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ChemicalBook--->CAS DataBase List--->184674-99-5

184674-99-5

184674-99-5 Structure

184674-99-5 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Desiccate at RT
[solubility ]

Soluble to 100 mM in water and to 100 mM in DMSO
[form ]

Powder
[color ]

White to off-white
Hazard InformationBack 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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