Abstract:
OBJECTIVE:The pharmacological profile of escitalopram, the S-(+)-enantiomer of citalopram, was studied and compared with citalopram and the R-(-)-enantiomer, R-citalopram. METHODS:Inhibition of the serotonin transporter (5-HTT) was studied in COS-1 cells expressing the human 5-HTT (h-5-HTT) and in rat brain synaptosomes. In vitro selectivity was studied relative to noradrenaline transporter (NAT) and dopamine transporter (DAT) function in rat brain synaptosomes, and affinities for other binding sites were determined. In vivo 5-HT activity was measured as inhibition of neuronal firing rate in rat dorsal raphe nucleus (DRN) and enhancement of 5-hydroxytryptophan (5-HTP)-induced behaviour (mouse and rat). Furthermore, studies were conducted in models of antidepressant (mouse forced-swim test), anxiolytic [foot-shock-induced ultrasonic vocalization (USV) in adult rats and mouse black and white box] and anti-aggressive activity (socially isolated mice). RESULTS:Escitalopram inhibited 5-HTT functions approximately 2 times more potently than citalopram and at least 40 times more potently than R-citalopram. Escitalopram showed insignificant activity at other monoamine transporters and 144 other binding sites. Escitalopram inhibited 5-HT neuronal firing in DRN and potentiated 5-HTP-induced behaviours more potently than citalopram; R-citalopram was inactive. Escitalopram and citalopram, but not R-citalopram, reduced forced-swimming-induced immobility and facilitated exploratory behaviour in the black and white box. Escitalopram and citalopram inhibited USV potently; R-citalopram was several times less potent. Escitalopram, citalopram and R-citalopram inhibited aggressive behaviour weakly. Escitalopram and citalopram had very potent anti-aggressive effects when co-administered with l-5-HTP. CONCLUSION:Escitalopram is a very selective 5-HT reuptake inhibitor. It is more potent than its racemate citalopram and is effective in animal models predictive of antidepressant and anxiolytic activities.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Sánchez C,Bergqvist PB,Brennum LT,Gupta S,Hogg S,Larsen A,Wiborg Odoi
10.1007/s00213-002-1364-zsubject
Has Abstractpub_date
2003-06-01 00:00:00pages
353-62issue
4eissn
0033-3158issn
1432-2072journal_volume
167pub_type
杂志文章abstract:RATIONALE:The purpose of the present investigation was to evaluate the effects of the D3 agonist (+/-)-7-hydroxy-dipropylaminotetralin (7-OH-DPAT), various dopamine (DA) agonists and DA antagonists on the antinociceptive effects of mu opioids. METHODS:Antinociception was assessed using a warm-water tail-withdrawal pro...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050999
更新日期:1999-06-01 00:00:00
abstract::The mesolimbic dopamine (DA) system has been implicated in conditioned reward (CR), locomotor sensitization, and the reinforcing properties of psychomotor stimulants. Stimuli with formerly motivationally neutral properties that gain incentive properties by their predictive association with primary reinforcers are term...
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pub_type: 杂志文章
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更新日期:1999-02-01 00:00:00
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journal_title:Psychopharmacology
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更新日期:2014-11-01 00:00:00
abstract::A novel self-stimulation methodology involving a fixed-interval (FI-5 s) schedule of reinforcement, microanalysis and threshold evaluation was used to investigate the effects of cocaine on rats lever pressing for electrical stimulation of the prefrontal cortex. Cocaine (15 mg/kg) increased medial prefrontal cortex (MP...
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doi:10.1007/BF02801979
更新日期:1992-01-01 00:00:00
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更新日期:2006-03-01 00:00:00
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pub_type: 杂志文章
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更新日期:1993-01-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2003-12-01 00:00:00
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pub_type: 已发布勘误
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更新日期:2011-02-01 00:00:00
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journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
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更新日期:1984-01-01 00:00:00
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pub_type: 临床试验,杂志文章
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更新日期:2003-08-01 00:00:00
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pub_type: 杂志文章
doi:10.1007/s00213-007-0908-7
更新日期:2007-12-01 00:00:00
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pub_type: 杂志文章
doi:10.1007/BF00427106
更新日期:1981-01-01 00:00:00
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pub_type: 杂志文章,随机对照试验
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更新日期:2020-06-01 00:00:00
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更新日期:2002-06-01 00:00:00
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更新日期:1985-01-01 00:00:00
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journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050811
更新日期:1999-01-01 00:00:00
abstract::The novel dopamine autoreceptor antagonists (-)-DS 121 and (+)-UH 232 were tested for their ability to alter cocaine self-administration behavior in rats reinforced on a progressive ratio (PR) schedule. (-)-DS 121 (15 mg/kg) and (+)-UH 232 (30 mg/kg) produced significant decreases in breaking point. (-)-DS 121 produce...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02246149
更新日期:1995-07-01 00:00:00
abstract:RATIONALE:Many of the biochemical, physiological, and behavioral effects of ethanol are known to be mediated by ionotropic glutamate receptors. Emerging evidence implicates metabotropic glutamate receptors (mGluRs) in the biobehavioral effects of ethanol and other drugs of abuse, but there is little information regardi...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-005-0217-y
更新日期:2006-01-01 00:00:00
abstract::Serotonin receptors of the 5HT2 type were labeled on platelet membranes using tritiated ketanserin. Blood was collected from the umbilical cord of newborns and venous samples were collected from 6-year-old children as well as junior-high and high school students (ages 13 through 18) to determine age-related changes in...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02245309
更新日期:1992-01-01 00:00:00
abstract::The capacity of the specific narcotic antagonists naltrexone and naloxone to block the discriminative effects produced by morphine in the rat were evaluated using a two-choice, discrete-trial avoidance task. The antagonists produced a dose-dependent and time-dependent blockade of morphine's effects as measured by resp...
journal_title:Psychopharmacology
pub_type: 杂志文章
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更新日期:1976-11-10 00:00:00
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journal_title:Psychopharmacology
pub_type: 杂志文章,评审
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更新日期:2005-06-01 00:00:00
abstract::ApolipoproteinE (ApoE) genotype has recently been identified as a major risk factor for Alzheimer's disease (AD) but the mechanism(s) by which ApoE isoforms influence this disease remain unclear. Recent studies suggest that mice deficient in ApoE may exhibit impaired central cholinergic function. Since this neurotrans...
journal_title:Psychopharmacology
pub_type: 杂志文章
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更新日期:1997-07-01 00:00:00
abstract::In the studies reported here, we investigated the effects of nicotine on memory for unrelated word lists. Nicotine was delivered through cigarette smoking, and memory performance was assessed using both intentional and incidental recall tasks, and employing an additional, indirect measure of memory. We report the resu...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02245856
更新日期:1995-06-01 00:00:00