Naluzotan 是一种新颖的，有效的，选择性的 5-HT1A 激动剂，IC₅₀ 和 K_i 值分别为约 20 nM 和 5.1 nM；同时是 hERG K⁺ 通道阻滞剂，IC₅₀ 值为 3800 nM，常用于焦虑和抑郁症的研究。

Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC 50 and K i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K channel blocker, with IC 50 of 3800 nM.

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5-HT1A Receptor 20 nM (IC50) 5-HT1A Receptor

Naluzotan behaves as a full agonist in an in vitro cell-based functional assay with an EC50 of 20 nM. Naluzotan 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. has not independently confirmed the accuracy of these methods. They are for reference only.

In rats Naluzotan shows 11% oral bioavailability with a serum t 1/2 of 2?3.5 h when administrated po, attaining a C max level of 24 ± 13 ng/mL (3 mg/kg, po). Naluzotan 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 shows 16% oral bioavailability, a serum t 1/2 of 1.1 h po, and a C max 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. 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.
[2]. 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.