Bioactivity | SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease[1][2][3]. | ||||||||||||
Invitro | SB 258719 (1, 3 and 10 μM; HEK 293 cells) 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.) significantly attenuates the 5-CT-induced hypothermia[2]. Animal Model: | ||||||||||||
Name | SB 258719 | ||||||||||||
CAS | 195199-95-2 | ||||||||||||
Formula | C18H30N2O2S | ||||||||||||
Molar Mass | 338.51 | ||||||||||||
Appearance | Liquid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |