| Identification | Back Directory | [Name]
NAD 299 Hydrochloride | [CAS]
184674-99-5 | [Synonyms]
NAD-299 HCl
Robalzotan (hydrochloride) | [Molecular Formula]
C18H24ClFN2O2 | [MDL Number]
MFCD00939873 | [MOL File]
184674-99-5.mol | [Molecular Weight]
354.85 |
| Hazard Information | Back Directory | [Uses]
NAD 299 Hydrochloride is a selective, high affinity 5-HT1A antagonist, used in psychotropic drug development. | [in vivo]
Robalzotan hydrochloride (1-100 μg/kg; i.v.) significantly increases the activity of such neurons at 5 μg/kg in rats, and reverses the acute inhibitory effect of citalopram (HY-121203) (300 μg/kg i.v.) or paroxetine (HY-122272) (100 μg/kg, i.v.) on the activity of 5-HT neurons in the dorsal raphe nucleus in rats[1].
Robalzotan hydrochloride (5, 50 μg/kg; i.v.) increases the firing rate of the 5-HT cells[1].
Robalzotan hydrochloride (2-100 μg/kg; i.v.) occupies 5-HT1A receptors in a dose-dependent in monkeys[2].
Robalzotan hydrochloride (0.3; 1 and 3 μmol/kg s.c) causes a dose-dependent increase of extracellular ACh levels in the rat FC[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. |
| [IC 50]
5-HT1A Receptor | [storage]
Desiccate at RT |
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