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 | 0.7–1.27–9 | 2.5–4.17–10 | 111–1476,7 | 0.002–0.0327,11,12 |
GluA1-flop | 45013 | 0.86–1.37–9,14 | 3.2–4.27–10,14 | 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 | 1.1–2.88–10,14,15,20 | 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 | 44.323–25 | 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 | 427–104031–34 | 1.6–2.529,32,33 | 3.4–5.331–36 | 1900–302031–33,35,37 | 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 | 22–23045–47 | 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 | 260–38245–47 | 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.
Determined from the peak response to rapid glutamate application.
Measurements are from outside out-patches; two time constants can be detected for many receptors.
See Lomeli et al. (1994) for RNA editing control of τ recovery.
The rate of recovery from desensitization is more complex; see Bowie (2002), Robert and Howe (2003).
Edited receptors or mutant receptors had a glutamine at the Q/R/N site.
Values predicted from simulations using rate constants.
Determined in X. laevis oocytes.
Determined for activation by kainate.
Onset and recovery from desensitization is variable from cell to cell.
Splice variants 7a and 7b have similar rates.
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).
SS/Peak current ratio is typically higher in whole-cell recordings.