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Synonyms: DL-Bupivacaine | Exparel® | Marcain® | Posimir® | Sensorcaine® | W-7 | Xaracoll®
bupivacaine is an approved drug (FDA (1972), EMA (2020))
Compound class: Synthetic organic
Comment: The isomer levobupivacaine is also an approved drug but has a longer duration of action and produces less vasodilation.
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: bupivacaine
1. Franqueza L, Longobardo M, Vicente J, Delpón E, Tamkun MM, Tamargo J, Snyders DJ, Valenzuela C. (1997)
Molecular determinants of stereoselective bupivacaine block of hKv1.5 channels.
Circ Res, 81 (6): 1053-64. [PMID:9400387]
2. Qu YJ, Bondarenko VE, Xie C, Wang S, Awayda MS, Strauss HC, Morales MJ. (2007)
W-7 modulates Kv4.3: pore block and Ca2+-calmodulin inhibition.
Am J Physiol Heart Circ Physiol, 292 (5): H2364-77. [PMID:17220193]
3. Schwoerer AP, Scheel H, Friederich P. (2015)
A Comparative Analysis of Bupivacaine and Ropivacaine Effects on Human Cardiac SCN5A Channels.
Anesth Analg, 120 (6): 1226-34. [PMID:25692452]
4. Yeung SY, Ohya S, Sergeant GP, Pucovský V, Greenwood IA. (2006)
Pharmacological and molecular evidence for the involvement of Kv4.3 in ultra-fast activating K+ currents in murine portal vein myocytes.
Br J Pharmacol, 149 (6): 676-86. [PMID:17016508]
5. Zhou W, Arrabit C, Choe S, Slesinger PA. (2001)
Mechanism underlying bupivacaine inhibition of G protein-gated inwardly rectifying K+ channels.
Proc Natl Acad Sci USA, 98 (11): 6482-7. [PMID:11353868]