Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes
dc.contributor.author | Bleasdale John E. , | en_US |
dc.contributor.author | Fisher Stephen K. , | en_US |
dc.date.accessioned | 2006-04-10T15:34:01Z | |
dc.date.available | 2006-04-10T15:34:01Z | |
dc.date.issued | 1993-10 | en_US |
dc.identifier.citation | Bleasdale John E., , Fisher Stephen K., (1993/10)."Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes." Neuroprotocols 3(2): 125-133. <http://hdl.handle.net/2027.42/30534> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6WNS-45P69GF-P/2/8ca6cbade97e29cec67e14186aebd826 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/30534 | |
dc.description.abstract | 1-[6-[[17[beta]-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]-hexyl]1H-pyrrole-2,5-dione (U-73122) is an aminosteroid that was identified initially as a potent inhibitor of platelet activation by receptor-specific agonists. U-73122 inhibits receptor-coupled generation of inositol 1,4,5-trisphosphate (but not cyclic AMP) and intracellular mobilization of Ca 2+ in a variety of cell types. U-73122 inhibits phosphoinositide-specific phospholipase C (PI-PLC) activity in cell-free systems, but exhibits little or no direct inhibition of phospholipases A2 and D. Structure-activity analysis revealed that the maleimide group of U-73122 is essential, but not sufficient, for inhibitory activity. The succinimide analog of U-73122 (U-73343) has negligible inhibitory activity and is a useful control compound. On the basis of information derived from the use of U-73122 in a variety of cell types, procedures for storing, dissolving, and presenting U-73122 to cells are recommended. While knowledge of the mechanism of action of U-73122 would extend the utility of this compound, U-73122 has already been employed successfully to examine PI-PLC involvement in a variety of cellular processes. The application of U-73122 in an investigation of muscarinic receptor sequestration in SK-N-SH neuroblastoma cells is illustrated. | en_US |
dc.format.extent | 842400 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Elsevier | en_US |
dc.title | Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Public Health | en_US |
dc.subject.hlbsecondlevel | Psychology | en_US |
dc.subject.hlbsecondlevel | Neurosciences | en_US |
dc.subject.hlbsecondlevel | Molecular, Cellular and Developmental Biology | en_US |
dc.subject.hlbtoplevel | Social Sciences | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Neuroscience Laboratory and Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48104-1687 | en_US |
dc.contributor.affiliationother | Metabolic Diseases Research, Upjohn Laboratories, Kalamazoo, Michigan 49001 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/30534/1/0000166.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1006/ncmn.1993.1046 | en_US |
dc.identifier.source | Neuroprotocols | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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