4-IBP

4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (K_i =1.7 nM) and moderate affinity for the σ₂ receptor (K_i = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research^{[1][2][3][4][5][6]}. In Vitro:4-IBP (1-100 nM) significantly reduces the migration ability of C32 melanoma, U373-MG glioblastoma, A549 non-small cell lung carcinoma, and PC3 prostate cancer cells^[1].
4-IBP (10 nM; 1-24 h) can significantly sensitize U373-MG glioblastoma cells to the pro-apoptotic effect of Lomustine (HY-13669) or the pro-autophagic effect of Temozolomide (HY-17364)^[1].
4-IBP (10 μM; 1-6 days) significantly inhibits the growth of T98G glioblastoma cells^[3].
In Vivo:4-IBP (2 mg/kg; i.v.; 3 times a week; 4 weeks) significantly enhances the therapeutic effect of Irinotecan (HY-16562) in immunodeficient mice bearing orthotopic A549 non-small cell lung cancer^[1].
4-IBP (2 mg/kg; subcutaneous implantation of an osmotic minipump; 28 days) significantly increases the survival rate and enhances the therapeutic effect of Temozolomide in immunocompromised mice orthotopically implanted with U373-MG glioblastoma^[1].
4-IBP (2 mg/kg/day; administered by an osmotic minipump implanted subcutaneously; 2-21 days) significantly increases the basal firing rate of 5-HT neurons in the dorsal raphe nucleus in male SD rats^[2].