Vortioxetine (Lu AA21004) HBr 960203-27-4

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Molecular Weight:

379.36 Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

Biological Activity

Lu-AA21004 inhibits recombinant human CYP1A2, CYP2C9, CYP2D6 and CYP3A4
with IC50 of 40 μM, 39 μM, 9.8 μM and 10 μM, respectively. Lu AA21004 is a partial h5-HT1B receptor agonist with EC50 of 460 nM
and intrinsic activity of 22% using a whole-cell cAMP-based assay.

Lu
AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM and is a
functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an
in vitro whole-cell cAMP assay.


For Lu-AA21004 the hepatic clearances and oral bioavailabilities in rats
are found to be 7.1 (L/h)/kg and 16%. Lu-AA21004 (2.5 mg/kg, 5 mg/kg,
or 10 mg/kg sc) increases the extracellular levels of 5-HT in the
ventral hippocampus in conscious rats. Lu-AA21004 (5 mg/kg, or 10 mg/kg
sc) also results in significantly higher basal levels of 5-HT in the
medial prefrontal cortex (mPFC) after 3 days of treatment.

Lu-AA21004
occupies SERT by 43% and 57% after 3 days of treatment with 5 mg/kg or
10 mg/kg in the rat medial prefrontal cortex. Lu AA21004
dose-dependent occupies 5-HT1B receptor and the SERT with ED50 of 3.2
mg/kg and 0.4 mg/kg in rats one hour after subcutaneous administration.
Lu AA21004 affects the Bezold-Jarisch reflex in the rat dose
dependently, inhibiting transient bradycardia with ED50 of 0.11 mg/kg.

Lu AA21004 (2.5-10.0 mg/kg s.c.) increases extracellular levels of 5-HT,
DA, and NA in the medial prefrontal cortex and in the ventral
hippocampus in rats. Lu AA21004 (5 mg/kg s.c.) increases in the
extracellular levels of 5-HT (200%) in the ventral hippocampus of rats
with 41% occupancy at the SERT. Lu AA21004 (7.8 mg/kg s.c.)
significantly decreases the immobility time in the FSL rats but not in
the FRL rats.

Lu AA21004 (8.0 mg/kg p.o.) produces an increase in social
interaction as well as a small, but significant, increase in locomotor
activity in rats. Lu AA21004 (7.9 mg/kg s.c.) shows a dose-dependent
anxiolytic-like effect in the conditioned fear assay in rats. Vortioxetine (10 mg/kg) significantly increases freezing 60 min before
acquisition in male Sprague-Dawley rats, suggesting enhanced contextual
memory formation during acquisition and/or consolidation.

Vortioxetine
(5 mg/kg) also causes increased freezing rates during retention, an
effect that reached statistical significance by post hoc tests.
Vortioxetine (2.5 mg/kg or 5 mg/kg) prior to acquisition shows average
exploration times of 29s and 33s for the novel object, respectively.

Vortioxetine (10 mg/kg) significantly reduces nociception in rats,
assessed as increased paw withdrawal latency. Vortioxetine at 5 and 10
mg/kg increases the levels of ACh to 224% and 204% of baseline 20 min
after injection.

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Product Categories : Neuronal Signaling > 5-HT Receptor Inhibitor