Description
Penitrem A (12627-35-9) is a fungal mycotoxin that acts as a selective, irreversible blocker of the smooth muscle high conductance Ca2+-activated K+?(BK, KCa1.1) channel (100% block at 10 nM).1?Displays brain neurotoxicity in rats along with dose-dependent convulsions and death.2?An important tool for studying the role of BK channels in vascular function which is effective in cellular, tissue and?in vivo?experiments.3?Inhibits BK channels in inside-out and cell-attached patches, whereas iberiotoxin (considered the gold standard BK channel blocker) does not.3?May be used to partially ablate Purkinje cells in immature rat cerebellum providing a model for neural stem cell transplantation studies.4
Chemical Properties
Solid
Occurrence
A series of closely related metabolites of Penicillium crustosum has recently been isolated and the components separated chromatographically. Penitrem A forms colourless crystals from EtOH.
Uses
Penitrem A is a tremorgenic mycotoxin isolated from Penicillium species. Penitrem A is a selective blocker of high-conductance Ca2+-activated potassium channels.
Uses
Penitrem A has been used as Ca
2+-Activated K
+ (BK) channel blocker to study its effect on BK current in bag cell neurons.
Definition
ChEBI: Penitrem A is an organooxygen compound and an organic heterotricyclic compound.
Biochem/physiol Actions
Penitrem A intoxication causes ataxia, polypnea, and sustained tremors and may lead to seizures and death. Penitrem A affects the central and peripheral nervous system. It impairs the GABAergic neurotransmission in the cerebellum.
Safety Profile
Poison by ingestion and intraperitoneal routes. An experimental teratogen. When heated to decomposition it emits very toxic fumes of Clí and NOx.
References
References/Citations:
