The Pharmacological Profile of Some Psychomotor Stimulant Drugs Including Chemical, Neurophysiological, Biochemical, and Toxicological Aspects

Garattini, S.; Samanin, R.

doi:10.1007/978-3-642-67767-0_14

Cited by 16 publications

(10 citation statements)

References 253 publications

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“…We found that the effects of amphetamine and morphine on DA release are sensitive to the peripheral administration of 5-HT 2A and 5-HT 2C/2B receptor antagonists, respectively. Although the clearance of the P 450 substrate amphetamine may be affected by drugs that undergo oxidative metabolism (Garattini and Samanin 1981), we found that its brain concentrations in SR 46349B-and SB 206553-pretreated rats were not different from those in controls. Morphine is cleared mainly by glucuronide conjugation, and like amphetamine, its transport to the brain is thought to occur mainly by passive diffusion (Murphey and Olsen 1994).…”

Section: Discussioncontrasting

confidence: 51%

5-HT2A and 5-HT2C/2B Receptor Subtypes Modulate Dopamine Release Induced in Vivo by Amphetamine and Morphine in Both the Rat Nucleus Accumbens and Striatum

Porras

Matteo

Fracasso

et al. 2002

Neuropsychopharmacology

199

161

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Section: Discussioncontrasting

confidence: 51%

5-HT2A and 5-HT2C/2B Receptor Subtypes Modulate Dopamine Release Induced in Vivo by Amphetamine and Morphine in Both the Rat Nucleus Accumbens and Striatum

Porras

Matteo

Fracasso

et al. 2002

Neuropsychopharmacology

199

161

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“…Finally, locomotor effects of opioids may be mediated by catecholaminergic mechanisms (see Oliverio et al 1984), but it seems unlikely that antihistaminics enhance morphine-induced hyperactivity by acting on these mechanisms. Catecholamines, in fact, are certainly involved in the action of amphetamine (Garattini and Samanin 1981), but in the present study antihistaminics did not change the stimulatory action of amphetamine.…”

Section: Discussionmentioning

confidence: 39%

Antihistaminics enhance morphine-, but not amphetamine-and scopolamine-induced hyperactivity in mice

et al. 1987

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Three histamine H1-receptor antagonists, chlorpheniramine, diphenhydramine and tripelennamine, were tested alone or in combination with morphine, amphetamine and scopolamine on locomotor activity in mice. All three antihistaminics, at some dosage levels, enhanced morphine-induced hyperactivity, but did not change or even reduce locomotor stimulation induced by amphetamine and scopolamine. The results suggest that H1-blocking agents may specifically interact, though not necessarily directly, with opiate mechanisms in producing behavioural effects.

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“…A similar phenomenon may also underlie the changes observed in both cis-isomers and the isomer trans-4S,5S. Such dual mechanisms are supported by observations of Ashby et al (1995) who showed that the suppressant effects of trans-4S,5S-4-methylaminorex on A10 dopamine cells are attenuated by pretreating animals with ␣-methyl-p-tyrosine or reserpine, which depletes newly synthesized cytoplasmic dopamine and vesicular stores of monoamines, respectively (Garattini and Samanin, 1981). Taken together, it seems that both cytoplasmic and vesicular dopamine mediate the effects of trans-4S, 5S-, cis-4S,5R-, and cis-4R,5S-4-methylaminorex, which implies an action mechanism involving both dopamine release and uptake inhibition.…”

mentioning

confidence: 64%

Acute Neurochemical and Behavioral Effects of Stereoisomers of 4-Methylaminorex in Relation to Brain Drug Concentrations

Kankaanpää

Ellermaa²,

Meririnne³

et al. 2002

J Pharmacol Exp Ther

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4-Methylaminorex is a stimulant drug of abuse that exists as four stereoisomers: cis-4R,5S, cis-4S,5R, trans-4S,5S, and trans-4R,5R. These isomers have previously been shown to differ markedly in various respects. In the present study we assessed the effects of the isomers of 4-methylaminorex (2.5, 5.0, and 10 mg/kg i.p.) on extracellular dopamine and 5-hydroxytryptamine (5-HT) levels in the nucleus accumbens, as well as behavior in the rats simultaneously. The relative concentrations of the isomers in the brain were also measured. The samples were collected by in vivo microdialysis and then analyzed for neurotransmitters with highperformance liquid chromatography/electrochemical detection and for cis-and trans-4-methylaminorex with gas chromatography/mass spectrometry. The behavioral effects of the isomers were assessed from videotapes recorded during the microdialysis experiments. All isomers elevated the extracellular levels of both dopamine and 5-HT, with the exception of trans-4R,5R. The rank order of potency for elevating dopamine was trans-4S,5S Ͼ cis-4S,5R Ϸ cis-4R,5S Ͼ trans-4R,5R, and for elevating 5-HT cis-4S,5R Ͼ trans-4S,5S Ϸ cis-4R,5S Ͼ trans-4R,5R. Analysis of the behavioral data, together with the neurochemical data, suggests that behavioral effects of the isomers of 4-methylaminorex are related to drug-induced dopamine release and, in the case of higher doses of the most efficacious isomers, to 5-HT as well. The brain concentrations of the isomers did not reflect their neurochemical efficacy, which implies that their differences are pharmacodynamic rather than pharmacokinetic.

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The Pharmacological Profile of Some Psychomotor Stimulant Drugs Including Chemical, Neurophysiological, Biochemical, and Toxicological Aspects

Cited by 16 publications

References 253 publications

5-HT2A and 5-HT2C/2B Receptor Subtypes Modulate Dopamine Release Induced in Vivo by Amphetamine and Morphine in Both the Rat Nucleus Accumbens and Striatum

5-HT2A and 5-HT2C/2B Receptor Subtypes Modulate Dopamine Release Induced in Vivo by Amphetamine and Morphine in Both the Rat Nucleus Accumbens and Striatum

Antihistaminics enhance morphine-, but not amphetamine-and scopolamine-induced hyperactivity in mice

Acute Neurochemical and Behavioral Effects of Stereoisomers of 4-Methylaminorex in Relation to Brain Drug Concentrations

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