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SB 243213 hydrochloride

Names

[ CAS No. ]:
200940-23-4

[ Name ]:
SB 243213 hydrochloride

[Synonym ]:
1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-, hydrochloride (1:2)
5-Methyl-N-{6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl}-6-(trifluoromethyl)-1-indolinecarboxamide dihydrochloride
Pazopanib + Tyverb/Tykerb

Biological Activity

[Description]:

SB 243213 hydrochloride is a selective and high-affinity 5-hydroxytryptamine (5-HT)2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride has improved anxiolytic profile[1].

[Target]

5-HT2C Receptor:9.37 (pKi)


[In Vivo]

SB-243213 hydrochloride is a potent inhibitor of central 5-HT2C receptor-mediated function in rats. SB-243213 hydrochloride exhibits anxiolytic-like activity in both the social interaction and Geller-Seifter conflict tests[1].

[References]

[1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20ClF3N4O2

[ Molecular Weight ]:
501.329

[ Exact Mass ]:
500.099365

[ PSA ]:
70.84000

[ LogP ]:
5.57770

Related Compounds