Astressin

更新时间：2025-08-21 08:16:37

Astressin结构式	常用名	Astressin	英文名	Astressin TFA
	CAS号	170809-51-5	分子量	3563.16000
	密度	N/A	沸点	N/A
	分子式	C₁₆₁H₂₆₉N₄₉O₄₂	熔点	N/A
	MSDS	中文版美版	闪点	N/A

Astressin用途

Astressin是有效的促肾上腺皮质激素释放因子 (CRF) 拮抗剂。

中文名	DPHE-HIS-LEU-LEU-ARG-GLU-VAL-LEU-GLU-NLE-ALA-ARG-ALA-GLU-GLN-LEU-ALA-GLN-GLU-ALA-HIS-LYS-ASN-ARG-LYS-LEU-NLE-GLU-ILE-ILE-NH2
英文名	astressin
英文别名	更多

描述	Astressin是有效的促肾上腺皮质激素释放因子 (CRF) 拮抗剂。
相关类别	信号通路 >> 其他 >> 其他多肽产品研究领域 >> 神经疾病
体外研究	Astressin对CRF结合蛋白的亲和力低,对克隆的垂体受体具有高亲和力(Ki = 2 nM)。 Astressin对CHO细胞中稳定表达的克隆人CRF-RA1具有高亲和力,并且具有抑制ACTH分泌的高效力[1]。
体内研究	在应激或肾上腺切除的大鼠中,Astressin比任何先前测试的拮抗剂在降低垂体促肾上腺皮质激素(ACTH)分泌方面明显更有效。静脉注射低剂量的astressin(30μg和100μg/ kg)仍然分别在45和90分钟时显着降低ACTH水平[1]。 Astressin显着逆转社交应激和ICV大鼠/人类CRF(r/hCRF)对高架十字迷宫引起的致焦虑样反应,但未能在熟悉的环境中阻断r/hCRF诱导的运动活动的影响[2] ]。在癫痫发作前30分钟和癫痫发作后10分钟,脑室内输注肽可使一些海马细胞区的损伤降低多达84％,其保护程度大于其他CRF拮抗剂对其他坏死性神经元损伤模型的报道。即使在激素毒素暴露后仅10分钟给药,Astressin也会起作用[3]。
动物实验	大鼠：大鼠饮食补充橙子，其水含有0.9％NaCl。它们在静脉注射载体或astressin之前48小时配备留置颈静脉插管。首先将Astressin在无菌，蒸馏的无热水中稀释，并将pH调节至7.0。在含有0.1％牛血清白蛋白和0.01％抗坏血酸的0.04M磷酸盐缓冲液（pH 7.4）中进一步稀释。在治疗前立即获得血液样品，并在15-120分钟后获得。将倾析的血浆样品冷冻直至测定ACTH浓度[1]。
参考文献	[1]. Gulyas J, et al. Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc Natl Acad Sci U S A. 1995 Nov 7;92(23):10575-9. [2]. Spina MG, et al. Behavioral effects of central administration of the novel CRF antagonist astressin in rats. Neuropsychopharmacology. 2000 Mar;22(3):230-9. [3]. Maecker H, et al. Astressin, a novel and potent CRF antagonist, is neuroprotective in the hippocampus when administered after a seizure. Brain Res. 1997 Jan 2;744(1):166-70.

分子式	C₁₆₁H₂₆₉N₄₉O₄₂
分子量	3563.16000
精确质量	3561.04000
PSA	1489.66000
LogP	9.58910
InChIKey	HPYIIXJJVYSMCV-UHFFFAOYSA-N
SMILES	CCCCC(NC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(=O)O)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(Cc1c[nH]cn1)NC(=O)C(N)Cc1ccccc1)C(C)C)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NC(CCC(=O)O)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NC(CCC(N)=O)C(=O)NC1CCC(=O)NCCCCC(C(=O)NC(CC(N)=O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCCC)C(=O)NC(CCC(=O)O)C(=O)NC(C(=O)NC(C(N)=O)C(C)CC)C(C)CC)NC(=O)C(Cc2c[nH]cn2)NC(=O)C(C)NC1=O
储存条件	2-8℃

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport

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Astressin

M.W. 3563.24 C161H269N49O42

[D-Phe12,Nle21,38,Glu30

ASTRESSIN TRIFLUOROACETATE SALT