English Journal

Drug effects on multiple and concurrent schedules of ethanol- and food-maintained behavior: context dependent selectivity.

Ginsburg BC1, Lamb RJ.Author information 1The University of Texas Health Science Center at San Antonio, Departments of Psychiatry and Pharmacology, 7703 Floyd Curl Dr. , San Antonio, TX 78229.AbstractBACKGROUND AND PURPOSE: Drugs that more potently or effectively reduce ethanol-maintained behavior versus an alternative are considered selective and are considered promising pharmacotherapies for alcoholism. Such results are often obtained using separate groups or multiple schedules where ethanol and the alternative are available alone or sequentially. Recently, we observed that when ethanol and food were available sequentially under a multiple schedule, fluvoxamine and varenicline were selective; yet this selectivity disappeared when ethanol and food were concurrently available.
British journal of pharmacology.Br J Pharmacol.2014 Apr 4. doi: 10.1111/bph.12707. [Epub ahead of print]
BACKGROUND AND PURPOSE: Drugs that more potently or effectively reduce ethanol-maintained behavior versus an alternative are considered selective and are considered promising pharmacotherapies for alcoholism. Such results are often obtained using separate groups or multiple schedules where ethanol a
PMID 24697498

Pharmacological profiles of aminoindanes, piperazines, and pipradrol derivatives.

Simmler LD1, Rickli A1, Schramm Y2, Hoener MC3, Liechti ME4.Author information 1Psychopharmacology Research, Division of Clinical Pharmacology and Toxicology, Department of Biomedicine, University Hospital Basel and University of Basel, Basel, Switzerland.2Department of Chemistry, University of Basel, Basel, Switzerland.3Neuroscience Research, Pharmaceuticals Division, F. Hoffmann-La Roche Ltd, Basel, Switzerland.4Psychopharmacology Research, Division of Clinical Pharmacology and Toxicology, Department of Biomedicine, University Hospital Basel and University of Basel, Basel, Switzerland. Electronic address: matthias.liechti@usb.ch.AbstractAminoindanes, piperazines, and pipradrol derivatives are novel psychoactive substances found in "Ecstasy" tablets as replacements for 3,4-methylenedioxymethamphetamine (MDMA) or substances sold as "ivory wave." The pharmacology of these MDMA- and methylphenidate-like substances is poorly known. We characterized the pharmacology of the aminoindanes 5,6-methylenedioxy-2-aminoindane (MDAI), 5-iodoaminoindane (5-IAI), and 2-aminoindane (2-AI), the piperazines meta-chlorophenylpiperazine (m-CPP), trifluoromethylphenylpiperazine (TFMPP), and 1-benzylpiperazine (BZP), and the pipradrol derivatives desoxypipradrol (2-diphenylmethylpiperidine [2-DPMP]), diphenylprolinol (diphenyl-2-pyrrolidinemethanol [D2PM]), and methylphenidate. We investigated norepinephrine (NE), dopamine (DA), and serotonin (5-hydroxytryptamine [5-HT]) uptake inhibition using human embryonic kidney 293 (HEK 293) cells that express the respective human monoamine transporters (NET, DAT, and SERT). We also evaluated the drug-induced efflux of NE, DA, and 5-HT from monoamine-preloaded cells and the binding affinity to monoamine transporters and receptors, including trace amine-associated receptor 1 (TAAR1). 5-IAI and MDAI preferentially inhibited the SERT and NET and released 5-HT. 2-AI interacted with the NET. BZP blocked the NET and released DA. m-CPP and TFMPP interacted with the SERT and serotonergic receptors. The pipradrol derivatives were potent and selective catecholamine transporter blockers without substrate releasing properties. BZP, D2PM, and 2-DPMP lacked serotonergic activity and TAAR1 binding, in contrast to the aminoindanes and phenylpiperazines. In summary, all of the substances were monoamine transporter inhibitors, but marked differences were found in their DAT vs. SERT inhibition profiles, release properties, and receptor interactions. The pharmacological profiles of D2PM and 2-DPMP likely predict a high abuse liability.
Biochemical pharmacology.Biochem Pharmacol.2014 Mar 15;88(2):237-44. doi: 10.1016/j.bcp.2014.01.024. Epub 2014 Jan 28.
Aminoindanes, piperazines, and pipradrol derivatives are novel psychoactive substances found in "Ecstasy" tablets as replacements for 3,4-methylenedioxymethamphetamine (MDMA) or substances sold as "ivory wave." The pharmacology of these MDMA- and methylphenidate-like substances is poorly known. We c
PMID 24486525

Anxiety-like effects of meta-chlorophenylpiperazine in paradoxically sleep-deprived mice.

Polesel DN1, Fukushiro DF2, Andersen ML3, Nozoe KT4, Mári-Kawamoto E2, Saito LP2, Carvalho FR5, Alvarenga TA4, Freitas D5, Tufik S4, Frussa-Filho R6, Lanaro R7, Costa JL8, Tavares MF9.Author information 1Departamento de Toxicologia e Análises Toxicológicas, Universidade de São Paulo, Brazil.2Departamento de Farmacologia, Universidade Federal de São Paulo, Brazil.3Departamento de Psicobiologia, Universidade Federal de São Paulo, Brazil. Electronic address: ml.andersen12@gmail.com.4Departamento de Psicobiologia, Universidade Federal de São Paulo, Brazil.5Departamento de Oftalmologia, Universidade Federal de São Paulo, Brazil.6Departamento de Farmacologia, Universidade Federal de São Paulo, Brazil; Departamento de Psicobiologia, Universidade Federal de São Paulo, Brazil.7Centro de Controle de Intoxicações, Universidade Estadual de Campinas, Brazil.8Centro de Controle de Intoxicações, Universidade Estadual de Campinas, Brazil; Laboratório de Química e Toxicologia Forense, Superintendência da Polícia Técnico Científica do Estado de São Paulo, Brazil.9Departamento de Toxicologia e Análises Toxicológicas, Universidade de São Paulo, Brazil; Departamento de Química Fundamental, Universidade de São Paulo, Brazil.AbstractChlorophenylpiperazines (CPP) are psychotropic drugs used in nightclub parties and are frequently used in a state of sleep deprivation, a condition which can potentiate the effects of psychoactive drugs. This study aimed to investigate the effects of sleep deprivation and sleep rebound (RB) on anxiety-like measures in mCPP-treated mice using the open field test. We first optimized our procedure by performing dose-effect curves and examining different pretreatment times in naïve male Swiss mice. Subsequently, a separate cohort of mice underwent paradoxical sleep deprivation (PSD) for 24 or 48h. In the last experiment, immediately after the 24h-PSD period, mice received an injection of saline or mCPP, but their general activity was quantified in the open field only after the RB period (24 or 48h). The dose of 5mgmL(-1) of mCPP was the most effective at decreasing rearing behavior, with peak effects 15min after injection. PSD decreased locomotion and rearing behaviors, thereby inhibiting a further impairment induced by mCPP. Plasma concentrations of mCPP were significantly higher in PSD 48h animals compared to the non-PSD control group. Twenty-four hours of RB combined with mCPP administration produced a slight reduction in locomotion. Our results show that mCPP was able to significantly change the behavior of naïve, PSD, and RB mice. When combined with sleep deprivation, there was a higher availability of drug in plasma levels. Taken together, our results suggest that sleep loss can enhance the behavioral effects of the potent psychoactive drug, mCPP, even after a period of rebound sleep.
Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2014 Mar 3;49:70-7. doi: 10.1016/j.pnpbp.2013.11.007. Epub 2013 Nov 19.
Chlorophenylpiperazines (CPP) are psychotropic drugs used in nightclub parties and are frequently used in a state of sleep deprivation, a condition which can potentiate the effects of psychoactive drugs. This study aimed to investigate the effects of sleep deprivation and sleep rebound (RB) on anxie
PMID 24269663

Japanese Journal

FDに対する漢方薬の効果と脳腸相関 : セロトニン・グレリンの役割(シンポジウム:機能性胃腸症(Functional Dyspepsia)の病態を巡る脳腸相関,2008年,第49回日本心身医学会総会(札幌))

武田宏司,武藤修一,服部智久 [他],定金千春
心身医学 49(7), 807-813, 2009-07-01
従来,functional dyspepsia(FD)の病態において消化管の機能異常が重視されてきたが,最近では脳-腸相関の関与が注目されている.六君子湯はFDに対する臨床効果が最も確立している漢方薬であり,特に食欲改善効果が顕著である.胃で産生される摂食ホルモンであるグレリンは,摂食調節に加えて,消化管運動,胃酸分泌にも関与することが示されており,脳-胃相関において重要な役割を果たしている.そこ …
NAID 110007331042

Synergistic actions of apomorphine and m-chlorophenylpiperazine on ejaculation, but not penile erection in rats

YONEZAWA A
Biomed Res 30, 71-78, 2009
NAID 80020251916

High throughput and sensitive determination of trazodone and its primary metabolite, m-chlorophenylpiperazine, in human plasma by liquid chromatography-tandem mass spectrometry

PATEL Bhavin N.,SHARMA Naveen,SANYAL Mallika,SHRIVASTAV Pranav S.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 871(1), 44-54, 2008-08-01
NAID 10028003563