Drugs

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

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

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

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