Spantide I

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。

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Spantide I名称

[ CAS 号 ]:
91224-37-2

[ 英文名 ]:
Spantide I TFA

[英文别名 ]:

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]

Spantide I生物活性

[ 描述 ]:

[ 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.

Spantide I物理化学性质

[ 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

Spantide I安全信息

Spantide I文献

Involvement of midbrain tectum neurokinin-mediated mechanisms in fear and anxiety.

Braz. J. Med. Biol. Res. 45(4) , 349-56, (2012)

Electrical stimulation of midbrain tectum structures, particularly the dorsal periaqueductal gray (dPAG) and inferior colliculus (IC), produces defensive responses, such as freezing and escape behavio...

Solution conformation of Substance P antagonists-[D-Arg1, D-Trp7,9, Leu11]-SP, [D-Arg1, D-Pro2, D-Trp7,9, Leu11]-SP and [D-Pro2, D-Trp7,9]-SP by CD, NMR and MD simulations.

Peptides 26 , 875-885, (2005)

Substance P (SP) is an important neuropeptide involved in pain transmission and induction of inflammation. Its antagonists are being extensively investigated for their non-narcotic analgesic and anti-...

Substance P stimulates late-stage rat osteoblastic bone formation through neurokinin-1 receptors.

Neuropeptides 41(1) , 25-31, (2007)

Substance P (SP) is a widely distributed neuropeptide that works as a neurotransmitter and neuromodulator. Recently, SP receptors, particularly neurokinin-1 receptors (NK(1)-Rs) that have a high affin...

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