SB-269970 is a potent and selective 5-HT7 receptor antagonist, with a high affinity (pKi = 8.9) [1]. SB-269970 can cross the blood-brain barrier and is widely used in neuroscience research to study the role of the 5-HT7 receptor in a variety of central nervous system functions[2]. SB-269970 is employed in pharmacological studies to explore its potential therapeutic applications in conditions such as depression, anxiety, and sleep disorders[3].
SB-269970 (1µM; 24h) treatment can inhibit proliferation in PC-3 cells and is associated with an apoptosis-inducing effect[4]. SB-269970 combined with MSX3 and ketanserin treatment can suppress pAKT expression in neuroblastoma cell lines over the long term[5].
SB-269970 (1mg/kg) exerted a specific antianxiety-like effect in the Vogel drinking test and elevated plus-maze test in rats[6]. SB-269970 (10 and 30mg/kg) significantly attenuated amphetamine-induced rearing and circling in rats[7].
References:
[1]. Lovell PJ, Bromidge SM, Dabbs S, et al. A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970). J Med Chem. 2000 Feb 10;43(3):342-5. doi: 10.1021/jm991151j. PMID: 10669560.
[2]. Nikiforuk A, Kos T, Fijał K, et al. Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on ketamine-induced schizophrenia-like deficits in rats. PLoS One. 2013 Jun 11;8(6):e66695. doi: 10.1371/journal.pone.0066695. PMID: 23776692; PMCID: PMC3679060.
[3]. Guscott M, Bristow LJ, Hadingham K, et al. Genetic knockout and pharmacological blockade studies of the 5-HT7 receptor suggest therapeutic potential in depression. Neuropharmacology. 2005 Mar;48(4):492-502. doi: 10.1016/j.neuropharm.2004.11.015. PMID: 15755477.
[4]. Cinar I, Sirin B, Halici Z, et al. 5-HT7 receptors as a new target for prostate cancer physiopathology and treatment: an experimental study on PC-3 cells and FFPE tissues. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jun;394(6):1205-1213. doi: 10.1007/s00210-021-02051-z. Epub 2021 Feb 2. PMID: 33528589.
[5]. Basaran KE, Korkmaz S, Satır-Basaran G, et al. Short and long-term blockades of adenosine 2A, 5-HT2A, and 5-HT7 receptors induce apoptosis, reduce proliferation, and show differential effects on miR-27b-3p expression in neuroblastoma cell lines. Neuroscience. 2024 Dec 17;563:212-221. doi: 10.1016/j.neuroscience.2024.11.032. Epub 2024 Nov 14. PMID: 39547336.
[6]. Wesołowska A, Nikiforuk A, Stachowicz K, et al. Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression. Neuropharmacology. 2006 Sep;51(3):578-86. doi: 10.1016/j.neuropharm.2006.04.017. Epub 2006 Jul 7. PMID: 16828124.
[7]. Waters KA, Stean TO, Hammond B, et al. Effects of the selective 5-HT(7) receptor antagonist SB-269970 in animal models of psychosis and cognition. Behav Brain Res. 2012 Mar 1;228(1):211-8. doi: 10.1016/j.bbr.2011.12.009. Epub 2011 Dec 16. PMID: 22189656.
SB-269970是一种强效且选择性的5-HT7受体拮抗剂，具有高亲和力(pKi=8.9)[1]。SB-269970能够穿过血脑屏障，广泛应用于神经科学研究中，用于探索5-HT7受体在中枢神经系统功能中的作用[2]。SB-269970在药理学研究中被广泛用于探索在抑郁症、焦虑症和睡眠障碍等疾病中的潜在治疗应用[3]。
SB-269970(1µM；24小时)处理可抑制PC-3细胞增殖，并诱导细胞凋亡[4]。SB-269970与MSX3和酮色林联合处理可长期抑制神经母细胞瘤细胞系中的pAKT表达[5]。
SB-269970(1mg/kg)在大鼠Vogel饮水实验和高架十字迷宫实验中表现出特定的抗焦虑作用[6]。SB-269970 (10和30mg/kg)处理显著减弱苯丙胺诱导的大鼠直立和转圈行为[7]。