SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂，pKi为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。

SB 258719 is a selective antagonist of 5-HT7 receptor with pKi of 7.5.

SB 258719 antagonised surmountably 5-CT-stimulated adenylyl cyclase activity. Schild analysis of the antagonism by SB 258719 gave a pA2?of 7.2±0.2 and slope not significantly different from 1, consistent with competitive antagonism[3].

SB 258719 (5-20 mg/kg, i.p.) reversed the hypothermic effect of 5-CT in mice[1]. Increased Wnt/β-catenin activity was attenuated by SB 258719 in HCC cell lines and patient-derived primary tumour tissues in the presence of 5-HT. SB 258719 also reduced tumour growth in vivo[2].

195199-95-2

C18H30N2O2S

338.51

SB 258719

DMSO:250 mg/mL (738.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years