ChemicalBook--->CAS DataBase List--->635323-95-4

635323-95-4

635323-95-4 Structure

635323-95-4 Structure
IdentificationBack Directory
[Name]

F-15599
[CAS]

635323-95-4
[Synonyms]

F15
F-15
F 15
NLX101
NLX-101
F-15599
NLX 101
NLX-101 F-15599
NLX-101; NLX 101; NLX101; F-15;599; F 15;599; F15;599; F15599
(3-CHLORO-4-FLUOROPHENYL)-[4-FLUORO-4-[[(5-METHYLPYRIMIDIN-2-YL)METHYLAMINO]METHYL]PIPERIDIN-1-YL]METHANONE
Methanone, (3-chloro-4-fluorophenyl)[4-fluoro-4-[[[(5-methyl-2-pyrimidinyl)methyl]amino]methyl]-1-piperidinyl]-
[Molecular Formula]

C19H21ClF2N4O
[MDL Number]

MFCD28502284
[MOL File]

635323-95-4.mol
[Molecular Weight]

394.85
Chemical PropertiesBack Directory
[Melting point ]

195 °C
[Boiling point ]

534.7±50.0 °C(Predicted)
[density ]

1.33±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO:200.0(Max Conc. mg/mL);506.5(Max Conc. mM)
[form ]

Solid
[pka]

8.20±0.20(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
Hazard InformationBack Directory
[Uses]

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
[in vivo]

F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID), without affecting motor performance of rats. Rats treated with F15599 manifest less LID and mild 5-HT syndrome with the high dose of 30 μg/μL[1]. F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p,) results in a significant and dose-dependent (MED?=?0.125 mg/kg) delay in the latency to attack, and a potent reduction (ID50?=?0.095 mg/kg) in the amount of aggressive behaviour directed towards the intruder rat. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement[2]. F15599 increases the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 μg/kg i.v and reduces that of dorsal raphe 5-hydroxytryptaminergic neurones at doses >10-fold higher (minimal effective dose 8.2 μg/kg i.v.). F15599 increases dopamine output in mPFC (an effect dependent on the activation of postsynaptic 5-HT1A receptors) with an ED50 of 30 μg/kg i.p., whereas it reduces hippocampal 5-HT release (an effect dependent exclusively on 5-HT1A autoreceptor activation) with an ED50 of 240 μg/kg i.p[3].

[IC 50]

5-HT1A Receptor: 3.4 nM (Ki)
[References]

[1] Meadows SM, et al. Characterizing the differential roles of striatal 5-HT1A auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia. Exp Neurol. 2017 Jun;292:168-178. DOI:10.1016/j.expneurol.2017.03.013
[2] de Boer SF, et al. Anti-aggressive effects of the selective high-efficacy 'biased' 5-HT?A receptor agonists F15599 and F13714 in male WTG rats. Psychopharmacology (Berl). 2016 Mar;233(6):937-47. DOI:10.1007/s00213-015-4173-x
[3] Lladó-Pelfort L, et al. Preferential in vivo action of F15599, a novel 5-HT(1A) receptor agonist, at postsynaptic 5-HT(1A) receptors. Br J Pharmacol. 2010 Aug;160(8):1929-40. DOI:10.1111/j.1476-5381.2010.00738.x
Spectrum DetailBack Directory
[Spectrum Detail]

F-15599(635323-95-4)1HNMR
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