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F17464

Chemical Structure : F17464

CAS No.: 1268334-26-4

F17464 (F 17464)

Catalog No.: PC-47096Not For Human Use, Lab Use Only.

F17464 is a dopamine D 3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 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).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 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).
F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist.
F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. 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, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice

Physicochemical Properties

M.Wt 536.040
Formula C25H30ClN3O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-{4-[4-(8-Oxo-8H-[1,3]-dioxolo-[4,5-g]-chromen-7-yl)-butyl]-piperazin-1-yl}-phenyl)-methanesulfonamide, hydrochloride

References

1. Bitter I, et al. Neuropsychopharmacology. 2019 Oct;44(11):1917-1924.

2. Cosi C, et al. Eur J Pharmacol. 2021 Jan 5;890:173635.

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