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RS 102221

Chemical Structure : RS 102221

CAS No.: 187397-18-8

RS 102221 (RS102221;RS-102221)

Catalog No.: PC-60815Not For Human Use, Lab Use Only.

A highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively; demonstrates 100-fold selectivity for the 5-HT2C versus 5-HT2A and 5-HT2B receptors; acts as an antagonist in a cell-based microphysiometry functional assay with pA2 of 8.1 and has no detectable intrinsic efficacy; increases food-intake and weight-gain in rats (2 mg/kg, i.p.); reverses the inhibitory effects of MK-212 and DOI on 'monosynaptic and 'intermediate' neurones.

Physicochemical Properties

M.Wt 649.08
Formula C27H31F3N4O7S.HCl
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride

References

1. Bonhaus DW, et al. Neuropharmacology. 1997 Apr-May;36(4-5):621-9.

2. Bonhaus DW, et al. Ann N Y Acad Sci. 1998 Dec 15;861:269.

3. Sévoz-Couche C, et al. Br J Pharmacol. 2000 Dec;131(7):1445-53.

4. McMahon LR, et al. J Neurosci. 2001 Oct 1;21(19):7781-7.

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