Naluzotan

SKU: orb1706933

Description

Naluzotan (PRX-00023) is a potent and selective 5-HT1A receptor agonist (Ki ~5.1 nM) with anxiolytic and potential antidepressant properties, as evidenced in preclinical research. It also exhibits moderate hERG channel blockade (IC50 3800 nM). This small molecule is used in vitro and in vivo to study serotonin signaling, mood disorders, and cardiac safety pharmacology.

Research Area

Cardiovascular Research, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 740873-06-7
• MW: 450.64
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₃₈N₄O₃S
• SMILES: CC(=O)Nc1cccc(c1)N1CCN(CCCCNS(=O)(=O)CC2CCCCC2)CC1
• Target: EGFR,Potassium Channel,5-HT Receptor

Bioactivity

• Target IC50:
  Cell-based functional assay:20 nM (EC50)|ERG K+ channel (human):3800 nM|5-HT1A receptor:20 nM|5-HT1A receptor:5.1 nM (Ki)|σ receptor:100 nM (Ki,guinea pig)
• In Vivo:
  In rats, when administered orally, Naluzotan shows 11% oral bioavailability with a serum half-life (t1/2) of 2−3.5 hours, reaching a Cmax level of 24 ± 13 ng/mL (3 mg/kg, oral). Naluzotan exhibits significant brain penetration, with a brain:serum concentration ratio of approximately 0.5 in rats at 1 hour following either intravenous or oral administration, and it achieves a brain concentration approximately equivalent to that of buspirone. In dogs, the pharmacokinetic profile of naluzotan demonstrates 16% oral bioavailability, a serum t1/2 of 1.1 hours when administered orally, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, oral). PRX-00023, at doses of 0.01-0.05 mg/kg administered intraperitoneally, significantly reduces ultrasonic vocalization (USV) rates in rats, but none of these doses induce sedation.
• In Vitro:
  Naluzotan, with an EC50 of 20 nM, behaves as a full agonist in an in vitro cell-based functional assay. It exhibits significant affinity for the guinea pig sigma receptor (Ki = 100 nM) but does not inhibit cytochrome P450 isoforms (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4.

Storage & Handling

• Storage: store at low temperature | 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

5HT Receptor, 5-HT1A, 5HTReceptor, hERG Potassium Channel, Naluzotan, PRX00023, PRX-00023, PRX 00023

Compound Identifiers

PubChem CID

11430856