RS-102221 

RS-102221 is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats^[1][2].

RS-102221 (0.3-300nM; 24 h) promotes the differentiation of adult hippocampal neural precursor cells (ahNPCs) and significantly increases the percentage of MAP-2⁺ cells^[1].

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

RS-102221 (2 mg/kg; i.p.; once daily for 14 d) increases food-intake and weight-gain in rats^[2].
RS-102221 (2 mg/kg; i.p.; single dose), combined with the 3,4-Methylenedioxy-N-methamphetamine (MDMA or 'ecstasy'), suppresses the MDMA-induced hypophagia for the first 1 h period, and also suppresses MDMA-induced hyperlocomotion in mice^[3].
RS-102221 (2 mg/kg; i.p.; single dose) can reduce anxiety and reduce the amplitude of startle reflex in mice in light and dark test^[4].

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

612.62

C₂₇H₃₁F₃N₄O₇S

185376-97-0

O=S(C1=CC=C(C(F)(F)F)C=C1)(NC2=CC(C(CCCCN(CC3)CCC3(NC(N4)=O)C4=O)=O)=C(OC)C=C2OC)=O

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• [1]. Bortolotto V, et al. Proneurogenic Effects of Trazodone in Murine and Human Neural Progenitor Cells. ACS Chem Neurosci. 2017 Sep 20;8(9):2027-2038.  [Content Brief]

  [2]. Bonhaus DW, et al. RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):621-9.  [Content Brief]

  [3]. Salzer I, et al. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca(2+)-activated chloride channels. Neuropharmacology. 2016 Nov;110(Pt A):277-286.  [Content Brief]

  [4]. Conductier G, et al. 3,4-N-methlenedioxymethamphetamine-induced hypophagia is maintained in 5-HT1B receptor knockout mice, but suppressed by the 5-HT2C receptor antagonist RS102221. Neuropsychopharmacology. 2005 Jun;30(6):1056-63.  [Content Brief]