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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
The sodium/calcium exchangers (NCX) use the extracellular sodium concentration to facilitate the extrusion of calcium out of the cell. Alongside the plasma membrane Ca2+-ATPase (PMCA) and sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA), as well as the sodium/potassium/calcium exchangers (NKCX, SLC24 family), NCX allow recovery of intracellular calcium back to basal levels after cellular stimulation. When intracellular sodium ion levels rise, for example, following depolarisation, these transporters can operate in the reverse direction to allow calcium influx and sodium efflux, as an electrogenic mechanism. Structural modelling suggests the presence of 9 TM segments, with a large intracellular loop between the fifth and sixth TM segments [1].
NCX1 (Sodium/calcium exchanger 1 / SLC8A1) C Show summary » |
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NCX2 (Sodium/calcium exchanger 2 / SLC8A2) C Show summary »
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NCX3 (Sodium/calcium exchanger 3 / SLC8A3) C Show summary » |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Transporters. Br J Pharmacol. 180 Suppl 2:S374-469.
Although subtype-selective inhibitors of NCX function are not widely available, 3,4-dichlorobenzamil and CBDMB act as non-selective NCX inhibitors, while SEA0400, KB-R7943, SN6, ORM-10103 [4] and ORM-10962 [5] act to inhibit NCX function with varying degrees of selectivity. BED is a preferential NCX3 inhibitor. It inhibits both modes of NCX3 operation, but only the reverse mode of NCX2 (and with reduced potency compared to NCX3) [7]. YM-244769 inhibits NCX3 preferentially over other isoforms [3,8]. Neurounina-1 stimulates NCX1 and NCX2 activity but not that of NCX3 [6].