| Identification | Back Directory | [Name]
Robalzotan | [CAS]
169758-66-1 | [Synonyms]
NAD 299
AZD7371
AZD-7371
AZD 7371
Robalzotan
Unii-I18m56ogme
NAD299; NAD-299
Robalzotan [inn]
NAD 299 hydrochlorid
NAD 299 hydrochloride
NAD 299 hydrochloride (Robalzotan)
(R)-3-(DicyclobutylaMino)-8-fluorochroMan-5-carboxaMide
(3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide
2H-1-Benzopyran-5-carboxamide, 3-(dicyclobutylamino)-8-fluoro-3,4-dihydro-, (3R)-
(3R)-3-(Dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamidehydrochloride | [Molecular Formula]
C18H23FN2O2 | [MOL File]
169758-66-1.mol | [Molecular Weight]
318.39 |
| Chemical Properties | Back Directory | [Boiling point ]
429.9±45.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Desiccate at RT | [pka]
15.72±0.40(Predicted) |
| Hazard Information | Back Directory | [Uses]
NAD 299 Hydrochloride is a selective, high affinity 5-HT1A antagonist, used in psychotropic drug development. | [Biological Activity]
Selective, high affinity 5-HT 1A receptor antagonist (K i = 0.6 nM in vitro ). | [in vivo]
Robalzotan (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 (5, 50 μg/kg; i.v.) increases the firing rate of the 5-HT cells[1].
Robalzotan (2-100 μg/kg; i.v.) occupies 5-HT1A receptors in a dose-dependent in monkeys[2].
Robalzotan (0.3; 1 and 3 μmol/kg s.c) causes a dose-dependent increase of extracellular ACh levels in the rat FC[3]. | [IC 50]
5-HT1A Receptor |
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