Drug intelligence / Profile preview

astressin

Development stage
Preclinical
Lead developer
Salk Institute for Biological Studies
Modality
Peptides, Small Molecules
Administration
Intracerebral, Intravenous
01

Overview

Astressin is a synthetic, cyclic 30-residue peptide designed as a potent antagonist of corticotropin-releasing factor (CRF) receptors. It competitively blocks CRF from binding to its receptors, thus inhibiting the release of adrenocorticotropic hormone (ACTH) from the pituitary and moderating central and peripheral components of the stress response. In preclinical studies, astressin potently blocks CRF-induced ACTH secretion and has demonstrated neuroprotective effects against excitotoxic and seizure-induced neuronal damage in animal models. It is considerably more potent than earlier CRF antagonists and has been used to study the physiological and neuroprotective effects of CRF antagonism in vivo and in vitro[1][2][8][10].

Other names
D-Phe(12), Nle(21,38), Glu(30), Lys(33)]-CRF (12-41)CHEBI:76649MFCD00798715MFCD-00798715MFCD 00798715Astressin trifluoroacetate saltfHLLREVLE-Nle-ARAEQLAQ-cyclo-(EAHK)NRKL-Nle-EII-NH2
02

Targets

CRHR1 (Corticotropin-releasing factor receptor 1)CRHR2 (Corticotropin-releasing hormone receptor 2)

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