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- W3093352009 abstract "F17464 (N-(3-{4-[4-(8-Oxo-8H-[1,3]-dioxolo-[4,5-g]-chromen-7-yl)-butyl]-piperazin-1-yl}-phenyl)-methanesulfonamide, hydrochloride) is a new potential antipsychotic with a unique profile. The compound exhibits high affinity for the human dopamine receptor subtype 3 (hD3) (Ki = 0.17 nM) and the serotonin receptor subtype 1a (5-HT1a) (Ki = 0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki = 8.9 and 12.1 nM, respectively). [14C]F17464 dynamic studies show a slower dissociation rate from hD3 receptor (t1/2 = 110 min) than from hD2s receptor (t1/2 = 1.4 min) and functional studies demonstrate that F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist. In human dopaminergic neurons F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated. In vivo F17464 target engagement of both D2 and 5-HT1a receptors is demonstrated in displacement studies in the mouse brain. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain - dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions. F17464 also rescues valproate induced impairment in a rat social interaction model of autism. All the neurochemistry and behavioural effects of F17464 are observed in the dose range 0.32–2.5 mg/kg i.p. in both rats and mice. The in vitro - in vivo pharmacology profile of F17464 in preclinical models is discussed in support of a therapeutic use of the compound in schizophrenia and autism." @default.
- W3093352009 created "2020-10-22" @default.
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- W3093352009 date "2021-01-01" @default.
- W3093352009 modified "2023-10-01" @default.
- W3093352009 title "Pharmacology profile of F17464, a dopamine D3 receptor preferential antagonist" @default.
- W3093352009 cites W1482174726 @default.
- W3093352009 cites W1592385480 @default.
- W3093352009 cites W1935860113 @default.
- W3093352009 cites W1964176367 @default.
- W3093352009 cites W1965196644 @default.
- W3093352009 cites W1966173192 @default.
- W3093352009 cites W1967332436 @default.
- W3093352009 cites W1976347553 @default.
- W3093352009 cites W1977764783 @default.
- W3093352009 cites W1984919926 @default.
- W3093352009 cites W1987279025 @default.
- W3093352009 cites W1991360875 @default.
- W3093352009 cites W1992930613 @default.
- W3093352009 cites W1997257761 @default.
- W3093352009 cites W2002495110 @default.
- W3093352009 cites W2007760893 @default.
- W3093352009 cites W2008849361 @default.
- W3093352009 cites W2013333057 @default.
- W3093352009 cites W2015465857 @default.
- W3093352009 cites W2021280871 @default.
- W3093352009 cites W2026961963 @default.
- W3093352009 cites W2037938599 @default.
- W3093352009 cites W2038445102 @default.
- W3093352009 cites W2039383065 @default.
- W3093352009 cites W2042713000 @default.
- W3093352009 cites W2043434584 @default.
- W3093352009 cites W2043514528 @default.
- W3093352009 cites W2049437018 @default.
- W3093352009 cites W2051289332 @default.
- W3093352009 cites W2053909439 @default.
- W3093352009 cites W2060554610 @default.
- W3093352009 cites W2061359205 @default.
- W3093352009 cites W2077760177 @default.
- W3093352009 cites W2080277334 @default.
- W3093352009 cites W2084087776 @default.
- W3093352009 cites W2102974182 @default.
- W3093352009 cites W2107387295 @default.
- W3093352009 cites W2108798732 @default.
- W3093352009 cites W2120935254 @default.
- W3093352009 cites W2127272758 @default.
- W3093352009 cites W2128717592 @default.
- W3093352009 cites W2133608824 @default.
- W3093352009 cites W2134918392 @default.
- W3093352009 cites W2137044087 @default.
- W3093352009 cites W2150382103 @default.
- W3093352009 cites W2166214376 @default.
- W3093352009 cites W2167223183 @default.
- W3093352009 cites W2167531441 @default.
- W3093352009 cites W2177873964 @default.
- W3093352009 cites W2188805245 @default.
- W3093352009 cites W2276857175 @default.
- W3093352009 cites W2305304932 @default.
- W3093352009 cites W2325014163 @default.
- W3093352009 cites W2325132056 @default.
- W3093352009 cites W2325615500 @default.
- W3093352009 cites W2328543694 @default.
- W3093352009 cites W2460049929 @default.
- W3093352009 cites W2509180953 @default.
- W3093352009 cites W2581158021 @default.
- W3093352009 cites W2586914431 @default.
- W3093352009 cites W2617228775 @default.
- W3093352009 cites W2731817207 @default.
- W3093352009 cites W2734335552 @default.
- W3093352009 cites W2735454576 @default.
- W3093352009 cites W2745925584 @default.
- W3093352009 cites W2753654430 @default.
- W3093352009 cites W2767956701 @default.
- W3093352009 cites W2768304164 @default.
- W3093352009 cites W2768542634 @default.
- W3093352009 cites W2783300428 @default.
- W3093352009 cites W2788671315 @default.
- W3093352009 cites W2803420227 @default.
- W3093352009 cites W2803666287 @default.
- W3093352009 cites W2806100246 @default.
- W3093352009 cites W2886986075 @default.
- W3093352009 cites W2891938205 @default.
- W3093352009 cites W2895043322 @default.
- W3093352009 cites W2897661347 @default.
- W3093352009 cites W2899269924 @default.
- W3093352009 cites W2906768105 @default.
- W3093352009 cites W2908214697 @default.
- W3093352009 cites W2913278138 @default.