransmitters and neurohormones in obsessive-compulsive disorder. By: Greenberg, Benjamin D.; Altemus, Margaret; Murphy, Dennis L.. International Review of Psychiatry, Mar97, Vol. 9 Issue 1, p31-44, 14p Abstract: There is considerable evidence that serotonergic systems modulate obsessive-compulsive disorder (OCD) symptomatology. The strongest such data are the antiobsessional effects of serotonin reuptake inhibitors (SRIs), unique among antidepressants. Although the mechanisms underlying the effectiveness of SRI treatment remain largely unknown, the available data support the position that enhanced 5-HT synaptic availability, resulting from a combination of effects on serotonin release and transport, is necessary for the therapeutic efficacy of SRI treatment. The ability of the serotonergic probe mCPP to exacerbate OCD symptoms in untreated patients, and findings that potent 5-HT receptor antagonists may reverse SRI-induced therapeutic benefits, also support serotonergic modulation of OCD symptomatology. There is as yet little evidence that dysregulation in serotonergic systems might be etiologically important in OCD. Although evidence that other neurotransmitter or neuropeptide systems are involved in OCD is considerably more preliminary than that implicating serotonergic mechanisms, there are some indications that such systems may be involved. Studies of the role of these systems, and how they may interact with serotonergic mechanisms, may be particularly helpful in further elucidating the neuropharmacology of OCD and in identifying potential new treatments. [ABSTRACT FROM AUTHOR]; DOI: 10.1080/09540269775574; (AN 9707012969)


  2. stjbm06

    stjbm06 Newbie

    Reputation Points:
    Feb 7, 2007
    from U.S.A.
    1: Forensic Sci Int. 2001 Sep 15;121(1-2):47-56.[​IMG] Links
    ==Piperazine-like compounds: a new group of designer drugs-of-abuse on the European market.== Instituto Nacional do Desporto, Laboratorio de Analises de Dopagem e Bioquimica, Av. Prof. Egas Moniz (Estadio Universitario), 1600-190 Lisbon, Portugal.

    1-Aryl-piperazine compounds are, depending on their substituents, selective for certain serotonin receptors and together with their easy availability and their so-called legal status, this group of psychoactive compounds are potential designer drugs-of-abuse. Internet in that respect is an important source of information and distribution facilities. Because this development may have consequences for the interpretation of future clinical and forensic toxicological case studies, some analytical aspects of 1-benzyl-piperazine (BZP), 1-[4-methoxyphenyl]-piperazine (pMeOPP) and 1-[3-trifluoromethylphenyl]-piperazine (TFMPP) were studied. BZP was not detected by the AxSYM FPIA technology designed to determine amphetamine-like compounds, but had showed some cross reactivity with EMIT d.a.u.. The cross reactivities at 300 and 12,000ng/ml (RS)-amphetamine equivalents were 0.4 and 1.3%, respectively. Although BZP was not identified directly by the REMEDi HS Drug Profiling System, it can be detected by this HPLC/UV scanning system. Using GC/NPD without derivatisation, BZP, pMeOPP and TFMPP can be analysed for and applying GC/MS without or with acetylation or trifluoroacetylation, these compounds can be identified unambiguously. The usefulness of GC/NPD and GC/MS in this respect was demonstrated by the quantitative and qualitative analysis of the content of a capsule with the synthetic stimulant A2, which proved to contain 86.4mg of BZP.

    PMID: 11516887 [PubMed - indexed for MEDLINE]
  3. Bajeda

    Bajeda Super Moderator Platinum Member & Advisor Supporter

    Reputation Points:
    Jul 13, 2006
    from U.S.A.
    If you could get the full-text pdfs for these and upload them to the appropriate section of the file archive that would be helpful, thanks.
  4. Jatelka

    Jatelka Psychedelic Shepherdess Platinum Member & Advisor

    Reputation Points:
    Oct 16, 2005
    from U.K.
    The first one is definately in the archive already