(-)-p-Bromotetramisole Oxalate(L-p-bromotetramisole) is a potent and non-specific inhibitor of alkaline phosphatase [1-2].
(-)-p-Bromotetramisole Oxalate (1 mM) augmented cAMP-stimulated iodide efflux and, by itself, stimulated a larger efflux than that evoked by cAMP agonists, suggesting that it may promote the opening of humancystic fibrosis transmembrane conductance regulator (CFTR) in CHO cells[3]. In PC12 cells, (-)-p-Bromotetramisole Oxalate (0.3 mM) enhances ionomycin-stimulated norepinephrine (NA) release[4].
(-)-p-Bromotetramisole Oxalate(30 mg/kg; ivgtt) significantly inhibited norepinephrine-induced MABP elevation and renal vascular resistance. It reduces renal vascular and blood pressure response to norepinephrine[5]. Systemic infusion of (-)-p-Bromotetramisole Oxalate (0.8 ml/min of 10 mM I-p-Bromotetramisole oxalate; ivgtt) increases Fractional excretion of phosphate (FEPi) in Sprague-Dawley rats[6].
References:
[1]. Borgers M. The cytochemical application of new potent inhibitors of alkaline phosphatases. J Histochem Cytochem. 1973 Sep;21(9):812-24. doi: 10.1177/21.9.812. PMID: 4741290.
[2]. Borgers M, Thoné F. The inhibition of alkaline phosphatase by L-p-bromotetramisole. Histochemistry, 1975, 44(3): 277-280.
[3]. Lansdell KA, Kidd JF, et,al. Regulation of murine cystic fibrosis transmembrane conductance regulator Cl- channels expressed in Chinese hamster ovary cells. J Physiol. 1998 Nov 1;512 ( Pt 3)(Pt 3):751-64. doi: 10.1111/j.1469-7793.1998.751bd.x. PMID: 9769419; PMCID: PMC2231228.
[4]. Kitamura T, Murayama T, et,al. Enhancement of Ca2+-induced noradrenaline release by vanadate in PC12 cells: possible involvement of tyrosine phosphorylation. Brain Res. 2000 Jan 31;854(1-2):165-71. doi: 10.1016/s0006-8993(99)02299-4. PMID: 10784118.
[5]. Jackson EK, Zhang Y,et,al. Alkaline Phosphatase Inhibitors Attenuate Renovascular Responses to Norepinephrine. Hypertension. 2017 Mar;69(3):484-493. doi: 10.1161/HYPERTENSIONAHA.116.08623. Epub 2017 Jan 30. PMID: 28137984; PMCID: PMC5310812.
[6]. Onsgard-Meyer M, McCoy AL, et,al. Effect of bromotetramisole on renal phosphate excretion. Proc Soc Exp Biol Med. 1996 Nov;213(2):193-5. doi: 10.3181/00379727-213-44050. PMID: 8931664.
(-)-P-Bromotetramisole Oxalate是一种有效的非特异性碱性磷酸酶抑制剂[1-2]。
(-)-P-Bromotetramisole Oxalate(1 mM)增强了cAMP刺激的碘化物外排，且其本身刺激的外排量大于cAMP激动剂引起的外排量，提示其可能促进CHO细胞中人囊性纤维化跨膜传导调节剂(CFTR)的开放[3]。(-)-P-Bromotetramisole Oxalate(0.3 mM)可增强PC12细胞的离子霉素刺激的去甲肾上腺素(NA) [4]。
(-)-P-Bromotetramisole Oxalate (30mg /kg; ivgtt)显著抑制去甲肾上腺素诱导的平均动脉血压升高和肾血管阻力。它能降低肾血管和血压对去甲肾上腺素的反应[5]。在大鼠中全身输注(-) -P-Bromotetramisole Oxalate(0.8 ml/min of 10 mM (-) -P-Bromotetramisole Oxalate; ivgtt)可增加磷酸的部分排泄(FEPi) [6]。