RS-102221 (hydrochloride)

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

Product Specifications

CAS Number

[187397-18-8]

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/rs-102221-hydrochloride.html

Concentration

10mM

Purity

98.03

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

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.Cl

Molecular Formula

C27H32ClF3N4O7S

Molecular Weight

649.08

References & Citations

[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. |[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. |[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. |[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.