184674-99-5
184674-99-5 structure
- Name: NAD 299 hydrochloride
- Chemical Name: (3R)-3-(Dicyclobutylamino)-8-fluoro-5-chromanecarboxamide hydrochloride (1:1)
- CAS Number: 184674-99-5
- Molecular Formula: C18H24ClFN2O2
- Molecular Weight: 354.847
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2021-01-20 10:31:09
- Modify Date: 2024-01-14 09:13:09
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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].
| Name | (3R)-3-(Dicyclobutylamino)-8-fluoro-5-chromanecarboxamide hydrochloride (1:1) |
|---|---|
| Synonyms |
(3R)-3-(Dicyclobutylamino)-8-fluoro-5-chromanecarboxamide hydrochloride (1:1)
2H-1-Benzopyran-5-carboxamide, 3-(dicyclobutylamino)-8-fluoro-3,4-dihydro-, (3R)-, hydrochloride (1:1) (3R)-3-(Dicyclobutylamino)-8-fluorochromane-5-carboxamide hydrochloride (1:1) |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
5-HT1A Receptor |
| In Vivo | 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. |
| References |
| Molecular Formula | C18H24ClFN2O2 |
|---|---|
| Molecular Weight | 354.847 |
| Exact Mass | 354.151031 |