Astressin

Astressin用途

Astressin是有效的促肾上腺皮质激素释放因子 (CRF) 拮抗剂。

Astressin名称

[ 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 TFA

[英文别名 ]:

Astressin
M.W. 3563.24 C161H269N49O42
[D-Phe12,Nle21,38,Glu30
ASTRESSIN TRIFLUOROACETATE SALT

Astressin生物活性

[ 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.

[相关活性小分子]

Astressin物理化学性质

[ 分子式 ]:
C₁₆₁H₂₆₉N₄₉O₄₂

[ 分子量 ]:
3563.16000

[ 精确质量 ]:
3561.04000

[ PSA ]:
1489.66000

[ LogP ]:
9.58910

[ 储存条件 ]:
2-8℃

Astressin安全信息

[ 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

Astressin文献

Neurokinin B signaling in the female rat: a novel link between stress and reproduction.

Endocrinology 155(7) , 2589-601, (2014)

Acute systemic stress disrupts reproductive function by inhibiting pulsatile gonadotropin secretion. The underlying mechanism involves stress-induced suppression of the GnRH pulse generator, the funct...

Corticotropin-releasing hormone and the sympathoadrenal system are major mediators in the effects of peripherally administered exendin-4 on the hypothalamic-pituitary-adrenal axis of male rats.

Endocrinology 155(7) , 2511-23, (2014)

Glucagon-like peptide-1 (GLP-1) and the GLP-1 receptor agonist, exendin-4 (Ex-4), potently stimulate hypothalamic-pituitary-adrenal (HPA) axis activity after either central or peripheral administratio...

Social stress and CRF-dopamine interactions in the VTA: role in long-term escalation of cocaine self-administration.

J. Neurosci. 34(19) , 6659-67, (2014)

The nature of neuroadaptations in the genesis of escalated cocaine taking remains a topic of considerable interest. Intermittent social defeat stress induces both locomotor and dopaminergic cross-sens...

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