Search Results - "Peglion, Jean Louis"
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Synthesis of Benzocyclobutenes by Palladium-Catalyzed C−H Activation of Methyl Groups: Method and Mechanistic Study
Published in Journal of the American Chemical Society (12-11-2008)“…An efficient catalytic system has been developed for the synthesis of benzocyclobutenes by C−H activation of methyl groups. The optimal conditions employed a…”
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Characterization of the Annonaceous acetogenin, annonacinone, a natural product inhibitor of plasminogen activator inhibitor-1
Published in Scientific reports (23-11-2016)“…Plasminogen activator inhibitor-1 (PAI-1) is the main inhibitor of the tissue type and urokinase type plasminogen activators. High levels of PAI-1 are…”
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Synthetic efforts toward the synthesis of octalactins
Published in Tetrahedron (09-06-2008)“…Octalactin B was synthesized from the commercially available methyl-3-butenoate and isobutyraldehyde, using enantioselective allyl- and crotyltitanations to…”
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The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis
Published in The Journal of pharmacology and experimental therapeutics (01-10-2004)“…These studies examined the influence of the selective 5-hydroxytryptamine (serotonin) (5-HT)(1A) receptor partial agonist S15535…”
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In Vivo Quantification of Myocardial Dihydropyridine Binding Sites: A PET Study in Dogs
Published in The Journal of nuclear medicine (1978) (01-09-2002)“…Abnormalities in myocardial L-type Ca(2+) channel abundance and function have been described in cardiac hypertrophy and failure. In vivo quantification of the…”
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S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
Published in The Journal of pharmacology and experimental therapeutics (01-08-2001)“…S33005 displayed marked affinity for native, rat, and cloned human serotonin (5-HT) transporters (SERT) and less pronounced affinity for norepinephrine (NE)…”
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Differential influence of selective 5-HT5A vs 5-HT1A , 5-HT1B , or 5-HT2C receptor blockade upon light-induced phase shifts in circadian activity rhythms: Interaction studies with citalopram
Published in European neuropsychopharmacology (01-12-2009)“…Abstract Though serotonergic mechanisms modulate circadian rhythms, roles of individual serotonin (5-HT) receptors remain uncertain since data are lacking for…”
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S33005, a novel ligand at both serotonin and norepinephrine transporters: II. Behavioral profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
Published in The Journal of pharmacology and experimental therapeutics (01-08-2001)“…Reflecting its potent inhibition of serotonin (5-HT) reuptake (accompanying paper), S33005 blocked spontaneous tail-flicks induced by parachloroamphetamine in…”
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Anti-Ischemic Effects of Ivabradine, a Selective Heart Rate-Reducing Agent, in Exercise-Induced Myocardial Ischemia in Pigs
Published in Journal of cardiovascular pharmacology (01-11-2003)“…The effects of ivabradine, a novel heart rate-reducing agent that inhibits the cardiac pacemaker current If, were compared with those of the β-adrenergic…”
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Modulations of the amide function of the preferential dopamine D3 agonist (R,R)-S32504 : Improvements of affinity and selectivity for D3 versus D2 receptors
Published in Bioorganic & medicinal chemistry letters (15-04-2009)“…Starting with the preferential dopamine (DA) D(3) agonist S32504, we prepared two series of derivatives of the general formula I-A and I-B, in an effort to…”
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Highly efficient synthesis of [11C]S12968 and [11C]S12967, for the in vivo imaging of the cardiac calcium channels using PET
Published in Journal of labelled compounds & radiopharmaceuticals (01-06-2001)“…The dihydrophyridines S12968 ((−)‐S11568, absolute configuration S) and S12967 ((+)‐S11568, absolute configuration R), 3‐ethyl 5‐methyl…”
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5-HT2C receptors mediate penile erections in rats : actions of novel and selective agonists and antagonists
Published in European journal of pharmacology (23-04-1997)“…The mixed 5-HT2A/5-HT2B/5-HT2C receptor agonist, m-(chlorophenyl)piperazine (mCPP), elicited penile erections in rats, an action mimicked by the selective…”
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Stereospecific in vitro and in vivo effects of the new sinus node inhibitor (+)-S 16257
Published in European journal of pharmacology (19-11-1997)“…The effects of the two isomers, (+)-S 16257 and (−)-S 16260, of a new bradycardic agent, (±)-S 15544 (7,8-dimethoxy 3-{3-{[(4,5-dimethoxybenzocyclobutan-1-yl)…”
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S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole
Published in The Journal of pharmacology and experimental therapeutics (01-06-2004)“…In forced-swim tests in mice and rats, the novel D(3)/D(2) receptor agonist S32504…”
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S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity in comparison to ropinirole
Published in The Journal of pharmacology and experimental therapeutics (01-06-2004)“…These studies evaluated the potential antiparkinsonian properties of the novel dopamine D(3)/D(2) receptor agonist S32504 [(+)-trans-3,4,4a,5,6,…”
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S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole
Published in The Journal of pharmacology and experimental therapeutics (01-06-2004)“…S32504 [(+)-trans-3,4,4a,5,6,10b-hexahydro-9-carbamoyl-4-propyl-2H-naphth[1,2-b]-1,4-oxazine] displayed marked affinity for cloned, human (h)D(3) receptors…”
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Modulation of mesolimbic dopamine release by the selective dopamine D3 receptor antagonist, (+)-S 14297
Published in European journal of pharmacology (24-11-1994)“…In Chinese hamster ovary cells stably transfected with recombinant rat dopamine D2 or D3 receptors, the naphthofurane antagonist, (+)-S 14297…”
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Synthesis of spiro[quinoline-2,4′-piperidines] Heck versus radical reaction
Published in Tetrahedron letters (07-05-1998)“…The synthesis of spiro[quinoline-2,4′-piperidines] by using a radical or a Heck reaction, as the key step, is described. Allylamino or propargylamino…”
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S 14297, a novel selective ligand at cloned human dopamine D3 receptors, blocks 7-OH-DPAT-induced hypothermia in rats
Published in European journal of pharmacology (01-08-1994)“…The selective dopamine D3 receptor agonist, 7-OH-DPAT ((+)-7-hydroxy-2-(di-n-propylamino)tetralin) and the novel naphthofurane, S 14297…”
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