Preferred Label : Guanabenz Acetate;
NCIt synonyms : 3-((2,6-Dichlorophenyl)methylene)carbazamidine Monoacetate;
NCIt definition : The orally bioavailable, acetate salt form of guanabenz, a centrally-acting alpha-2
adrenergic receptor agonist, with anti-hypertensive and potential antineoplastic,
cytoprotective and bone resorption inhibitory activities. Upon oral administration,
guanabenz suppresses endoplasmic reticulum (ER) stress by inhibiting the stress-induced
dephosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2a), thereby
enhancing the phosphorylation level of eIF2a. This causes elF2a-mediated downregulation
of the Rac1 pathway, upregulates the expression of activating transcription factor
4 (ATF4), which plays a key role in osteoblastogenesis, and downregulates the expression
of nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1), which is a transcription
factor that plays a key role in osteoclastogenesis. This enhances osteoblastogenesis
and suppresses osteoclastogenesis. Altogether, this promotes new bone formation and
prevents bone degradation. In addition, guanabenz blocks the proliferation, survival,
motility and invasiveness of tumor cells through the eIF2a-mediated downregulation
of Rac1 signaling. Rac1, a Ras-related small GTPase belonging to the Rho family, plays
a key role in tumor cell proliferation, survival and motility.;
UNII : 443O19GK1A;
InChIKey : MCSPBPXATWBACD-GAYQJXMFSA-N;
CAS number : 23256-50-0;
Drug name : Wytensin;
Chemical formula : C8H8Cl2N4.C2H4O2;
Origin ID : C65826;
UMLS CUI : C0733381;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- is_salt_form_of
