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Departments of 1 Pharmacology, 2 Neurosurgery, and 3 Anesthesiology, Kyoto University Faculty of Medicine, Kyoto 606-8507, Japan
We compared
the Ca2+ channels activated by endothelin-1 (ET-1) in
Chinese hamster ovary (CHO) cells stably expressing endothelin type A
(ETA) or endothelin type B (ETB) receptors
using the Ca2+ channel blockers LOE-908 and SK&F-96365. In
both CHO-ETA and CHO-ETB, ET-1 at 0.1 nM
activated the Ca2+-permeable nonselective cation channel-1
(NSCC-1), which was sensitive to LOE-908 and resistant to SK&F-96365.
ET-1 at 1 nM activated NSCC-2 in addition to NSCC-1; NSCC-2 was
sensitive to both LOE-908 and SK&F-96365. ET-1 at 10 nM activated the
same channels as 1 nM ET-1 in both cell types, but in
CHO-ETA, it additionally activated the store-operated
Ca2+ channel (SOCC), which was resistant to LOE-908 and
sensitive to SK&F-96365. Up to 1 nM ET-1, the level of the formation of inositol phosphates (IPs) was low and similar in both cell types, but,
at 10 nM ET-1, it was far greater in CHO-ETA than in
CHO-ETB. These results show that, in CHO-ETA
and CHO-ETB, ET-1 up to 10 nM activated the same
Ca2+ entry channels: 0.1 nM ET-1 activated NSCC-1, and
ET-1 
1 nM activated NSCC-1 and NSCC-2. Notably, in
CHO-ETA, 10 nM ET-1 activated SOCCs because of the higher
formation of IPs.
endothelin-1; endothelin receptor; calcium channel; calcium ion; Chinese hamster ovary
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