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Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
SB-277011-A (trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolininecarboxamide), is a brain-penetrant, high-affinity, and selective dopamine D(3) receptorExpand
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Behavioural and pharmacokinetic studies on nicotine, cytisine and lobeline
Previous work has suggested that cytisine and lobeline are of low potency in producing nicotine-like behavioural effects, despite having some nicotine-like peripheral effects and potently inhibitingExpand
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Attenuation of haloperidol‐induced catalepsy by a 5‐HT2C receptor antagonist
Atypical neuroleptics produce fewer extrapyramidal side‐effects (EPS) than typical neuroleptics. The pharmacological profile of atypical neuroleptics is that they have equivalent or higher antagonistExpand
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LPA1 receptor-deficient mice have phenotypic changes observed in psychiatric disease
Several psychiatric diseases, including schizophrenia, are thought to have a developmental aetiology, but to date no clear link has been made between psychiatric disease and a specific developmentalExpand
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SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety
SB-243213 (5-methyl-1-[[-2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline hydrochloride) is a new, selective 5-hydroxytryptamine (5-HT)2C receptor inverse agonist. SB-243213Expand
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Long-term evaluation of isolation-rearing induced prepulse inhibition deficits in rats: an update
RationaleRats reared in social isolation from weaning show prepulse inhibition (PPI) deficits which are thought to model the sensorimotor gating deficits seen in schizophrenia and other psychiatricExpand
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High affinity binding of [3H] (−)-nicotine to rat brain membranes and its inhibition by analogues of nicotine
Analysis of the characteristics of cerebral binding of [3H] (-)-nicotine revealed a single population of sites with high affinity (KD = 6.0 +/- 0.6 nM). The regional distribution of the binding ofExpand
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Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with
A selective dopamine D(3) receptor antagonist offers the potential for an effective antipsychotic therapy, free of the serious side effects of currently available drugs. Using clearance and brainExpand
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Localization of serotonin-4 receptors in the striatonigral pathway in rat brain
Rats were injected unilaterally with 6-hydroxydopamine either in the medial forebrain bundle or in the dorsolateral substantia nigra. Another group was injected unilaterally with kainate in theExpand
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Pharmacological characterization of the discriminative stimulus properties of the dopamine D1 agonist, SKF 81297
A range of selective dopamine Dl and D2 receptor agonists and antagonists was used to characterize the discriminative stimuli produced by d-amphetamine (0.5 mg/kg) and the Dl agonist SKF 81297 (0.1Expand
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