Naluzotan hydrochloride

SKU: orb1819153

Description

Naluzotan hydrochloride (PRX 00023 hydrochloride) is a potent and selective 5-HT1A receptor agonist (Ki ~5.1 nM) and a hERG K+ channel blocker (IC50 3800 nM). It is a research compound used in preclinical studies investigating anxiety and depression, including in vitro receptor binding assays and in vivo behavioral models.

Research Area

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

Key Properties

• CAS Number: 740873-82-9
• MW: 487.1
• Purity: 99.96% (May vary between batches)
• Formula: C₂₃H₃₉ClN₄O₃S
• SMILES: Cl.O=C(NC1=CC=CC(=C1)N2CCN(CC2)CCCCNS(=O)(=O)CC3CCCCC3)C
• Target: EGFR,Potassium Channel,5-HT Receptor
• Solubility: DMSO:50 mg/mL (102.65 mM)

Bioactivity

• Target IC50:
  ERG K+ (human):3800 nM|5-HT1A:20 nM|5-HT1A:5.1 nM
• In Vivo:
  In rats Naluzotan hydrochloride shows 11% oral bioavailability with a serum t1/2 of 2−3.5 h when administrated po, attaining a Cmax level of 24 ± 13 ng/mL (3 mg/kg, po). Naluzotan hydrochloride shows significant brain penetration, achieving a brain:serum concentration ratio of approximately 0.5 in the rat at 1 h following either intravenous or oral administration and reaching brain concentration approximately equivalent to that of buspirone. In dogs the pharmacokinetic profile of Naluzotan hydrochloride shows 16% oral bioavailability, a serum t1/2 of 1.1 h po, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, po). PRX-00023 (0.01-0.05 mg/kg, i.p.) significantly reduces USV rates, but done of these doses produce sedation in rats.
• In Vitro:
  Naluzotan hydrochloride behaves as a full agonist in an in vitro cell-based functional assay with an EC50 of 20 nM. Naluzotan hydrochloride has significant affinity is 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: 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, 5HTReceptor, 5-HT1A, Naluzotan Hydrochloride, hERG Potassium Channel, PRX00023 Hydrochloride, PRX-00023 Hydrochloride, PRX 00023 hydrochloride, PRX 00023 Hydrochloride

Compound Identifiers

PubChem CID

25096194