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Publication : A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K+ channels.

First Author  Inagaki N Year  1996
Journal  Neuron Volume  16
Issue  5 Pages  1011-7
PubMed ID  8630239 Mgi Jnum  J:135498
Mgi Id  MGI:3793935 Doi  10.1016/s0896-6273(00)80124-5
Citation  Inagaki N, et al. (1996) A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K+ channels. Neuron 16(5):1011-7
abstractText  We have cloned an isoform of the sulfonylurea receptor (SUR), designated SUR2. Coexpression of SUR2 and the inward rectifier K+ channel subunit Kir6.2 in COS1 cells reconstitutes the properties of K(ATP) channels described in cardiac and skeletal muscle. The SUR2/Kir6.2 channel is less sensitive than the SUR/Kir6.2 channel (the pancreatic beta cell KATP channel) to both ATP and the sulfonylurea glibenclamide and is activated by the cardiac K(ATP) channel openers, cromakalim and pinacidil, but not by diazoxide. In addition, SUR2 binds glibenclamide with lower affinity. The present study shows that the ATP sensitivity and pharmacological properties of K(ATP) channels are determined by a family of structurally related but functionally distinct sulfonylurea receptors.
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