IQM-PC332, a Novel DREAM Ligand with Antinociceptive Effect on Peripheral Nerve Injury-Induced Pain
Abstract
:1. Introduction
2. Results
2.1. Effect of IQM-PC332 on Mechanical Sensitivity in CCI Animals
2.2. Effect of IQM-PC332 on IA in DRG Neurons
2.3. Effect of IQM-PC332 on T-Type and HVA Ca2+ Currents in DRG Neurons
2.4. Effect of IQM-PC332 on TRPV1 Channels in DRG Neurons
2.5. Effect of IQM-PC332 on Electrical Activity of DRG Neurons
3. Discussion
4. Materials and Methods
4.1. Chronic Constriction Injury of The Sciatic Nerve
4.2. Behavioural Testing
4.2.1. Mechanical Sensitivity
4.2.2. Motor Coordination
4.3. Isolation of DRG Neurons
4.4. Electrophysiological Recordings
4.4.1. Solutions and Drug Application
4.4.2. Voltage/Current Protocols and Data Analysis
4.5. Statistics
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
Abbreviations
BDNF | Brain derived neurotrophic factor |
Cav | Voltage-activated calcium channel/current |
CCI | Chronic constriction injury |
DMEM | Dulbecco’s modified Eagle’s Medium-low glucose |
DREAM | Downstream regulatory element antagonist modulator |
DRG | Dorsal root ganglia |
ED50 | Effective dose 50% |
HVA | High voltage-activated |
IC50 | Inhibitory concentration 50% |
i.p. | Intraperitoneal |
i.pl. | Intraplantar |
IQM-PC332 | (2-[2-(3,4-Dichlorophenyl)acetylamino]-4-(4′-n-butylphenyl)benzoic acid) |
KChIP3 | Potassium channel interacting protein 3 |
KD | Dissociation constant |
Kv | Voltage-activated potassium channel/current |
MPE | Maximum possible effect |
Nav | Voltage-activated sodium channel/current |
PWT | Paw withdrawal threshold |
TRPV1 | Transient receptor potential vanilloid-1 |
Vh | Holding voltage |
Vcomm | Voltage command |
Vr | Resting membrane potential |
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Socuéllamos, P.G.; Olivos-Oré, L.A.; Barahona, M.V.; Cercós, P.; Pérez Pascual, M.; Arribas-Blázquez, M.; Naranjo, J.R.; Valenzuela, C.; Gutiérrez-Rodríguez, M.; Artalejo, A.R. IQM-PC332, a Novel DREAM Ligand with Antinociceptive Effect on Peripheral Nerve Injury-Induced Pain. Int. J. Mol. Sci. 2022, 23, 2142. https://doi.org/10.3390/ijms23042142
Socuéllamos PG, Olivos-Oré LA, Barahona MV, Cercós P, Pérez Pascual M, Arribas-Blázquez M, Naranjo JR, Valenzuela C, Gutiérrez-Rodríguez M, Artalejo AR. IQM-PC332, a Novel DREAM Ligand with Antinociceptive Effect on Peripheral Nerve Injury-Induced Pain. International Journal of Molecular Sciences. 2022; 23(4):2142. https://doi.org/10.3390/ijms23042142
Chicago/Turabian StyleSocuéllamos, Paula G., Luis A. Olivos-Oré, María Victoria Barahona, Pilar Cercós, Marta Pérez Pascual, Marina Arribas-Blázquez, José Ramón Naranjo, Carmen Valenzuela, Marta Gutiérrez-Rodríguez, and Antonio R. Artalejo. 2022. "IQM-PC332, a Novel DREAM Ligand with Antinociceptive Effect on Peripheral Nerve Injury-Induced Pain" International Journal of Molecular Sciences 23, no. 4: 2142. https://doi.org/10.3390/ijms23042142