Naluzotan is an effective and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM. Naluzotan is used for the treatment of anxiety and depression and is also a weak hERG K+ channel blocker (IC50: 3800 nM).

Naluzotan behaves as a full agonist in an in vitro cell-based functional assay (EC50: 20 nM). Naluzotan has obviously affinity is the guinea pig sigma receptor (Ki = 100 nM). However, it does not inhibit cytochrome P450 isoforms (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4[1].

Naluzotan displays 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 rats, Naluzotan (3 mg/kg, p.o.) treatment, displays 11% oral bioavailability with a serum t1/2 of 2?3.5 h when administrated, attaining a Cmax level of 24 ± 13 ng/mL. In dogs, the pharmacokinetic profile of Naluzotan (3 mg/kg, p.o.) treatment, shows 16% oral bioavailability, a serum t1/2 of 1.1 h, and a Cmax level of 174 ± 141 ng/mL [1]. PRX-00023 (0.01-0.05 mg/kg, i.p.) significantly reduces USV rates but done of these doses produce sedation in rats[2].

740873-06-7

C23H38N4O3S

450.64

PRX 00023

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years