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Naluzotan

Catalog No. T16265   CAS 740873-06-7
Synonyms: PRX 00023

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

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Naluzotan Chemical Structure
Naluzotan, CAS 740873-06-7
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1 mg In stock $ 700.00
5 mg In stock $ 1,800.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.
Targets&IC50 Cell-based functional assay:20 nM (EC50), 5-HT1A receptor:20 nM, 5-HT1A receptor:5.1 nM (Ki), σ receptor:100 nM (Ki,guinea pig), ERG K+ channel (human):3800 nM
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[2].
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)[1]. 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[1].
Synonyms PRX 00023
Molecular Weight 450.64
Formula C23H38N4O3S
CAS No. 740873-06-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Brunelli SA, et al. PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety. Pharmacol Biochem Behav. 2009 Nov;94(1):8-15. 2. Becker OM, et al. An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. J Med Chem. 2006 Jun 1;49(11):3116-35.

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Keywords

Naluzotan 740873-06-7 Angiogenesis GPCR/G Protein JAK/STAT signaling Neuroscience Tyrosine Kinase/Adaptors EGFR 5-HT Receptor PRX 00023 PRX00023 PRX-00023 inhibitor inhibit

 

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