Comparison of intravenous cocaethylene and cocaine in humans.

Abstract:

RATIONALE:Cocaethylene is a pharmacologically active homolog and metabolite of cocaine, formed by transesterification of cocaine in the presence of ethanol. Here we relate findings from a randomized, placebo-controlled, double-blind study in which we examined the physiological and subjective effects and pharmacokinetics of i.v. administered cocaethylene in human volunteers using cocaine as a comparator. METHODS:Cocaine-dependent participants randomly received one study drug, cocaethylene (0.25 or 0.5 mg/kg), cocaine (0.25 or 0.5 mg/kg), or placebo, during each experimental session which occurred on separate days. RESULTS:Cocaethylene was less potent in elevating heart rate than equivalent doses of cocaine. Similar differences between cocaine and cocaethylene were found for subjective measures ("Cocaine High", "Rush", "Stimulated" and "Good Drug Effects"). All active drug conditions produced significant increases in systolic blood pressure relative to placebo, but no significant effect on diastolic blood pressure was observed. Cocaethylene demonstrated a slower clearance, larger volume of distribution and correspondingly longer elimination half-life than cocaine. CONCLUSION:The findings from this study confirm those of previous studies that show that cocaethylene has pharmacological properties in common with cocaine, but is less potent.

journal_title

Psychopharmacology

authors

Hart CL,Jatlow P,Sevarino KA,McCance-Katz EF

doi

10.1007/s002139900363

subject

Has Abstract

pub_date

2000-04-01 00:00:00

pages

153-62

issue

2

eissn

0033-3158

issn

1432-2072

journal_volume

149

pub_type

临床试验,杂志文章,随机对照试验
  • Translating the smoking cessation properties of the antidepressant nortriptyline using reinforcing, discriminative and aversive stimulus effects of nicotine in rats.

    abstract:RATIONALE:The antidepressant nortriptyline is a second-line pharmacotherapy for smoking cessation. Given that there is limited preclinical data available on the effects of nortriptyline on responses to nicotine, the present study sought to evaluate its effects on the reinforcing, discriminative stimulus (DS) and aversi...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-011-2413-2

    authors: Wing VC,Shoaib M

    更新日期:2012-02-01 00:00:00

  • Anxiogenic drugs beta-CCE and FG 7142 increase extracellular dopamine levels in nucleus accumbens.

    abstract::Two experiments were conducted to study the effects of anxiogenic drugs on dopamine release and metabolism in nucleus accumbens. Microdialysis probes were implanted into the nucleus accumbens, and rats were tested the day after implantation. In the first experiment, groups of rats received injections of saline, 1.25 o...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02245888

    authors: McCullough LD,Salamone JD

    更新日期:1992-01-01 00:00:00

  • Chronic treatment with a selective inhibitor of casein kinase I delta/epsilon yields cumulative phase delays in circadian rhythms.

    abstract:INTRODUCTION:Casein kinase I epsilon/delta phosphorylates certain clock-related proteins as part of a complex arrangement of transcriptional/translational feedback loops that comprise the circadian oscillator in mammals. Pharmacologic inhibition leads to a delay of the oscillations with the magnitude of this effect dep...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-010-1860-5

    authors: Sprouse J,Reynolds L,Kleiman R,Tate B,Swanson TA,Pickard GE

    更新日期:2010-07-01 00:00:00

  • Basolateral amygdala inactivation abolishes conditioned stimulus- and heroin-induced reinstatement of extinguished heroin-seeking behavior in rats.

    abstract:RATIONALE:Drug-paired stimuli elicit drug craving and relapse in addicts and drug-seeking behavior in rats. The functional integrity of the basolateral amygdala (BLA) is necessary for reinstatement of cocaine-seeking behavior elicited by cocaine-conditioned stimuli, but not by cocaine itself. It is unclear, however, wh...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-001-0997-7

    authors: Fuchs RA,See RE

    更新日期:2002-04-01 00:00:00

  • Serotonin 1A receptor availability in patients with schizophrenia and schizo-affective disorder: a positron emission tomography imaging study with [11C]WAY 100635.

    abstract:BACKGROUND:Postmortem and positron emission tomography (PET) studies have reported several alterations in serotonin 1A receptor (5-HT(1A)) binding parameters in patients with schizophrenia. This study examines 5-HT(1A) availability in vivo in individuals with schizophrenia and schizo-affective disorder. MATERIALS AND ...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-006-0543-8

    authors: Frankle WG,Lombardo I,Kegeles LS,Slifstein M,Martin JH,Huang Y,Hwang DR,Reich E,Cangiano C,Gil R,Laruelle M,Abi-Dargham A

    更新日期:2006-12-01 00:00:00

  • The influence of acetylsalicylic acid on cognitive processing: an event-related potentials study.

    abstract::The central effects of acetylsalicylic acid (ASA) are discussed controversially. In animal models, it has been shown that ASA can interact with the central serotonergic and catecholaminergic neuronal system. However, the relevance of this interaction for humans is still unknown. We performed a study on the influence o...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/s002130050683

    authors: Austermann M,Grotemeyer KH,Evers S,Rödding D,Husstedt IW

    更新日期:1998-08-01 00:00:00

  • Effects of fatty acid amide hydrolase (FAAH) inhibitors on working memory in rats.

    abstract:RATIONALE:Manipulations of the endocannabinoid system could potentially produce therapeutic effects with minimal risk of adverse cannabis-like side effects. Inhibitors of fatty acid amide hydrolase (FAAH) increase endogenous levels of the cannabinoid-receptor agonist, anandamide, and show promise for treating a wide ra...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-015-4140-6

    authors: Panlilio LV,Thorndike EB,Nikas SP,Alapafuja SO,Bandiera T,Cravatt BF,Makriyannis A,Piomelli D,Goldberg SR,Justinova Z

    更新日期:2016-05-01 00:00:00

  • The discriminative stimulus properties of cocaine: effects of microinfusion of cocaine, a 5-HT1A agonist or antagonist, into the ventral tegmental area.

    abstract::Serotonin (5-HT) afferents may modulate the dopamine mesoaccumbens circuit, which has been shown to be critically involved in the locomotor stimulatory, discriminative stimulus, and rewarding properties of cocaine. In the present study, we investigated the role of 5-HT1A receptors in the ventral tegmental area (VTA) i...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130050586

    authors: De La Garza R 2nd,Callahan PM,Cunningham KA

    更新日期:1998-05-01 00:00:00

  • Differential effects of systemically administered nor-binaltorphimine (nor-BNI) on kappa-opioid agonists in the mouse writhing assay.

    abstract::The opioid antagonist effects of systemically administered nor-binaltorphimine (nor-BNI) were evaluated against the kappa agonists CI-977, U69,593, U50,488, ethylketocyclazocine (EKC), Mr2034 and bremazocine, the mu agonist morphine and the alkaloid delta agonist BW-373U86 in the acetic acid-induced writhing assay in ...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02245071

    authors: Broadbear JH,Negus SS,Butelman ER,de Costa BR,Woods JH

    更新日期:1994-07-01 00:00:00

  • Effects of d-amphetamine, maprotiline, L-dopa, and haloperidol on the components of the predatory behavior of the ferret, Putorius furo L.

    abstract::Ferret predation on rats was examined in an arena. One hour before the test one of the following drugs was administered. d-Amphetamine (0.8 and 1.4 mg/kg IM), MAPROTILINE (10 AND 40 Mg/kg orally), L-dopa (30 and 60 mg/kg orally), or haloperidol (0.14 and 0.6 mg/kg IM). Provided that capture was successful, the sequenc...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00427524

    authors: Schmidt WJ

    更新日期:1979-09-01 00:00:00

  • Inhibition of shaking movements in rats by central administration of cholinergic and adrenergic agents.

    abstract::Shaking movements of the body, similar to that made by a dog when wet ('wet-dog shakes'), occur in rats in response to pharmacological stimuli and in response to stimuli associated with cold and skin irritation. In this study, shaking movements, elicited by a variety of stimuli, were inhibited by central administratio...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00429002

    authors: Wei ET

    更新日期:1983-01-01 00:00:00

  • Effects of AZD3480, a neuronal nicotinic acetylcholine receptor agonist, and donepezil on dizocilpine-induced attentional impairment in rats.

    abstract:BACKGROUND AND RATIONALE:Nicotinic acetylcholine systems play major roles in cognitive function. Nicotine and a variety of nicotinic agonists improve attention, and nicotinic antagonist exposure impairs it. This study was conducted to investigate the effect of a novel nicotinic receptor agonist at α4β2 nicotinic recept...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-012-2712-2

    authors: Rezvani AH,Cauley MC,Johnson EC,Gatto GJ,Levin ED

    更新日期:2012-10-01 00:00:00

  • Platelet membrane fluidity and treatment response in cognitively-impaired, depressed elderly: initial results.

    abstract::A prospective study of response to treatment with nortriptyline was carried out in a group of 14 inpatients with mixed symptoms of depression and dementia. Platelet membrane fluidity, as reflected by the fluorescence anisotropy of DPH labeled membranes, was determined for all 14 drug-free subjects prior to treatment b...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00174688

    authors: Zubenko GS,Reynolds CF 3rd,Perel JM,Decker C,Malinakova I

    更新日期:1988-01-01 00:00:00

  • Effect of 5-HT2 receptor antagonists on a cranial nerve reflex in the rabbit: evidence for inverse agonism.

    abstract::This study examined the role of the serotonin 5-HT2 receptor in motor function by examining the effect of antagonists on the motor performance of a cranial nerve reflex, the nictitating membrane (NM) reflex of the rabbit. The NM reflex was elicited by varying intensities of a tactile stimulus and the magnitudes of the...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130050820

    authors: Harvey JA,Welsh SE,Hood H,Romano AG

    更新日期:1999-01-01 00:00:00

  • Pindolol decreases prolactin and growth hormone responses to intravenous L-tryptophan.

    abstract::The effects of pindolol on the prolactin (PRL) and growth hormone (GH) responses to intravenous tryptophan (LTP) were studied in eight healthy male volunteers. Pindolol pretreatment (40 mg over 48 h) markedly attenuated the GH response to LTP and modestly, but significantly, reduced the LTP-induced increase in plasma ...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02244090

    authors: Smith CE,Ware CJ,Cowen PJ

    更新日期:1991-01-01 00:00:00

  • Cortical and hippocampal EEG power spectra in animal models of schizophrenia produced with methamphetamine, cocaine, and phencyclidine.

    abstract::Cortical and hippocampal EEGs in animal models of schizophrenia were compared to those obtained with psychotomimetics or antipsychotic agents by utilizing power spectral analysis. Models of positive schizophrenic symptoms were created with methamphetamine (MAP) and cocaine, and a model of both negative and positive sy...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130050306

    authors: Yamamoto J

    更新日期:1997-06-01 00:00:00

  • Early postnatal clonidine treatment results in altered regional catecholamine utilisation in adult rat brain.

    abstract::Clonidine is a clinically used antihypertensive which has been suggested to produce physiological changes in children after exposure in utero. The aim of our study was to test the hypothesis that chronic exposure of the developing brain to an alpha 2-adrenergic agonist like clonidine would influence the adult neuroche...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02253583

    authors: Feenstra MG,van Galen H,Boer GJ

    更新日期:1992-01-01 00:00:00

  • Arousal and the pupil: why diazepam-induced sedation is not accompanied by miosis.

    abstract:RATIONALE:There is a close relationship between arousal and pupil diameter, decrease in the level of arousal being accompanied by constriction of the pupil (miosis), probably reflecting the attenuation of sympathetic outflow as sedation sets in. Paradoxically, sedation induced by benzodiazepines is not accompanied by m...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00213-007-0884-y

    authors: Hou RH,Samuels ER,Langley RW,Szabadi E,Bradshaw CM

    更新日期:2007-11-01 00:00:00

  • A reliable method to study cue-, priming-, and stress-induced reinstatement of cocaine self-administration in mice.

    abstract:RATIONALE:Cocaine addiction is a relapsing psychiatric disorder with a high prevalence in developed countries. To date, the reinstatement model has been difficult to implement in mice. The design of an appropriate reinstatement model in mice is required in order to use genetically modified animals with the aim of clari...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-008-1184-x

    authors: Soria G,Barbano MF,Maldonado R,Valverde O

    更新日期:2008-09-01 00:00:00

  • Assessment of a combination of physostigmine and scopolamine as pretreatment against the behavioural effects of organophosphates in the common marmoset (Callithrix jacchus).

    abstract:RATIONALE:There is a requirement to ensure that UK armed forces are provided with the best possible medical countermeasures to prevent or mitigate the effects of exposure to nerve agents. When pretreatments are under consideration, it is of particular importance to ensure that they do not in themselves give rise to adv...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-002-1324-7

    authors: Muggleton NG,Bowditch AP,Crofts HS,Scott EA,Pearce PC

    更新日期:2003-03-01 00:00:00

  • Smoking withdrawal is associated with increases in brain activation during decision making and reward anticipation: a preliminary study.

    abstract:RATIONALE:Acute nicotine abstinence is associated with disruption of executive function and reward processes; however, the neurobiological basis of these effects has not been fully elucidated. METHODS:The effects of nicotine abstinence on brain function during reward-based probabilistic decision making were preliminar...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-011-2404-3

    authors: Addicott MA,Baranger DA,Kozink RV,Smoski MJ,Dichter GS,McClernon FJ

    更新日期:2012-01-01 00:00:00

  • Dose-dependent influence of buspirone on the activities of selective serotonin reuptake inhibitors in the mouse forced swimming test.

    abstract::Recent clinical data suggest that buspirone may enhance the efficacy and/or reduce the latency to therapeutic effect of selective serotonin reuptake inhibitors (SSRIs) in unipolar major depressive disorder. The present study, using the mouse forced swimming test, was performed to investigate further the mechanisms inv...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130050663

    authors: Redrobe JP,Bourin M

    更新日期:1998-07-01 00:00:00

  • Oral behaviour induced by intranigral muscimol is unaffected by haloperidol but abolished by large lesions of superior colliculus.

    abstract::It has been suggested that the GAbAergic striatonigral projection may form part of the efferent pathway responsible for the expression of dopamine-related oral behaviour. Consistent with this suggestion are reports that bilateral injection of the GABA agonist muscimol can produce stereotyped gnawing and biting. We rep...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00464579

    authors: Taha EB,Dean P,Redgrave P

    更新日期:1982-01-01 00:00:00

  • Increased sensitivity to benzodiazepine antagonists in rats following chronic treatment with a low dose of diazepam.

    abstract::The effects of benzodiazepine (BZ) antagonists on operant behavior were examined in rats chronically administered a low dose of diazepam (DZ). The low maintenance dose of DZ (5 mg/kg twice daily) was selected as more closely associated with its anxiolytic effects than the higher treatment doses previously used to stud...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02244103

    authors: Lucki I,Kucharik RF

    更新日期:1990-01-01 00:00:00

  • Increased salivary cortisol after waking in depression.

    abstract:RATIONALE:Cortisol hypersecretion is regarded as important in the pathophysiology of major depression. However, recent studies in community-based samples have been inconclusive. OBJECTIVE:To determine whether acutely depressed, medication-free subjects show an exaggerated release of cortisol in saliva in relation to a...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-005-0062-z

    authors: Bhagwagar Z,Hafizi S,Cowen PJ

    更新日期:2005-10-01 00:00:00

  • The effect of peripheral noradrenaline depletion on responding on a schedule of differential reinforcement of low rates of response (DRL).

    abstract::First, it was confirmed that systemic injection of the neurotoxin 6-hydroxydopamine HBr (30 mg/kg IP) depleted noradrenaline levels in rat heart, but not centrally. Losses averaged 90% of control 1 day after injection, and 50% at 42 days. The same drug and dose was then administered to 50% of a group of rats which had...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00431782

    authors: Salmon P,Stanford C,Gray JA

    更新日期:1985-01-01 00:00:00

  • The delta opioid receptor antagonist naltrindole attenuates both alcohol and saccharin intake in rats selectively bred for alcohol preference.

    abstract::This study demonstrates that the selective delta receptor antagonists ICI 174864 and naltrindole (NTI) attenuate alcohol intake in a dose-dependent manner, without altering water intake, in rats selectively bred for alcohol preference. ICI 174864 had a very limited duration of action, as evidenced by the fact that sup...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02246191

    authors: Krishnan-Sarin S,Jing SL,Kurtz DL,Zweifel M,Portoghese PS,Li TK,Froehlich JC

    更新日期:1995-07-01 00:00:00

  • Characteristics of oral movements in rats during and after chronic haloperidol and fluphenazine administration.

    abstract::Rats were chronically administered either haloperidol (HAL) or fluphenazine (FLU) via depot injections for 8 months, given these same drugs in their drinking water for the next 2 months, and then withdrawn from the drugs. Throughout the experiment the animals were tested repeatedly in an enclosed tube using a computer...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00174701

    authors: See RE,Levin ED,Ellison GD

    更新日期:1988-01-01 00:00:00

  • Basal and cocaine-induced sex differences in the DARPP-32-mediated signaling pathway.

    abstract:RATIONALE:Behavioral and dopamine responses to cocaine are sexually dimorphic: Female rats exhibit higher levels of locomotor and reward-associated behaviors after cocaine administration and dopamine release than do males. Activation of the dopamine- and cAMP-regulated phosphoprotein of Mr 32 kDa (DARPP-32) intracellul...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-008-1388-0

    authors: Zhou L,Nazarian A,Sun WL,Jenab S,Quinones-Jenab V

    更新日期:2009-03-01 00:00:00

  • Scopolamine-induced locomotor stimulation in mice: effect of diazepam and a benzodiazepine antagonist.

    abstract::The benzodiazepine diazepam and the benzodiazepine antagonist Ro 15-1788 were tested alone or in combination for their influence on scopolamine-induced locomotor stimulation in mice. The benzodiazepine antagonist had no effect by itself, but prevented the enhancement of scopolamine-induced locomotor stimulation produc...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00464583

    authors: Sansone M

    更新日期:1982-01-01 00:00:00