<Suppliers Price>

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

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.