Robalzotan hydrochloride  (Synonyms: 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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

354.85

C₁₈H₂₄ClFN₂O₂

184674-99-5

O=C(C1=C2C[C@@H](N(C3CCC3)C4CCC4)COC2=C(F)C=C1)N.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.