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. 2004 Nov;124(5):555–567. doi: 10.1085/jgp.200409077

TABLE II.

Kinetic Analysis of Mutant Receptors

Mutant k+1 k−1 K1 k+2 k−2 K2 β1 α1 Θ1 β2 α2 Θ2 k+b k−b KB
μM μM mM
Wild type 126
± 7
4500
± 399
35 182
± 11
14000
± 525
77 262
± 29
2310
± 200
0.11 44600
± 1010
1670
± 33
27 24
± 1
110000
± 1940
4.6
αD89N 3
± 0.1
1380
± 52
460 37
± 1
51800
± 1420
1400 2070
± 64
3200
± 72
0.64 40000a 2500
± 30
16 20
± 1
97400
± 1480
4.9
αD89E 14
± 0.6
1160
± 65
83 99
± 3
33700
± 744
340 962 3250 0.30 47500
± 1620
2570
± 63
18 21
± 1
111000
± 2500
5.3
αD89Tb 0.8
± 0.03
910
± 35
1140 44
± 4
57000
± 4680
1300 222
± 23
3070
± 323
0.07 49000
± 6080
1380
± 102
36 22
± 1
107000
± 2220
4.9
αT148L 114
± 5
3600
± 325
32 236
± 11
16500
± 626
70 249
± 29
2450
± 165
0.10 39400
± 779
1680
± 28
23 22
± 1
109000
± 1590
5.0
αT150A 334
± 19
8480
± 507
29 118
± 3
26100
± 778
221 287
± 21
2220
± 77
0.13 58000
± 1860
2010
± 52
29 20
± 1
103000
± 1860
5.2
αT148L + T150A 186
± 18
2460
± 252
13 105
± 5
24400
± 1080
232 ND ND 39200
± 1490
1270
± 34
31 25
± 1
101000
± 1640
4.0
αT148D 28
± 1
6060
± 618
216 130
± 10
27500
± 1890
212 918
± 116
2830
± 162
0.32 31500
± 1330
1500
± 44
21 23
± 1
99500
± 1880
4.3
αD89N + T148D 89
± 4
6530
± 553
73 118
± 5
29900
± 1120
253 ND ND 30100
± 953
2320
± 37
13 20
± 1
109000
± 2010
5.5
αT150D 50
± 6
19500
± 2550
390 89
± 14
31500
± 4850
354 232
± 42
6870
± 718
0.12 13900
± 604
1730
± 31
8 21
± 2
122000
± 4390
5.8
αD89N + T150D 59
± 10
15300
± 4650
259 82
± 16
32100
± 5120
391 249
± 72
4980
± 363
0.05 9580
± 682
2060
± 27
5 33
± 3
138000
± 4060
4.7

Kinetic parameters and error estimates are derived from global fitting of Scheme II to data obtained over a wide range of ACh concentrations (materials and methods). Units are μM−1s−1 for the association rate constants, s−1 for all others. Gating equilibrium constants (Θ) are ratios of channel opening (β) to closing rate (α) constants. ND, a second open time component was not detectable.

a

Opening rate constant is a lower bound (see text and Fig. 6).

b

Fitting was achieved using Scheme II modified to include two desensitized states linked to the open state. Fitted desensitization rate constants for αD89T, k+d/k−d, in units of s−1 are D1 (41/529) and D2 (65/30).

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