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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
PRX 00023
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
740873-06-7
- 规格：
1 mg
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Naluzotan
CAS No. : 740873-06-7
MCE 国际站：Naluzotan
产品活性：Naluzotan 是一种新颖的，有效的，选择性的 5-HT1A 激动剂，IC50 和 Ki 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。
研究领域：GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel
作用靶点：5-HT Receptor | Potassium Channel
In Vitro: 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.
In Vivo: In rats Naluzotan 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 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 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.
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