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. 2010 Sep;62(3):405–496. doi: 10.1124/pr.109.002451

TABLE 16.

Kinetic parameters describing glutamate activation of AMPA, kainate and NMDA receptors

EC501 τ-Deactivation2 τ-Desensitization τ-Recovery3,4 SS/Peak Ratio
μM ms ms ms
GluA1-flip 500–7005,6 0.7–1.279 2.5–4.1710 111–1476,7 0.002–0.0327,11,12
GluA1-flop 45013 0.86–1.379,14 3.2–4.2710,14 147–1557,14 0.023–0.0807,14,15
GluA2-flipQ16 139017 0.62–1.19,17 5.9–9.99,10,17 11.717 0.06817
GluA2-flopQ16 1140–138013,17 0.54–0.99,17 1.2–1.99,10,17 31.317 0.01117
GluA3-flip 1000–197015,18,19 0.5615 3.0–5.18,10,15,20 15–7015,21 0.024–0.05415,21
GluA3-flop 1100–178015,18,19 0.63–1.0514,15 1.1–2.8810,14,15,20 55–14214,15,22 0.0115
GluA4-flip 181012,18 0.68 3.6–5.18,10 6–216,21 0.006–0.0421
GluA4-flop 44.32325 0.68 0.98,10 31–4321 0.00321
GluA1-flip/GluA2-flip 5.126 28–6726 0.00926
GluA3-flip/GluA2-flip 4.926 15–2626 0.015–0.02226
GluK1a Q16 63027 4.1–8.9,6927,28 50,510029,30 0.0129
GluK2 Q16 427–10403134 1.6–2.529,32,33 3.4–5.33136 1900–30203133,35,37 0.008–0.0431,35,36
GluK3a38 590039 8.4–939 0.0439
GluK1 Q/GluK540 1941 2.1–1542
GluK2 Q/GluK5 15–3134,41 0.5, 4634 4.734 2400–270034
GluK3a/GluK4 7.639 0.0339
GluK3a/GluK5 5.339 0.01839
GluN1/GluN2A 1.8–7.743,44 22–2304547 386–750, 200045,47 61845 0.28–4248,49
GluN1/GluN2B 0.9–443,44,50 71–95, 538–61745,50 100, 49550 1014–210045,50 0.027–0.5318,50,51
GluN1/GluN2C 1.024,52,53 260–3824547 59–71954 1.047
GluN1/GluN2D 0.424,53,55 1700–440845,56 N.A. N.A. 1.056

N.A., not applicable; i.e., GluN1/GluN2C and GluN1/GluN2D receptors show no or minimal desensitization in the continued presence of agonist.

1

Determined from the peak response to rapid glutamate application.

2

Measurements are from outside out-patches; two time constants can be detected for many receptors.

3

See Lomeli et al. (1994) for RNA editing control of τ recovery.

4

The rate of recovery from desensitization is more complex; see Bowie (2002), Robert and Howe (2003).

16

Edited receptors or mutant receptors had a glutamine at the Q/R/N site.

18

Values predicted from simulations using rate constants.

24

Determined in X. laevis oocytes.

25

Determined for activation by kainate.

30

Onset and recovery from desensitization is variable from cell to cell.

38

Splice variants 7a and 7b have similar rates.

40

Determined by rapid application of glutamate; kainate-evoked currents desensitized with a dual exponential time course, with the fastest time constant being 15 ms (Herb et al., 1992).

51

SS/Peak current ratio is typically higher in whole-cell recordings.