Antisauvagine-30 TFA (aSvg-30 TFA) 是有效的、高度选择性的、竞争性的 CRF2 受体 的多肽拮抗剂。Antisauvagine-30 TFA 对 mCRFR2β 和 CRFR1 的 Kd 值分别为1.4 nM 和150 nM。
Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively[1][2][3][4].
Antisauvagine-30 (aSvg-30) prevents stress-enhanced fear conditioning and Mek-1/2-dependent activation of Erk-1/2 and p90Rsk-1. Antisauvagine-30 (aSvg-30) did not affect the phosphorylation of the PKA regulatory subunit II of stressed mice[1][2].
Antisauvagine-30 (aSvg-30; i.h. 400 ng/0.5 μl per mouse) selectively prevents the stress-induced enhancement of fear conditioning without affecting the fear conditioning of nonstressed mice[2].Antisauvagine-30 (aSvg-30) injected i.c.v. elicits a significant anxiogenic effect[3]. Animal Model: Nine-week-old male BALB/c mice[2].
[1]. Brauns O, et al. Pharmacological and chemical properties of astressin, antisauvagine-30 and alpha-helCRF: significance for behavioral experiments. Neuropharmacology. 2001 Sep;41(4):507-16. [2]. Sananbenesi F, et al. Mitogen-activated protein kinase signaling in the hippocampus and its modulation by corticotropin-releasing factor receptor 2: a possible link between stress and fear memory. J Neurosci. 2003 Dec 10;23(36):11436-43. [3]. Radulovic J, et al. Modulation of learning and anxiety by corticotropin-releasing factor (CRF) and stress: differential roles of CRF receptors 1 and 2. J Neurosci. 1999 Jun 15;19(12):5016-25. [4]. Klaus Eckart, et al. Action of CRF and its analogs. Current Medicinal Chemistry, 1999, 6, 1035-1053.
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