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PKA/AKAP/VR-1 Module: A Common Link of Gs-Mediated Signaling to Thermal Hyperalgesia
The PKA/AKAP/VR-1 module presents as the molecular correlate of Gs-mediated inflammatory hyperalgesia, and potentiation of current responses to heat depends on phosphorylation at predicted PKA consensus sites.
Voltage-gated sodium channels as primary targets of diverse lipid-soluble neurotoxins.
State- and Use-Dependent Block of Muscle Nav1.4 and Neuronal Nav1.7 Voltage-Gated Na+ Channel Isoforms by Ranolazine
Both muscle and neuronal Na+ channels are as sensitive to ranolazine block as their cardiac counterparts and at its therapeutic plasma concentrations, ranolazines interacts predominantly with the open but not resting or inactivated Na+ channel channels.
Tricyclic antidepressants as long-acting local anesthetics
Block of Human Heart hH1 Sodium Channels by the Enantiomers of Bupivacaine
Differences in bupivacaine stereoselectivity and intrinsic affinity between hH1 and &mgr;1 Na+ channels are small and most likely of minor clinical relevance.
Coapplication of Lidocaine and the Permanently Charged Sodium Channel Blocker QX-314 Produces a Long-lasting Nociceptive Blockade in Rodents
Coapplication of lidocaine and its quaternary derivative QX-314 produces a long-lasting, predominantly nociceptor-selective block, likely by facilitating Qx-314 entry through TRPV1 channels.
Single point mutations affect fatty acid block of human myocardial sodium channel α subunit Na+ channels
- Yong-Fu Xiao, Q. Ke, Alexander Leaf
- Biology, MedicineProceedings of the National Academy of Sciences…
- 6 March 2001
Results demonstrate that substitution of asparagine with lysine at the site of 406 in the domain-1-segment-6 region (D1-S6) significantly decreased the inhibitory effect of PUFAs on INa, and coexpression with β1 decreased this effect even more.
Amitriptyline versus Bupivacaine in Rat Sciatic Nerve Blockade
Findings suggest that amitriptyline could extend its clinical usefulness for peripheral nerve blockade and is a more potent blocker of neuronal Na+ channels than bupivacaine in vivo and in vitro.
Topical Amitriptyline in Healthy Volunteers