Table 1.
Effects of partial agonists on single GluN1/GluN2A channel currents
Agonists GluN1/GluN2 | reported efficacy (%) | amplitude (pA) | Po * | MOT (ms) | MCT (ms) | n | period analyzed (min) | events analyzed |
---|---|---|---|---|---|---|---|---|
Glu/Gly | 100 | 9.1 ± 0.6 | 0.64 ± 0.06 | 11.2 ± 1.1 | 6.4 ± 1.7 | 5 | 190 | 1,256,063 |
Glu/DCS | 75b, 93c | 9.2 ± 0.4 | 0.45 ± 0.11 | 8.4 ± 1.4 | 12 ± 3 | 5 | 109 | 438,502 |
Glu/Ala | 79d | 9.5 ± 0.4 | 0.27 ± 0.04 | 5.3 ± 0.6 | 14 ± 2 | 6 | 165 | 941,880 |
Glu/ACPC | 80a | 10.0 ± 0.3 | 0.27 ± 0.04 | 5.0 ± 0.8 | 12 ± 2 | 11 | 187 | 1,810,577 |
Glu/ACBC | 40a | 10.0 ± 0.2 | 0.07 ± 0.02 | 3.8 ± 0.6 | 39 ± 12 | 5 | 62 | 99,860 |
HCA/Gly | 86e | 10.0 ± 0.5 | 0.29 ± 0.06 | 4.7 ± 0.7 | 15 ± 3 | 10 | 287 | 1,791,508 |
SYM/Gly | 72e | 10.0 ± 0.6 | 0.36 ± 0.09 | 5.7 ± 0.9 | 13 ± 3 | 5 | 98 | 554,762 |
HQA/Gly | 75e | 10.2 ± 0.5 | 0.25 ± 0.04 | 5.8 ± 0.7 | 18 ± 2 | 5 | 217 | 997,465 |
QA/Gly | 20f, 60g | 10.0 ± 0.6 | 0.13 ± 0.06 | 6.2 ± 1.0 | 218 ± 87 | 8 | 165 | 328,578 |
References are: a) Inanobe 2005, b) Sheinen 2001, c) Priestley 1995, d) Chen 2008, e) Erreger 2007, f ) Blanke 2008, g) de Cavalho 1996.
Open probability was calculated as the fractional occupancy of the open state when fitting the entire sequence of events to kinetic models having five closed and one open states (5C1O).