A comparison of the effects of 1-benzylpiperazine and dexamphetamine on human performance tests

Bye, Carole; Munro-Faure, A. D.; Peck, A. W.; Young, P. A.

doi:10.1007/bf00558280

Cited by 93 publications

(68 citation statements)

References 9 publications

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“…Stimulant effects, however, were slight, and whilst mean performance in the vigilance test 1.25-2.25 h post-drug was almost always higher than following lactose, the difference was not significant. The sensitivity of this test in detecting a stimulant effect of drugs was established by Bye et al (1973), who showed that the performance of a group of 12 subjects was significantly improved following doses of dexamphetamine (1 and 2.5 mg). The second trial confirmed the lack of any significant stimulant effect following L(+)pseudoephedrine, though mean values were higher compared with those following lactose in both the tapping test and the first two vigilance tests.…”

Section: Discussionmentioning

confidence: 99%

“…By contrast, drowsiness is a well recognized side effect of effective antihistamines, but attempts to measure this phenomenon and compare the relative effects of different drugs have not been made. In view of this it was decided to investigate the central effects of the two ephedrine isomers, triprolidine, and a combination of L(+)pseudoephedrine and triprolidine using an experimental design and test procedures which had previously proved extremely sensitive to dexamphetamine in our hands (Bye, Munro-Faure, Peck & Young, 1973).…”

Section: Introductionmentioning

confidence: 99%

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Effects on the Human Central Nervous System of Two Isomers of Ephedrine and Triprolidine, and Their Interaction

Bye

Dewsbury

Peck

1974

Brit J Clinical Pharma

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1 D(-)ephedrine is four times as potent as L(+)pseudoephedrine in producing both tachycardia and a rise in systolic blood pressure. No changes in diastolic blood pressure occurred in 12 subjects with doses of up to D(-)ephedrine (50 mg) and L(+)pseudoephedrine (180 mg). 2 Significant evidence of stimulation of the central nervous system occurred only after D(-)ephedrine in that tapping rates were increased and subjects could reliably detect that they had received an active drug. While mean performance rates in an auditory vigilance test were higher following both ephedrine isomers these changes were not significant. 3 Impairment of both tapping rates and auditory vigilance occurred following triprolidine in another group of 12 subjects. The effect was generally related to dose of antihistamine given and lasted up to 7.25 hours. Subjective effects were reliably recognized by subjects following all treatments containing triprolidine (2.5 mg or more) for up to 4.75 hours. Using analogue lines for self rating the subjective effects following triprolidine indicated both mental and physical impairment differing significantly from scores after lactose and L(+)pseudoephedrine (60 mg). 4 Combination of triprolidine (2.5 mg) and L(+)pseudoephedrine (60 mg) produced effects similar to triprolidine alone on both subjective measures and the auditory vigilance test. It is suggested that these objective tests and subjective scales could be used to measure effects on the central nervous system produced by antihistamines together with similar drugs, and their interaction with other compounds administered concurrently.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effects on the Human Central Nervous System of Two Isomers of Ephedrine and Triprolidine, and Their Interaction

Bye

Dewsbury

Peck

1974

Brit J Clinical Pharma

Self Cite

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“…Amphetamine has well-documented effects on psychomotor and cognitive function (Koelega 1993), and there is some evidence that its effects on vigilance are more pronounced than its effects on motor performance. Two previous studies have shown that low doses of amphetamine (5 to 10 mg) improve performance of an auditory vigilance task, while leaving a simple motor task (finger tapping) unaffected (Bye et al 1973;Hamilton et al 1983). This study of brain activity after administration of amphetamine and during performance of two tasks allowed us to examine the relationship between changes in regional brain activity and changes in behavior induced by the drug.…”

mentioning

confidence: 90%

An fMRI Study of the Effect of Amphetamine on Brain Activity,

Uftring

Wachtel

Chu

et al. 2001

Neuropsychopharmacology

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“…Similar to MDMA, however, TFMPP displays presynaptic actions that include stimulation of SERT-mediated 5-HT release from neurons, as demonstrated in vitro (Pettibone and Williams, 1984) and in vivo (Auerbach et al, 1991). There is limited information available on the molecular mechanism of BZP, but this drug elicits amphetamine-like behavioral effects in rodents (Jones et al, 1980) and humans (Bye et al, 1973). No scientific investigations regarding the neurobiology of BZP plus TFMPP (BZP/TFMPP) are available.…”

Section: Introductionmentioning

confidence: 99%

N-Substituted Piperazines Abused by Humans Mimic the Molecular Mechanism of 3,4-Methylenedioxymethamphetamine (MDMA, or ‘Ecstasy’)

Baumann

Clark

Budzynski

et al. 2004

Neuropsychopharmacol

217

157

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3,4-Methylenedioxymethamphetamine (MDMA, or 'Ecstasy') is an illicit drug that stimulates the release of serotonin (5-HT) and dopamine (DA) from neurons. Recent evidence reveals that drug users are ingesting piperazine analogs, like 1-benzylpiperazine (BZP, or 'A2') and 1-(m-trifluoromethylphenyl)piperazine (TFMPP, or 'Molly'), to mimic psychoactive effects of MDMA. In the present study, we compared the neurochemistry of MDMA, BZP, and TFMPP in rats. MDMA (1-3 mg/kg, i.v.) increased dialysate 5-HT and DA in a dose-related fashion, with actions on 5-HT being predominant. BZP (3-10 mg/kg, i.v.) elevated dialysate DA and 5-HT, while TFMPP (3-10 mg/kg, i.v.) elevated 5-HT. Administration of BZP plus TFMPP at a 1:1 ratio (BZP/TFMPP) produced parallel increases in dialysate 5-HT and DA; a 3 mg/kg dose of BZP/TFMPP mirrored the effects of MDMA. At a 10 mg/kg dose, BZP/TFMPP increased dialysate DA more than the summed effects of each drug alone, and some rats developed seizures. Our results show that BZP/TFMPP and MDMA share the ability to evoke monoamine release, but dangerous drug-drug synergism may occur when piperazines are coadministered at high doses.

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A comparison of the effects of 1-benzylpiperazine and dexamphetamine on human performance tests

Cited by 93 publications

References 9 publications

Effects on the Human Central Nervous System of Two Isomers of Ephedrine and Triprolidine, and Their Interaction

Effects on the Human Central Nervous System of Two Isomers of Ephedrine and Triprolidine, and Their Interaction

An fMRI Study of the Effect of Amphetamine on Brain Activity,

N-Substituted Piperazines Abused by Humans Mimic the Molecular Mechanism of 3,4-Methylenedioxymethamphetamine (MDMA, or ‘Ecstasy’)

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