corticotropin-releasing factor (CRF) receptor antagonist
CAS：170809-51-5
分子式：C161H269N49O42
分子量：3563.2
纯度：98%
存储：Store at -20°C

Background:

Astressin is a potent corticotropin releasing factor (CRF) antagonist.

Astressin has low affinity for the CRF binding protein and high affinity (Ki=2 nM) for the cloned pituitary receptor. Astressin shows high affinity for cloned human CRF-RA1 stably expressed in CHO cells and high potency to inhibit ACTH secretion[1].

Astressin is significantly more potent than any previously tested antagonist in reducing hypophyseal corticotropin (ACTH) secretion in stressed or adrenalectomized rats. Low doses of astressin (30 μg and 100 μg per kg) administered i.v. still produce a significant decrease in ACTH levels at 45 and 90 min, respectively[1]. Astressin significantly reverses the anxiogenic-like response induced by both social stress and ICV rat/humanCRF (r/hCRF) on the elevated plus-maze, but fails to block the effects of r/hCRF-induced locomotor activity in a familiar environment[2]. Intracerebroventricular infusion of the peptide both 30 min before and 10 min after seizures decreases damage in some hippocampal cell fields by as much as 84%, a magnitude of protection greater than reported for other CRF antagonists against other models of necrotic neuronal injury. Astressin protects even if administered only 10 min following excitotoxin exposure[3].

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.