Related Experiment Video
Updated: Feb 5, 2026

11:54
Measurement of BK-polyomavirus Non-Coding Control Region Driven Transcriptional Activity Via Flow Cytometry
Published on: July 13, 2019
9.4K
Pioglitazone, a PPAR-γ Activator, Stimulates BK
Tsang-Shan Chen1, Ming-Chi Lai2, Te-Yu Hung2
1Department of Neurology, Tainan Sin-Lau Hospital, Tainan, Taiwan.
Frontiers in Pharmacology
|September 14, 2018
Summary
Pioglitazone stimulates Ca2+-activated K+ currents and inhibits M-type K+ currents in hippocampal neurons. These effects on potassium channels may explain its broad pharmacological actions.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- Pioglitazone (PIO) is a thiazolidinedione known to activate peroxisome proliferator-activated receptor-γ (PPAR-γ).
- PIO exhibits anti-inflammatory, anti-proliferative, anti-diabetic, and antidepressive properties.
- Its effects on specific potassium currents in central neurons are not well understood.
Purpose of the Study:
- To investigate the impact of Pioglitazone on Ca2+-activated K+ currents (IK(Ca)) and M-type K+ currents in hippocampal neurons.
- To elucidate the specific potassium channels affected by PIO.
Main Methods:
- Whole-cell and inside-out patch-clamp recordings were used to measure potassium currents in mHippoE-14 cells.
- The effects of PIO (10 μM) on IK(Ca) and M-type K+ currents were analyzed.
- Specific channel blockers (paxilline, TRAM-39, apamin) were used to identify the type of K+ channels involved.
Main Results:
- Pioglitazone (10 μM) significantly increased the amplitude of Ca2+-activated K+ current (IK(Ca)) in hippocampal neurons.
- PIO's stimulation of IK(Ca) was reversed by paxilline, indicating involvement of large-conductance Ca2+-activated K+ (BKCa) channels.
- PIO concentration-dependently activated BKCa channels (EC50 = 7.6 μM), altering their open and closed times and shifting their activation curve.
- Pioglitazone also suppressed the amplitude of M-type K+ currents in these neurons.
Conclusions:
- Pioglitazone modulates both Ca2+-activated K+ (specifically BKCa channels) and M-type K+ currents in hippocampal neurons.
- These perturbations of potassium channel activity may contribute to the diverse pharmacological effects of Pioglitazone.
- Further research into these channel interactions could reveal new therapeutic strategies.
Related Concept Videos
Stimulants
1.0K
Stimulants are substances that enhance neural activity and elevate dopamine levels in the brain, leading to their highly addictive nature. These drugs include cocaine, amphetamines, MDMA, caffeine, and nicotine, each with distinct mechanisms of action and varied health implications.
Cocaine can be administered via snorting, injection, or smoking. It primarily functions by blocking the reuptake of dopamine, resulting in a euphoric high characterized by an intense sensation of happiness and...
Cocaine can be administered via snorting, injection, or smoking. It primarily functions by blocking the reuptake of dopamine, resulting in a euphoric high characterized by an intense sensation of happiness and...
1.0K
Co-activators and Co-repressors
8.7K
Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
8.7K
tRNA Activation
23.0K
Aminoacyl-tRNA synthetases are present in both eukaryotes and bacteria. Though eukaryotes have 20 different aminoacyl-tRNA synthetases to couple to 20 amino acids, many bacteria do not have genes for all of these aminoacyl-tRNA synthetases. Despite this, they still use all 20 amino acids to synthesize their proteins. For instance, some bacteria do not have the gene encoding the enzyme that couples glutamine with its partner tRNA. In these organisms, one enzyme adds glutamic acid to all of the...
23.0K
Activation Energy
86.7K
Activation energy is the minimum amount of energy necessary for a chemical reaction to move forward. The higher the activation energy, the slower the rate of the reaction. However, adding heat to the reaction will increase the rate, since it causes molecules to move faster and increase the likelihood that molecules will collide. The collision and breaking of bonds represents the uphill phase of a reaction and generates the transition state. The transition state is an unstable high-energy state...
86.7K
Motor Unit Stimulation
3.8K
When the neuron of a motor unit fires an action potential, it triggers a series of events, leading to a twitch contraction in the muscle fibers. The process of excitation-contraction coupling is crucial in relaying the action potential to the muscle fibers.
The latent period of contraction marks the onset of excitation-contraction coupling, when the action potential propagates across the sarcolemma, preparing the muscle fibers for contraction. As the fibers enter the contraction phase, the...
The latent period of contraction marks the onset of excitation-contraction coupling, when the action potential propagates across the sarcolemma, preparing the muscle fibers for contraction. As the fibers enter the contraction phase, the...
3.8K
Muscle Stimulation Frequency
4.6K
The contraction strength of muscles is regulated by motor neurons, which modulate the frequency of action potentials dispatched to the motor units based on the body's requirements. This process of varying the muscle stimulation frequency allows muscles to contract with a force that is precisely tailored to the needs of the moment, whether lifting a feather or a heavy box.
Wave summation
At low firing rates, motor neurons induce individual twitch contractions in muscle fibers. These twitches...
Wave summation
At low firing rates, motor neurons induce individual twitch contractions in muscle fibers. These twitches...
4.6K

