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SB 258719 hydrochloride

Names

[ CAS No. ]:
1217674-10-6

[ Name ]:
SB 258719 hydrochloride

[Synonym ]:
N,3-Dimethyl-N-[(2R)-4-(4-methyl-1-piperidinyl)-2-butanyl]benzenesulfonamide hydrochloride (1:1)
N,3-Dimethyl-N-[(2R)-4-(4-methylpiperidin-1-yl)butan-2-yl]benzenesulfonamide hydrochloride (1:1)
Benzenesulfonamide, N,3-dimethyl-N-[(1R)-1-methyl-3-(4-methyl-1-piperidinyl)propyl]-, hydrochloride (1:1)

Biological Activity

[Description]:

SB 258719 (hydrochloride) is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 (hydrochloride) can be used for the research of cancer and neurological diseases[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT7 Receptor:7.5 (pKi)


[In Vitro]

SB-258719 (1, 3 and 10 μM; HEK 293 cells) (hydrochloride) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no signifcant alteration in the maximal response to 5-CT[1].

[In Vivo]

SB-258719 (5~20 mg/kg; i.p.) (hydrochloride) significantly attenuates the 5-CT-induced hypothermia[2]. Animal Model: Male Swiss Webster mice (20~25 g)[2]. Dosage: 5~20 mg/kg Administration: I.p. Result: Significantly attenuated the 5-CT-induced hypothermia.

[References]

[1]. Thomas DR, et al. Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol. 1998;124(6):1300-1306.

[2]. Guscott MR, et al. The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor. Neuropharmacology. 2003;44(8):1031-1037.

[3]. Fatima S, et al. 5-Hydroxytryptamine promotes hepatocellular carcinoma proliferation by influencing β-catenin. Mol Oncol. 2016;10(2):195-212.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H31ClN2O2S

[ Molecular Weight ]:
374.97

[ Exact Mass ]:
374.179474

Related Compounds