Vortioxetine hydrobromide

SKU: orb1305547

Description

Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a multimodal serotonergic agent acting as a serotonin transporter (SERT) inhibitor and a modulator of several 5-HT receptor subtypes. This pharmacological profile makes it a valuable research tool for investigating mood disorders, cognitive function, and neuropharmacology in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 960203-27-4
• MW: 379.36
• Purity: 99.98%
• Formula: C₁₈H₂₂N₂S·HBr
• SMILES: c1c(c(cc(c1)C)C)Sc1ccccc1N1CCNCC1.Br
• Target: Serotonin Transporter,5-HT Receptor
• Solubility: Ethanol:14 mg/mL (36.9 mM);DMSO:45 mg/mL (118.62 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.27 mM)

Bioactivity

• Target IC50:
  5-HT7:19nM|5-HT11B:33nM|SERT:1.6nM|5-HT13A:3.7nM|5-HT1A:15nM
• In Vivo:
  Lu AA21004 acts as an agonist for the h5-HT1B receptor, with an EC50 value of 460 nM and demonstrating 22% intrinsic activity in whole-cell assays. It inhibits recombinant human cytochrome P450 enzymes CYP1A2, CYP2C9, CYP2D6, and CYP3A4 with IC50 values of 40 μM, 39 μM, 9.8 μM, and 10 μM, respectively. Furthermore, Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM in vitro whole-cell cAMP assays and functions as a competitive antagonist with an IC50 of 2 μM.
• In Vitro:
  Subcutaneous injection of Lu AA21004 (2.5-10.0 mg/kg) into the medial prefrontal cortex and ventral hippocampal area of rats was found to elevate extracellular levels of 5-HT, DA, and NA. A specific dose of Lu AA21004 (5 mg/kg) targeting the rats’ ventral hippocampal region resulted in a 200% increase in extracellular 5-HT levels. Additionally, administration of Lu AA21004 (at doses of 5 and 10 mg/kg) showed a significant elevation in ACh levels to 224% and 204% respectively, 20 minutes post-injection. This compound, when administered to the ventral hippocampal area of awake rats at doses of 5 and 10 mg/kg, enhanced extracellular 5-HT levels, and a 3-day treatment of the medial prefrontal cortex with Lu-AA21004 (at 5 and 10 mg/kg) substantially raised the basal levels of 5-HT. Furthermore, Lu AA21004 (10 mg/kg) notably decreased pain perception in rats. In terms of pharmacokinetics within rats, Lu-AA21004 exhibited a liver clearance rate of 7.1 (L/h)/kg and an oral bioavailability of 16%. Lastly, Lu AA21004 dose-dependently affected the rats' Bezold-Jarisch reflex by inhibiting transient bradycardia (ED50: 0.11 mg/kg).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-hydroxytryptamine Receptor, 5-HTT, 5HTReceptor, 5HT Receptor, 5-HT7, 5-HT3A, 5-HT1A, 5-HT Receptor, 5-HT1B, Inhibitor, inhibit, Lu AA 21004, Lu AA 21004 Hydrobromide, Lu AA21004, Lu AA-21004, Lu AA21004 hydrobromide, Lu AA21004 Hydrobromide, Lu AA-21004 Hydrobromide, SLC6A4, SERT, Serotonin Receptor, Serotonin Transporter, SerotoninTransporter, Vortioxetine, Vortioxetine (Lu AA21004) HBr, Vortioxetine HBr, Vortioxetine hydrobromide, Vortioxetine Hydrobromide

Compound Identifiers

PubChem CID

56843850