NAD 299 hydrochloride

Robalzotan hydrochloride (NAD-​299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system[1][2][3].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT1A Receptor

Robalzotan hydrochloride (1-100 µg/kg；i.v.) 在大鼠体内以 5 µg/kg 显着增加此类神经元的活性，并逆转 citalopram (HY-121203) (300 µg/kg i.v.) 或 paroxetine (HY-122272) (100 µg/kg， i.v.) 对大鼠中缝背核 5-HT神经元活性的影响[1]. Robalzotan hydrochloride (5, 50 µg/kg；静脉注射) 提高 5-HT 细胞的放电率[1]。 Robalzotan hydrochloride (2-100 µg/kg; i.v.) 在猴子体内以剂量依赖性方式占据 5-HT1A 受体[2]。 Robalzotan hydrochloride (0.3；1 和 3 µmol/kg 皮下注射) 引起大鼠 FC 细胞外 ACh 水平的剂量依赖性增加[3]。 Animal Model: 300-600 g, male Sprague-Dawley rats (5-HT cells)[1] Dosage: 1, 5, 12.5, 25, 50, 100 µg/kg Administration: I.v. Result: Significantly increased the activity of such neurons at 5 µg/kg, increasing doses of robalzotan 5-100 µg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons. Animal Model: 3-4 kg, cynomolgus monkeys[2] Dosage: 2, 10, 20, 100 µg/kg Administration: I.v. Result: Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.

[1]. Arborelius L, et al. The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. Eur J Pharmacol. 1999 Oct 8;382(2):133-8.  

[2]. Farde L, et al. PET-Determination of robalzotan (NAD-299) induced 5-HT(1A) receptor occupancy in the monkey brain. Neuropsychopharmacology. 2000 Apr;22(4):422-9.  

[3]. Hu, Xiao Jing, et al. Modulation of acetylcholine release by serotonergic 5-HT1A and 5-HT1B receptors : a microdialysis study in the awake rat. 2007.