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BAM15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced kidney tubule damage. [1] [2] It is being studied for the treatment of obesity [3] sepsis, [1] [4] and cancer. [5] [6]
In humans, DNP causes dose-dependent mitochondrial uncoupling, causing the rapid loss of ATP as heat and leading to uncontrolled hyperthermia—up to 44 °C (111 °F)—and death in case of overdose. Researchers noticed its effect on raising the basal metabolic rate in accidental exposure and developed it as one of the first weight loss drugs ...
An uncoupler or uncoupling agent is a molecule that disrupts oxidative phosphorylation in prokaryotes and mitochondria or photophosphorylation in chloroplasts and cyanobacteria by dissociating the reactions of ATP synthesis from the electron transport chain.
It is referred to as an uncoupling agent because it disrupts ATP synthesis by transporting hydrogen ions through the mitochondrial membrane before they can be used to provide the energy for oxidative phosphorylation. [2] It is a nitrile and hydrazone. FCCP was first described in 1962 by Heytler. [3]
Rottlerin is a potent large conductance potassium channel (BKCa++) opener. [5] BKCa++ is found in the inner mitochondrial membrane of cardiomyocytes. [6] Opening these channels is beneficial for post-ischemic changes in vasodilation. [7]
Mitochondrial uncoupling protein 2 is a protein that in humans is encoded by the UCP2 gene. [ 5 ] Mitochondrial uncoupling proteins (UCP) are members of the larger family of mitochondrial anion carrier proteins (MACP).