SB-705498

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Chemical Structure| 501951-42-4 同义名 : -
CAS号 : 501951-42-4
货号 : A722112
分子式 : C17H16BrF3N4O
纯度 : 99%
分子量 : 429.23
MDL号 : MFCD13152399
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 TRPV1 is a non-selective cation channel, predominantly expressed by peripheral sensory neurons. It plays a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. SB-705498 is a potent TRPV1 antagonist with pKb value of 7.5 in FLIPR-Ca2+-based assays versus capsaicin at TRPV1. Co-application of 1μM SB-705498 completely and reversibly inhibited capsaicin-mediated activation of human TRPV1 by measure of whole cell currents by patch clamp. Pre-treatment with SB-705498 at doses of 3mg/kg and 10mg/kg, p.o., for 2h, dose-dependently antagonized capsaicin induced secondary hyperalgesia in rat. SB-705498 can potently inhibit the multiple modes of TRPV1 activation, including capsaicin-, acid- and heat-mediated activation of human TRPV1.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.65mL

2.33mL

1.16mL

23.30mL

4.66mL

2.33mL
参考文献

[1]Bareille P, Murdoch RD, et al. The effects of a TRPV1 antagonist, SB-705498, in the treatment of seasonal allergic rhinitis. Int J Clin Pharmacol Ther. 2013 Jul;51(7):576-84.

[2]Rami HK, Thompson M, et al. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91.

[3]Lambert GA, Davis JB, et al. The effects of the TRPV1 receptor antagonist SB-705498 on trigeminovascular sensitisation and neurotransmission. Naunyn Schmiedebergs Arch Pharmacol. 2009 Oct;380(4):311-25.

[4]Belvisi MG, Birrell MA, et al. XEN-D0501, a Novel Transient Receptor Potential Vanilloid 1 Antagonist, Does Not Reduce Cough in Patients with Refractory Cough. Am J Respir Crit Care Med. 2017 Nov 15;196(10):1255-1263.

[5]Holland C, van Drunen C, et al. Inhibition of capsaicin-driven nasal hyper-reactivity by SB-705498, a TRPV1 antagonist. Br J Clin Pharmacol. 2014 May;77(5):777-88.