Spantide I

更新时间：2024-01-09 21:39:34

Spantide I结构式	常用名	Spantide I	英文名	Spantide I TFA
	CAS号	91224-37-2	分子量	1497.79000
	密度	N/A	沸点	N/A
	分子式	C₇₅H₁₀₈N₂₀O₁₃	熔点	N/A
	MSDS	N/A	闪点	N/A

Spantide I用途

Spantide I 是substance P 的类似物,是选择性的神经激肽-1 受体 (NK1 receptor) 的拮抗剂,其对NK1 和 NK2 受体的 Ki 值分别为 230 nM 和 8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子 IL-10,从而显著减少角膜穿孔。

英文名	(D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P
英文别名	更多

描述	Spantide I 是substance P 的类似物,是选择性的神经激肽-1 受体 (NK1 receptor) 的拮抗剂,其对NK1 和 NK2 受体的 Ki 值分别为 230 nM 和 8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子 IL-10,从而显著减少角膜穿孔。
相关类别	研究领域 >> 炎症/免疫信号通路 >> 神经信号通路 >> 神经激肽受体信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体
靶点	NK1:230 nM (Ki) NK2:8150 nM (Ki)
体内研究	Spantide I(通过脑室灌注50和100 nM)导致所有受检动物完全呼吸停止[2]。Spantide I(36μg/小鼠,每天ip)显著降低角膜穿孔数、细菌计数和中性粒细胞数。Spantide I还下调I型细胞因子(如IFN-γ)以及MIP-2、IL-6、TNF-α和IL-1β的mRNA水平[3]。动物模型：雌性,8周龄C57BL/6(B6)和BALB/c小鼠[3]。剂量：36μg/只。给药：第1天和第0天(感染日)和每天到第5天pi(感染后)。结果：在第3天和第5天,复合治疗组小鼠的眼部疾病较PBS组明显减轻。在第3天和第5天,与PBS处理的小鼠角膜相比,PMNs的含量明显减少。3天和5天时角膜TNF-αmRNA水平显著降低。第1天时IL-18mrna水平显著降低。
参考文献	[1]. J C Beaujouan, et al. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br J Pharmacol. 1993 Mar;108(3):793-800. [2]. M Zubrzycka, et al. Comparison of antagonistic properties of substance P analogs, spantide I, II and III, on evoked tongue jerks in rats. Endocr Regul. 2000 Mar;34(1):13-8. [3]. Linda D Hazlett, et al. Spantide I decreases type I cytokines, enhances IL-10, and reduces corneal perforation in susceptible mice after Pseudomonas aeruginosa infection. Invest Ophthalmol Vis Sci. 2007 Feb;48(2):797-807.

分子式	C₇₅H₁₀₈N₂₀O₁₃
分子量	1497.79000
精确质量	1496.84000
PSA	548.21000
LogP	7.06100
储存条件	-20°C

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M.W. 1497.80 C75H108N20O13

SPANTIDE

1-Arg-7,9-Trp-11-Leu-substance p

SPANTIDE HYDROCHLORIDE

Spantide I

Substance P-[D-Arg1,D-Trp7,9,Leu11]