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lidocaine is an approved drug (FDA (1948))
Compound class: Synthetic organic
Comment: Lidocaine was the first-in-class amino amide-type local anesthetic to be discovered.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: lidocaine
1. Chevrier P, Vijayaragavan K, Chahine M. (2004)
Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine.
Br J Pharmacol, 142 (3): 576-84. [PMID:15148257]
2. Hill RJ, Duff HJ, Sheldon RS. (1989)
Class I antiarrhythmic drug receptor: biochemical evidence for state-dependent interaction with quinidine and lidocaine.
Mol Pharmacol, 36 (1): 150-9. [PMID:2546048]
3. How SW, Cheng AL. (1992)
Present status of cancer treatment in Taiwan.
Gan To Kagaku Ryoho, 19 (8 Suppl): 1136-8. [PMID:1514825]
4. Makielski JC, Limberis J, Fan Z, Kyle JW. (1999)
Intrinsic lidocaine affinity for Na channels expressed in Xenopus oocytes depends on alpha (hH1 vs. rSkM1) and beta 1 subunits.
Cardiovasc Res, 42 (2): 503-9. [PMID:10533585]
5. Nuss HB, Tomaselli GF, Marbán E. (1995)
Cardiac sodium channels (hH1) are intrinsically more sensitive to block by lidocaine than are skeletal muscle (mu 1) channels.
J Gen Physiol, 106 (6): 1193-209. [PMID:8786356]
6. Ragsdale DS, McPhee JC, Scheuer T, Catterall WA. (1996)
Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels.
Proc Natl Acad Sci USA, 93 (17): 9270-5. [PMID:8799190]