NLX-101（F-15599）|CAS 635323-95-4|DC Chemicals

Cas No.:	635323-95-4
Chemical Name:	NLX-101
Synonyms:	NLX-101; NLX 101; NLX101; F-15,599; F 15,599; F15,599; F15599
SMILES:	O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CN(C3=NC=C(C)C=N3)C)(F)CC2
Formula:	C₁₉H₂₁ClF₂N₄O
M.Wt:	394.85
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:

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].

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