Discriminative stimulus properties of amphetamine and structurally related phenalkylamines

Young, Richard; Glennon, Richard A.

doi:10.1002/med.2610060105

Cited by 85 publications

(31 citation statements)

References 60 publications

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“…Finally, this investigation shows that AMPH is more efficient than PEA in CA release. Considering that various behaviors result from CA release [1,19,20], previous results [36] can be explained by our data. Indeed, these authors have revealed that PEA administration was not able to induce the same behavioral response obtained in the presence of AMPH.…”

Section: Discussionsupporting

confidence: 49%

Effects of Amphetamine and Phenylethylamine on Catecholamine Release in the Glomerular Layer of the Rat Olfactory Bulb

Mesfioui

Math²,

Jmari

et al. 1998

Biol Signals Recept

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In the present work, we have shown electrochemically that in the rat olfactory bulb (OB), extracellular dopamine (DA) was highest in the glomerular layer (GL), whereas extracellular noradrenaline (NA) appeared to be more uniformly distributed across layers. The GL catecholamine (CA) responses to amphetamine (AMPH) and phenylethylamine (PEA) were also characterized electrochemically using an in vivo model. Results of this investigation show that at a lower dose (1 mg/kg), PEA had no effect on CA release. In contrast, at a higher dose (10 mg/kg), it produced similar increases in either extracellular DA (17.5 ± 7%) or extracellular NA (14 ± 3%), and DA exhibited dose-independent increases to AMPH (93 ± 8%: 1 mg/kg vs. 97 ± 6%: 10 mg/kg) whereas NA exhibited dose-dependent increases to AMPH (24.5 ± 6%: 1 mg/kg vs. 39 ± 7%: 10 mg/kg). These data indicate that (i) PEA may increase CA release but less efficiently than AMPH. (ii) AMPH is more efficient on the DAergic than on the NAergic system since AMPH-induced DA release exceeded 2–4 times the AMPH-induced NA release.

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Section: Discussionsupporting

confidence: 49%

Effects of Amphetamine and Phenylethylamine on Catecholamine Release in the Glomerular Layer of the Rat Olfactory Bulb

Mesfioui

Math²,

Jmari

et al. 1998

Biol Signals Recept

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“…Lastly, evidence that the stimulus e¤ects produced by cathinone, amphetamine, and methamphetamine are mediated by dopaminergic mechanisms is derived from the Þnding that they can be blocked by the administration of dopamine receptor antagonists, such as haloperidol (e.g., Kalix and Glennon 1986;Schechter 1986;Young and Glennon 1986). In addition, since methcathinone is capable of inducing release of radioactivity from [H 3 ] dopamine-prelabeled tissue of rat caudate nucleus in a manner similar to that observed with cathinone, amphetamine, and methamphetamine (Glennon et al 1987), it was anticipated that haloperidol would block the S([)-CAT stimulus.…”

Section: Discussionmentioning

confidence: 99%

“…Also evaluated was fenßuramine, a structurally related but nonstimulant anorectic agent, and cis-(±)-4-methylaminorex (U4Euh); recently, this latter compound has appeared on the clandestine market as a designer drug and is a derivative of the cyclic phenylisopropylamine aminorex (Davis and Brewster 1988). In the last experiment, haloperidol, a dopamine receptor antagonist known to e¤ectively antagonize the stimulus e¤ect of amphetamine (for review see Young and Glennon 1986), was tested as an antagonist of the S([)-CAT stimulus.…”

Section: Introductionmentioning

confidence: 99%

Discriminative stimulus effects of S (−)-methcathinone (CAT): a potent stimulant drug of abuse

Young

Glennon

1998

Psychopharmacology

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Methcathinone ("CAT") is a CNS stimulant that is a very significant drug of abuse in the former Soviet Union. It has also appeared on the clandestine market in the United States and has been recently classified as a Schedule I substance. In the present study, S(-)-methcathinone [S(-)-CAT, 0.50 mg/kg, IP] was employed as the training drug in a two-lever drug discrimination task in rats. Once established, the S(-)-CAT stimulus was shown to have a rapid onset to action (within 5 min) and a duration of effect of approximately 60-90 min. In tests of stimulus generalization (substitution), the S(-)-CAT (ED50 = 0.11 mg/kg) stimulus generalized to S(+)-methamphetamine (ED5 = 0.17 mg/kg), S(-)-cathinone (ED50 = 0.19 mg/kg), S(+)-amphetamine (ED50 = 0.23 mg/kg), aminorex (ED50 = 0.27 mg/kg), (+/-)-CAT (ED50 = 0.25 mg/kg), (+/-)-cathinone (ED50 = 0.41 mg/kg), R(+)-CAT (ED50 = 0.43 mg/kg), cis-4-methylaminorex (ED50 = 0.49 mg/kg), methylphenidate (ED50 = 0.83 mg/kg), and cocaine (ED50= 1.47 mg/kg). S(-)-CAT-stimulus generalization did not occur to fenfluramine, a structurally related nonstimulant anorectic. Lastly, haloperidol (AD50 = 0.18 mg/kg), a dopamine receptor antagonist, potently antagonized the S(-)-CAT stimulus. It is concluded that S(-)-methcathinone is a very potent CNS stimulant, which appears to produce its stimulus effect, at least in part, via a dopaminergic mechanism.

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“…Animals making fewer than five total responses during the 2.5-min extinction session were considered as being behaviorally disrupted. Percent drug-appropriate responding and response rate data refer only to animals making ≥5 responses during the extinction session (Young and Glennon 1986).…”

Section: Drug Discriminationmentioning

confidence: 99%

MD-354 selectively antagonizes the antinociceptive effects of (−)nicotine in the mouse tail-flick assay

et al. 2010

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MD-354 selectively antagonizes the antinociceptive actions of (-)nicotine in the tail-flick, but not in the hot-plate assay, or either the motor effects, or discriminative stimulus effects of (-)nicotine. The most parsimonious explanation is that MD-354 might act as a negative allosteric modulator of alpha 7 nACh receptors, and radioligand binding and functional data are provided to support this conclusion.

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Discriminative stimulus properties of amphetamine and structurally related phenalkylamines

Cited by 85 publications

References 60 publications

Effects of Amphetamine and Phenylethylamine on Catecholamine Release in the Glomerular Layer of the Rat Olfactory Bulb

Effects of Amphetamine and Phenylethylamine on Catecholamine Release in the Glomerular Layer of the Rat Olfactory Bulb

Discriminative stimulus effects of S (−)-methcathinone (CAT): a potent stimulant drug of abuse

MD-354 selectively antagonizes the antinociceptive effects of (−)nicotine in the mouse tail-flick assay

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