Journal article
Forskolin alters acetylcholine receptor gating by a mechanism independent of adenylate cyclase activation
Molecular pharmacology, v 34(4), pp 427-430
Oct 1988
PMID: 2459589
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Abstract
The diterpene forskolin activates adenylate cyclase in a receptor-independent fashion and is commonly used to obtain a rapid elevation of intracellular cAMP levels. Application of 10-20 microM forskolin to Xenopus oocytes that express Torpedo nicotinic acetylcholine (ACh) receptors leads to an acceleration in the decay of ACh-elicited currents, which could be taken as evidence for modulation of ACh receptor gating by cAMP-dependent protein kinase. However, the effect is not mimicked by phosphodiesterase inhibitors or intracellular injection of a cAMP analog. In addition, 1,9-dideoxyforskolin, which is unable to activate adenylate cyclase, has a similar effect. Finally, the action of forskolin is rapidly reversible, with full onset and recovery occurring within the exchange time of the recording chamber. These results suggest that forskolin is a potent local anesthetic and that this property of this widely used compound must be taken into account when using it to study ion channel modulation.
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Details
- Title
- Forskolin alters acetylcholine receptor gating by a mechanism independent of adenylate cyclase activation
- Creators
- M M White - Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104
- Publication Details
- Molecular pharmacology, v 34(4), pp 427-430
- Publisher
- United States
- Grant note
- NS 23885 / NINDS NIH HHS
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:A1988Q634100002
- Scopus ID
- 2-s2.0-0023708347
- Other Identifier
- 991014878123904721
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- Web of Science research areas
- Pharmacology & Pharmacy