Piperazines.. research chems??

Discussion in 'Piperazines' started by androoo, Mar 11, 2006.

  1. androoo

    androoo Newbie

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  2. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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    Because they are chemicals which have a very short history of use and their effects have not been fully determined. Why do you not class the as RCs? Is it because they are available in a nice package in your local head shop?
     
  3. Nagognog2

    Nagognog2 Iridium Member

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    Or perhaps you know someone who is importing these and you have a vested interest in people thinking they are safe?
     
  4. androoo

    androoo Newbie

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    Mr Paranoia ;)

    As far as i know they have been around quite a while (BZP was synthesised in '73).. and have been tested/researched.
     
  5. androoo

    androoo Newbie

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  6. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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    Most Research Chemicals have been around quite a while, the main research I have seen on piperizines is into their use as a worming agent in cattle.
     
    Last edited: Mar 11, 2006
  7. androoo

    androoo Newbie

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  8. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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  9. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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    Having them labled as anything else gives a false impression of their safety, or lack thereof IMO.
     
  10. androoo

    androoo Newbie

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    why does erowid.org not consider these chemicals to be research chemicals then?
     
  11. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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    Erowid is not infallible believe it or not. There are actually many inaccuracies in Erowid if you look for them. By the definition given in the FAQ you linked to they should be classed as an RC.
     
  12. androoo

    androoo Newbie

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    i understand that.. but they are one of the most accurate sources of information on the net when it comes to drugs.
    so why are they classed as research chemicals here?
    is it worth emailing erowid.org to point out their mistake?
     
  13. Nagognog2

    Nagognog2 Iridium Member

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    The decision to regard piperazines as RC's is based on the lack of knowledge regarding their long-term effects on people. What erowid does is what erowid does. We consider them RC's due to the lack of established knowledge. End of story.

    Just because some unscrupulous people choose to buy a barrel of piperazines from a chemical plant in China, slap a misleading label on them claiming they are just like MDMA, and put them on the shelf in some head-shop - does not make them safe. If you wish to play Russian Roulette with your body, that is your choice. But do not make claims regarding their safety on this forum. We take a dismal view of people making claims that cannot be backed up.
     
  14. Alfa

    Alfa Productive Insomniac Staff Member Administrator

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    Androoo, your question is if piperazines have been researched well on humans. First of all piperazines are a class of chemicals, containing an unkown amount of substances. Many of them have never been synthesized at all. Viagra is a piperazine of which the effects on humans has been researched, which excludes it as a RC. Several piperazines have a long history as pesticides. XTC tabs containing MCPP have caused a lot of health problems worldwide. Not much is know about the pharmacology of MCPP.

    The piperazines used in legal highs, include Flipperazine. I have been researching this substance, but could not find more then some vague data. The best data I could find about it was from user experience. So, considering this: how can you not classify this as research chemicals?
    Is there something I have missed? You are most certain that piperazines are well researched for human use. You post this in multiple topics. I can only assume that you have this research in possession.

    So, I dare you; please post these invaluable clinical trials on human pharmacology & toxicity here, so we can be pursuaded to your argument and exclude bzp, tfmpp, pfpp & mcpp from the title research chemicals.
     
    Last edited: Mar 12, 2006
  15. Abrad

    Abrad R.I.P. Platinum Member & Advisor R.I.P.

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  16. androoo

    androoo Newbie

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    ok.. i accept that i may have gotten this one wrong ;)
    i can't find as much research as i thought i'd find..

    I'll be doing my own research with Jax on sat night.. 150mg BZP & 75mg TFMPP.. do we have to use the SWIM thing even if its a legal chemical and its blatently obvious that its me i'm talking about?
     
  17. radiometer

    radiometer bananadine addict Platinum Member & Advisor

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    post deleted by radiometer
     
    Last edited: Mar 17, 2006
  18. Jackyl

    Jackyl Titanium Member

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    mCPP human studies

    Here you are:

    Pharmacokinetic and pharmacodynamic profile of oral and intravenous meta-chlorophenylpiperazine in healthy volunteers.

    Gijsman HJ, Van Gerven JM, Tieleman MC, Schoemaker RC, Pieters MS, Ferrari MD, Cohen AF, Van Kempen GM.

    Department of Psychiatry, Centre for Human Drug Research, Leiden University Medical Centre, The Netherlands.

    meta-Chlorophenylpiperazine (mCPP) is a compound that is frequently used in challenge tests of the serotonergic system. Its human pharmacology is largely unexplored. The objective of this study was to investigate the pharmacokinetic and pharmacodynamic profile of mCPP. Eight female and six male healthy volunteers were included in a randomized, double-blind, double-dummy, three-way crossover design of single-dose intravenous (0.1 mg/kg), oral (0.5 mg/kg), and placebo treatment, with 24-hour follow-up. mCPP showed a large variability in clearance (11-92 mL/hr) and bioavailability (14-108%). Two female subjects dropped out because of headache and dysphoria. During the 27 occasions in which mCPP was administered, autonomic physical symptoms were observed in 23 subjects and disturbances of mood in 6 subjects. Oral and intravenous mCPP caused sudden increases in cortisol levels, prolactin levels, and total scores of the Body Sensation Questionnaire. Administration of mCPP also led to concentration-dependent increases of saccadic peak velocity and adaptive tracking performance and to a decrease of electroencephalographic occipital theta activity. No clinically relevant effects on electrocardiogram, temperature, and blood pressure were found. In conclusion, it is doubtful whether mCPP is a useful compound for challenge tests in view of the large pharmacokinetic variability after intravenous and oral administration. The effects of mCPP are consistent with disinhibition of the central nervous system.


    Psychopharmacology (Berl). 1990;100(3):339-44. Links
    Effects of m-chlorophenylpiperazine in normal subjects: a dose-response study.Kahn RS, Wetzler S, Asnis GM, Kling MA, Suckow RF, van Praag HM.
    Department of Psychiatry, Albert Einstein College of Medicine, Montefiore Medical Center, New York, NY 10467.

    m-Chlorophenylpiperazine (MCPP), a direct 5HT receptor agonist, was administered orally to 20 normal subjects in two doses (0.25 and 0.5 mg/kg) in a placebo-controlled design. Behavioral responses; ACTH, cortisol, prolactin and MCPP blood level; temperature and pulse rate were measured over a 210-min period after administration of tablets. Non-linear dose-response relationships between MCPP and ACTH, cortisol and prolactin response were found. On the higher dose, a significant increase in the number of physical symptoms was also noted and three subjects (15%) had a panic attack, while one subject (5%) had a panic attack on the lower dose. No effects on other behavioral variables, pulse rate and temperature were found using either dose. These findings attest to the usefulness of MCPP as a challenge agent to assess 5HT receptor hypersensitivity when given at a low oral dose (i.e. around 0.25 mg/kg), and to assess 5HT receptor hyposensitivity when given at higher oral doses (i.e. around 0.5 mg/kg).

    Psychiatry Res. 1990 Aug;33(2):189-98. Links
    Effects of serotonin antagonists on m-chlorophenylpiperazine-mediated responses in normal subjects.Kahn RS, Kalus O, Wetzler S, Cahn W, Asnis GM, van Praag HM.
    Department of Psychiatry, Montefiore Medical Center/Albert Einstein College of Medicine, Bronx, NY.

    The serotonin (5HT) agonist, m-chlorophenylpiperazine (MCPP), has been used as a challenge agent to assess central 5HT receptor sensitivity in normal subjects and patients with panic disorder, obsessive-compulsive disorder, and major depression. Adrenocorticotropin, cortisol, and prolactin responses to MCPP were among the variables measured. MCPP's usefulness as a probe of 5HT receptors, however, hinges on its 5HT selectivity. To address MCPP's selectivity for 5HT, this study tested whether two different 5HT antagonists, methysergide (4 mg p.o.) and metergoline (4 mg p.o.), could block the hormonal and behavioral effects of MCPP (0.5 mg/kg p.o.) in 10 normal male subjects in comparison to placebo. Both 5HT antagonists abolished the prolactin release to MCPP. Metergoline, the antagonist with the more potent 5HT binding affinity, significantly blocked MCPP's effect on cortisol release as compared to placebo, and methysergide showed a nonsignificant trend to that effect. MCPP alone did not have a significant effect on behavioral variables, perhaps explaining why neither 5HT antagonist affected these measures. The findings from this study suggest that both MCPP-induced prolactin release and cortisol release are indeed 5HT-mediated effects.

    Psychopharmacology (Berl). 1992;106(3):388-90. Links
    A dose-response study of intravenous m-chlorophenylpiperazine in normal subjects.Kalus O, Wetzler S, Kahn RS, Asnis GM, van Praag HM.
    Department of Psychiatry, Albert Einstein College of Medicine, Montefiore Medical Center, Bronx, NY.

    A placebo-controlled dose-response study of the direct serotonin receptor agonist m-chlorophenylpiperazine (MCPP), intravenously infused over 90 s in 0.06 and 0.08 mg/kg doses, was conducted in nine normal male subjects. Cortisol, prolactin, MCPP serum levels and behavioral responses were measured over a 210-min period. Both doses caused significant cortisol and prolactin release and were associated with significantly greater behavioral effects as compared to placebo. Though the two doses were associated with different MCPP serum levels, they did not significantly differ in their hormonal and behavioral effects.


    The application of the principles of clinical drug development to pharmacological challenge tests of the serotonergic system.

    J Psychopharmacol. 2004 Mar;18(1):7-13.

    Gijsman HJ, Cohen AF, van Gerven JM.
    South London and Maudsley NHS Trust, London, UK. [email protected]

    Pharmacological challenge tests of the serotonergic system have extensively been used during the past 20 years and new tests are in development. It is of crucial importance to standardize challenge tests to ascertain that observed variability is due to the state of the challenged system and not caused by variability of the test itself. This is even more important now that challenge tests increasingly are used in complex studies (e.g. in combination with neuroimaging and in large population studies with repeated tests over time). The Guideline for Good Clinical Practice may be of great help in the standardization of these tests. This is a recently developed guideline for pharmaceutical drug-development, which increasingly is used as a reference for all research in humans. To exemplify the possible usefulness of this approach, we apply it to meta-chlorophenylpiperazine, one of the most commonly used drugs in serotonergic challenge tests. We conclude that much can be learned from the development of this particular challenge. In the discussion, we address general issues that emerged from this review and their relevance to the development of future challenge tests.

    Addict Biol. 2005 Dec;10(4):321-3. Links
    Methylone and mCPP, two new drugs of abuse?Bossong MG, Van Dijk JP, Niesink RJ.
    Drugs Information and Monitoring System (DIMS), Trimbos Institute for Mental Health and Addiction, Utrecht, the Netherlands. [email protected]

    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.

    Drug Alcohol Depend. 2001 Dec 1;65(1):97-101. Links
    The subjective effects of MDMA and mCPP in moderate MDMA users.Tancer ME, Johanson CE.
    Substance Abuse Research Division, Department of Psychiatry and Behavioral Neurosciences, Wayne State University School of Medicine, Detroit, MI 48207, USA. [email protected]

    The present study is part of a research program designed to better understand the neurochemical mechanisms underlying the abuse liability of 3,4-methylenedioxymethamphetamine (MDMA) in humans. In these studies, MDMA will be compared to prototypical dopamine (D-amphetamine) and serotonin (meta-chlorophenylpiperazine, mCPP) releasing agents on a variety of measures related to dependence. In order to determine an acceptable dose range (safe but active) of MDMA and mCPP for these studies, moderate MDMA users were administered escalating doses of MDMA (75, 110 and 145 mg/70 kg) and mCPP (17.5, 35 and 52.5 mg/70 kg). Each participant received a single dose under controlled laboratory conditions, i.e. this was a six-group design with a separate group for each dose. There were five participants tested in each group. MDMA increased blood pressure and heart rate whereas mCPP had no effect on these physiological measures. MDMA produced increases in subjective effects indicative of both stimulant (increases in POMS Elation, ARCI Amphetamine, VAS High and Stimulated scale scores) and hallucinogenic effects (increases on five of the six scales of the Hallucinogenic Rating Scale). mCPP produced similar stimulant effects (e.g. increases on POMS Elation, VAS High and Stimulated), as well as hallucinogenic effects (four of the six scales of the Hallucinogenic Rating Scale), which has not been observed in previous studies.
    See: https://drugs-forum.com/forum/local_links.php?action=jump&id=509&catid=33


    Drug Alcohol Depend. 2006 Jan 4;81(1):27-36. Epub 2005 Jun 21. Links
    Discriminative stimulus effects of 3,4-methylenedioxymethamphetamine (MDMA) in humans trained to discriminate among d-amphetamine, meta-chlorophenylpiperazine and placebo.Johanson CE, Kilbey M, Gatchalian K, Tancer M.
    Department of Psychiatry and Behavioral Neurosciences, Wayne State University, Drug Abuse Research Division, 2761 East Jefferson, Detroit, MI 48207, USA. [email protected]

    In animals, two-choice drug discrimination studies have demonstrated that the behavioral effects of 3,4-methylenedioxymethamphetamine (MDMA) are mediated by dopaminergic and serotonergic systems. In order to delineate the relative role of these systems, three-choice paradigms have been used in animals, with findings indicating a more prominent role for serotonin. Human studies assessing the subjective and physiological effects of MDMA have also indicated a mixed action. To parallel animal studies, the participants in the present study were trained to discriminate among a prototypic dopaminergic agonist, d-amphetamine, a prototypic serotonergic agonist, meta-chlorophenylpiperazine (mCPP) and placebo and then were tested with two doses of MDMA. In addition, subjective and physiological effects were measured. The results demonstrated that humans could be trained to discriminate among 20 mg d-amphetamine, 0.75 mg/kg mCPP and placebo. When tested with 1.0 and 1.5 mg/kg, half the participants reported MDMA to be like amphetamine and half like mCPP. There were no clear differences between these two groups in other dimensions, although there was an indication that the individuals who discriminated MDMA as d-amphetamine were more sensitive to the effects of all the drugs. The subjective effects of all three drugs overlapped, although the effects of MDMA appeared more amphetamine-like.

    Ther Drug Monit. 2004 Apr;26(2):127-31. Links
    Chemistry, pharmacology, toxicology, and hepatic metabolism of designer drugs of the amphetamine (ecstasy), piperazine, and pyrrolidinophenone types: a synopsis.Maurer HH, Kraemer T, Springer D, Staack RF.
    Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D-66421 Homburg (Saar), Germany. [email protected]

    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 piperazine- and pyrrolidinophenone-derived designer drugs. However, it cannot be concluded at the moment whether this genetic polymorphism is of clinical relevance.

    Drug Alcohol Depend. 2003 Oct 24;72(1):33-44. Links
    Reinforcing, subjective, and physiological effects of MDMA in humans: a comparison with d-amphetamine and mCPP.Tancer M, Johanson CE.
    Department of Psychiatry and Behavioral Neurosciences, Substance Abuse Research Division, Addiction Research Institute, Wayne State University, 2761 E Jefferson, Detroit, MI 48207, USA. [email protected]

    3,4-methylenedioxymethamphetamine (MDMA) is a widely used drug of abuse chemically related to both the amphetamines and mescaline. Laboratory animal studies have shown that MDMA is a potent re-uptake inhibitor and releaser of dopamine and serotonin. Although the subjective and physiological effects of MDMA have been compared to d-amphetamine in humans, no direct comparison with a serotonin releasing agent has been reported and reinforcing effects have not been evaluated. In this paper we report a direct comparison of the reinforcing, subjective, and physiological effects of MDMA (1 and 2 mg/kg) to d-amphetamine (10 and 20 mg), to metachlorophenylpiperazine (mCPP--a serotonin releasing agent (0.5 and 0.75 mg/kg)), and to placebo using a within-subject design in 12 volunteers with moderate MDMA experience. Both the high dose of d-amphetamine and MDMA showed significant reinforcing effects as indicated by high cross-over values on the multiple choice procedure compared to all other treatments. All three drugs showed dose-dependent changes in subjective effects whereas physiological effects were most pronounced for MDMA with almost no changes seen with mCPP. The subjective effects of MDMA were similar both to those of mCPP and d-amphetamine, suggesting that both dopamine and serotonin systems are involved in mediating these effects. In contrast, only the dopaminergic agents, d-amphetamine and MDMA, had reinforcing effects.

    Psychopharmacology (Berl). 1999 Nov;147(1):56-65. Links
    Altered neuroendocrine and behavioral responses to m-chlorophenylpiperazine in 3,4-methylenedioxymethamphetamine (MDMA) users.McCann UD, Eligulashvili V, Mertl M, Murphy DL, Ricaurte GA.
    Biological Psychiatry Branch, National Institute of Mental Health, Bethesda, MD 20892-1272, USA. [email protected]

    RATIONALE: (+/-) 3,4-Methylenedioxymethamphetamine (MDMA, "Ecstasy") is a popular drug of abuse and a brain serotonin neurotoxin in animals. Growing evidence indicates that humans are also susceptible to MDMA's neurotoxic effects, although few functional consequences of MDMA-induced 5-HT damage have been identified. OBJECTIVE: The present study sought to determine whether possible differences between MDMA users and control subjects could be unmasked by utilizing a pharmacological challenge with the mixed 5-HT agonist, meta-chlorophenylpiperazine (m-CPP). It was postulated that 5-HT neurotoxicity in MDMA users would be associated with altered 5-HT responsivity, exemplified by altered physiological and behavioral responses to m-CPP. METHODS: Twenty-five MDMA users who had not taken MDMA for at least 3 weeks and 25 controls received intravenous placebo (normal saline) and m-CPP (0.08 mg/kg) in a fixed order, single blind design. Repeated measures of mood, physical symptoms, and blood samples for neuroendocrine analyses were collected during the 90 min after each infusion. RESULTS: MDMA users reported more positive and fewer negative emotions and physical symptoms following m-CPP than controls, and were significantly less likely to report an m-CPP-induced panic attack. Male MDMA users had diminished cortisol and prolactin responses to m-CPP. CONCLUSIONS: The present data indicate that MDMA users have alterations in 5-HT neuronal function, possibly as a consequence of MDMA-induced brain serotonin neural injury.



    Biol Psychiatry. 1992 Dec 1;32(11):1055-61. Links
    Effect of m-chlorophenylpiperazine on plasma homovanillic acid concentrations in healthy subjects.Kahn RS, Knott P, Gabriel S, DuMont K, Mastroianni L, Davidson M.
    Department of Psychiatry, Mount Sinai School of Medicine, Bronx Veterans Administration Hospital, Bronx, New York.

    In view of the abundant anatomical and functional interactions between serotonin and dopamine systems, this study examined the effect of the serotonin agonist, m-chlorophenylpiperazine (mCPP) on plasma concentrations of the dopamine metabolite, homovanillic acid. Plasma prolactin levels, body temperature, and mCPP blood level were also measured. mCPP (0.35 mg/kg) and placebo were administered orally to 10 healthy men in a randomized double-blind design. Variables were measured for 210 min after administration of capsules. mCPP raised prolactin and temperature as compared to placebo, but did not affect plasma homovanillic acid concentrations. Results suggest that mCPP does not alter dopamine function.

    Psychiatry Res. 1992 Jul;43(1):1-12. Links
    Serotonin function in schizophrenia: effects of meta-chlorophenylpiperazine in schizophrenic patients and healthy subjects.Kahn RS, Siever LJ, Gabriel S, Amin F, Stern RG, DuMont K, Apter S, Davidson M.
    Clinical Research Unit, Bronx Veterans Administration Hospital, NY 10468.

    This study examined serotonin (5-hydroxytryptamine; 5HT) receptor responsivity in 22 chronic schizophrenic patients and 17 healthy control subjects. The 5HT agonist meta-chlorophenylpiperazine (MCPP) was used as a probe of serotonergic function. MCPP (0.35 mg/kg) or placebo was administered orally after a 3-week drug-free period in a randomized double-blind design. Hormonal (adrenocorticotropic hormone and prolactin), temperature, and behavioral responses and MCPP blood levels were assessed for 210 minutes after administration of the capsules. The schizophrenic patients had blunted temperature responses compared with those of the healthy control subjects: MCPP raised body temperature in the control subjects, but not in the patients. Behavioral responses also differed in the two groups: MCPP increased the total Brief Psychiatric Rating Scale (BPRS) score in the control subjects and tended to decrease it in the patients. In patients, MCPP decreased the BPRS psychosis subscore. Hormonal responses did not differ significantly in the two groups. These findings suggest that further exploration of 5HT function in schizophrenia is warranted.

    Psychiatry Res. 1996 Oct 16;64(3):147-59. Links
    Effects of meta-chlorophenylpiperazine on neuroendocrine and behavioral responses in male schizophrenic patients and normal volunteers.Maes M, Meltzer HY.
    Clinical Research Center for Mental Health, University Department of Psychiatry, Antwerp, Belgium.

    Functional alterations in the central serotonergic system, including presynaptic and postsynaptic function, have been reported in schizophrenia. Recently, there have been conflicting reports that the increase in plasma cortisol or prolactin concentrations induced by meta-chlorophenylpiperazine (mCPP) was significantly blunted in schizophrenic patients compared with normal volunteers. Studies of the behavioral effects of mCPP, a serotonin (5-HT) receptor partial agonist with high affinity for 5-HT1C binding sites, have also yielded conflicting results in schizophrenic patients. The purpose of this study was to examine plasma levels of prolactin and cortisol, body temperature, and behavioral responses to mCPP and placebo in a single-blind study in 25 schizophrenic and 15 normal men. No differences either between schizophrenic patients and normal volunteers or between paranoid and undifferentiated/residual subtypes of schizophrenia were found in mCPP-induced prolactin, cortisol, or temperature responses. Schizophrenic patients and normal volunteers reported significant increases in feeling calm and feeling strange of comparable magnitude following mCPP. No significant differences between normal volunteers and schizophrenic patients were found in post-mCPP behavioral ratings, such as anxiety, irritability, depression, restlessness, or arousal.

    Am J Psychiatry. 1994 Nov;151(11):1626-30. Links
    Comment in:
    Am J Psychiatry. 1995 Dec;152(12):1833-4; author reply 1834-5.
    Am J Psychiatry. 1995 Dec;152(12):1834; author reply 1834-5.
    Neuroendocrine and behavioral responses to intravenous m-chlorophenylpiperazine (mCPP) in depressed patients and healthy comparison subjects.Anand A, Charney DS, Delgado PL, McDougle CJ, Heninger GR, Price LH.
    Clinical Neuroscience Research Unit, Connecticut Mental Health Center, New Haven.

    OBJECTIVE: This double-blind study was undertaken to compare central serotonergic function in depressed patients and healthy comparison subjects by examining neuroendocrine and mood responses to intravenous infusion of the serotonin agonist m-chlorophenylpiperazine (mCPP). METHOD: The participants were 20 drug-free patients with DSM-III-R major depression and 18 healty comparison subjects. After an overnight fast, the subjects received an intravenous infusion of mCPP, 0.1 mg/kg, or placebo saline. Blood was obtained for measurement of serum prolactin, growth hormone (GH), and cortisol. Visual analogue scales were used to assess mood. RESULTS: The depressed patients had a blunted GH response and felt less drowsy than the comparison subjects; prolactin, cortisol, and the remaining behavioral ratings showed no differences between the two groups. CONCLUSIONS: In light of findings with other provocative agents, the blunted GH response to mCPP may reflect a defect in GH production in depression and could be a marker of the depressed state. The lack of differences in the other neuroendocrine variables suggests that the functioning of postsynaptic serotonergic receptors responsive to mCPP may be relatively intact in depression.

    Neuropsychopharmacology. 1997 Nov;17(5):342-50. Links
    Neurobiology of tryptophan depletion in depression: effects of m-chlorophenylpiperazine (mCPP).Price LH, Malison RT, McDougle CJ, McCance-Katz EF, Owen KR, Heninger GR.
    Butler Hospital, Department of Psychiatry and Human Behavior, Brown University School of Medicine, Providence, Rhode Island 02906, USA.

    This study utilized neuroendocrine and mood responses to intravenous (i.v.) infusion of the serotonin (5-HT) agonist m-chlorophenylpiperazine (mCPP) to evaluate central 5-HT function in depressed patients undergoing acute tryptophan (TRP) depletion. Twenty-two drug-free patients with DSM-III-R major depression participated. Each patient underwent two randomized, double-blind TRP depletion tests, one sham and one active. At the estimated time of maximum TRP depletion, each patient received an i.v. infusion of mCPP 0.1 mg/kg. Blood was obtained for serum cortisol, prolactin, and growth hormone. Multiple rating scales were used to assess mood. The cortisol response to i.v. mCPP was significantly greater during TRP depletion than during sham depletion, and free plasma TRP was negatively correlated with the cortisol response during TRP depletion. These findings are consistent with the hypothesis that acute TRP depletion in drug-free depressed patients induces a compensatory up-regulation of postsynaptic 5-HT receptors, most likely of the 5-HT2A/2C subtype. Such changes suggest a mechanism by which acute and potent manipulations of 5-HT function in depressed patients could be used to effect rapid clinical improvement.

    More references

    Smith, K. A., A. D. Oldman, et al. (1994). “Effects of meta-chlorophenylpiperazine on neuroendocrine responses and food intake in healthy female volunteers.” Journal of Serotonin Research 1: 127-132.

    Silverstone, P. H. and P. J. Cowen (1994). “The 5-HT3 antagonist BRL 46470 does not attenuate m-chlorophenylpiperazine (mCPP)-induced changes in human volunteers.” Biological Psychiatry 36: 309-316.

    Silverstone, P. H., J. E. Rue, et al. (1994). “The effects of administration of mCPP on psychological, cognitive, cardiovascular, hormonal and MHPG measurements in human volunteers.” International Clinical Psychopharmacology 9: 173-178.

    Walsh, A. E. S., K. A. Smith, et al. (1994). “m-Chlorophenylpiperazine decreases food intake in a test meal.” Psychopharmacology 116: 120-122.

    Hormonal and Subjective Responses to Intravenous m-Chlorophenylpiperazine in Women...
    Levitan et al.
    Arch Gen Psychiatry.1998; 55: 244-249.

    And there is more, much more, on mCPP in scientific literature.
     
    Last edited: Sep 7, 2006
  19. radiometer

    radiometer bananadine addict Platinum Member & Advisor

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    Apr 13, 2005
    from U.S.A.
    They have? Where?
     
  20. Jackyl

    Jackyl Titanium Member

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    Mar 8, 2005
    from virgin_islands
    That´s probably Germany.