What are p38 kinase inhibitors? The p38 mitogen-activated protein kinases are responsive to stress stimuli, such as cytokines, resulting in inflammation. Inhibition of these kinases is antiinflammatory. They have potential utility in autoimmune disease and inflammatory states; however, clinical trials to date have not been successful. Inhibition may result in prolonged QTc interval and will …
What is the current status of the cannabinoids to treat pain? There are two cannabinoid receptors, CB1 and CB2. Both receptors are G protein coupled positively to potassium channels and negatively to N-type and P/Q-type calcium channels, resulting in postsynaptic membrane hyperpolarization and a presynaptic reduction in neurotransmitter release. CB1 receptors are located peripherally and …
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What are some of the new ways to modulate the postsynaptic N methyl d aspartate ionophore? Presynaptic release of glutamate binds to the postsynaptic glutamate receptor of the N -methyl- d -aspartate (NMDA) ionophore, resulting in channel opening and influx of sodium and calcium. This in turn results in postsynaptic depolarization and pain transmission. There have been many studies evaluating the …
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Are there any new calcium channel modulators in the pipeline? There are several N-type calcium channel blockers (intrathecal ziconotide) and modulators (pregabalin and gabapentin) currently on the market. Clinical effectiveness has been mixed with both positive and negative clinical trials. Mirogabalin is a new promising N-type calcium channel modulator. Pregabalin and gabapentin bind the alpha-2-delta …
What are transient receptor potential cation channels, subfamily 1, and what role do they play in pain transmission? The transient receptor potential cation channels, subfamily 1 (TRPV1) channel is a capsaicin and vanilloid receptor 1 that is expressed on pain fibers. TRPV1 provides a sensation of scalding heat and pain when activated. It also functions …
Are there any other voltage gated ion channels that are targets for pain modulation? Potassium voltage-gated channel subfamily Q members are potential targets for pain management. The M potassium channel is a slowly activating and deactivating channel that regulates neuronal excitability. A defect in the KCNQ3 gene results in neonatal convulsions; therefore, activators of the …
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How does sodium channel blockade reduce pain? Voltage-gated sodium channels are upregulated after nervous system injury and disease, resulting in spontaneous and elicited pain. In addition, gain- and loss-of-function mutations in a specific sodium channel subtype, Nav 1.7, have been linked to the pain syndromes primary erythromelalgia and congenital insensitivity to pain, respectively. Sodium channels …