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Mujteba, S.

Publications and source records attributed to Mujteba, S..

2 recordsLinked to original sources

Loss of SUR1 and Kir6.2 ATP-sensitive potassium channel subunits produces comparable neuronal excitability and morphine antinociception

ATP-sensitive potassium (KATP) channels are integral membrane proteins that play a crucial role in linking cellular metabolism to neuronal excitability. KATP channels in peripheral nociception and pain emphasize metabolic gating as a determinant of dorsal root ganglia and spinal cord excitability, particularly in pathophysiological states. Activation of KATP channels reduces excitability and and also contributes to opioid induced analgesia. KATP channels are composed of multiple subunits, that are assembled in several subtypes, including Kir6.2/SUR1 which is found predominantly in neurons in the nervous system. It remains unclear whether both Kir6.2 and SUR1 subunits are required to regulate neuronal excitability under naive conditions and to mediate morphine-induced antinociception. These experiments aim to determine whether neuron-specific loss of either Kir6.2 or SUR1 increases dorsal root ganglion (DRG) neuronal excitability, and attenuates morphine antinociception in mice. We found that loss of SUR1 or Kir6.2 activity or expression both increased DRG excitability in whole cell patch clamp studies. Using DRG cultured from SUR1 and Kir6.2 floxed animals, we also found that loss of either subunit decreased potassium flux induced by diazoxide. Morphine induced antinociception was also attenuated after Cre-mediated recombination in SUR1 and Kir6.2 floxed animals. Chronic morphine administration also decreased Kir6.2 (gene: Kcnj11) RNA signal in mouse DRG, but not spinal cords. Together, these findings suggest that, despite evidence from single-cell sequencing and other datasets indicating potentially distinct expression patterns of SUR1 and Kir6.2, these subunits most likely function cooperatively to form functional KATP channels under normal physiological conditions.

neuroscience↗

KATP Channel Prodrugs Reduce Inflammatory and Neuropathic Hypersensitivity, Morphine Induced Hypersensitivity, and Precipitated Withdrawal in Mice

Previous studies show ATP-sensitive potassium (KATP) channel openers can reduce hypersensitivity associated with chronic pain models in rodents, and reduce morphine tolerance. Many agonists of KATP channels are not soluble in physiologically relevant vehicles, requiring adaptation for clinical use. This study compared the antinociception activity of novel KATP channel targeting prodrugs, CKLP1, CKLP2, and CF3-CKLP. These prodrugs are activated by endogenous alkaline phosphatase enzymes present in the peripheral and central nervous systems. Analgesic capabilities of intrathecally injected prodrugs were tested in rodent models of spinal nerve ligation (SNL) and Complete Freunds Adjuvant (CFA) as models for neuropathic and inflammatory pain, respectively. CKLP1 and CKLP2 significantly increased mechanical paw withdrawal thresholds 1-2 hours after intrathecal administration in the SNL model, but all three prodrugs were able to attenuate hypersensitivity up to 7 days after CFA treatment. The reduction of opioid tolerance and opioid-induced hypersensitivity in mice treated chronically with morphine was significantly reduced in CKLP1 and CKLP2 treated animals. Prodrug cleavage was confirmed in mouse spinal cords using liquid chromatography. These studies may aid in the further development of KATP channel prodrugs for use in treatments of chronic pain, opioid tolerance, and withdrawal.

pharmacology and toxicology↗