Summary data for all receptor constructs
| Receptor | Mutation | Location | k0(min−1) | m | pKapp |
|---|---|---|---|---|---|
| M1 | wt | 0.0316 (0.0009) | 0.863 (0.105) | 6.02 (0.14) | |
| M1 | LAGQ ⇒ EDGE | o2 | 0.0382 (0.0068) | 0.994 (0.003) | 6.74 (0.13) |
| M2 | wt | 0.166 (0.010) | 0.984 (0.013) | 6.79 (0.06) | |
| M2 | N ⇒ D | 419 | 0.161 (0.027) | 1.001-a | 7.43 (0.09) |
| M2 | N ⇒ E | 419 | 0.184 (0.014) | 1.001-a | 7.20 (0.04) |
| M2 | N ⇒ K | 419 | 0.0815 (0.0082) | 0.881 (0.104) | 5.84 (0.21) |
| M2 | EDGE ⇒ LAGQ | o2 | 0.110 (0.011) | 1.001-a | 6.04 (0.03) |
| M3 | wt | 0.0198 (0.0015) | 1.001-a | 5.03 (0.05) | |
| M3 | K ⇒ N | 419 | 0.0418 (0.0035) | 0.996 (0.004) | 6.23 (0.04) |
| M4 | wt | 0.0280 (0.0027) | 1.001-a | 5.93 (0.17) | |
| M4 | PDNQ ⇒ LAGQ | o2 | 0.0235 (0.0034) | 0.963 (0.022) | 5.96 (0.13) |
| M4 | D ⇒ N | 419 | 0.0158 (0.0019) | 1.001-a | 5.38 (0.08) |
| M5 | wt | 0.00867 (0.00060) | 0.720 (0.035) | 4.79 (0.09) | |
| M5 | T ⇒ A | 401 | 0.0137 (0.0009) | 0.658 (0.047) | 4.71 (0.10) |
| M5 | I ⇒ V | 405 | 0.00856 (0.00076) | 0.746 (0.054) | 4.80 (0.20) |
| M5 | V ⇒ I | 409 | 0.00925 (0.00023) | 0.853 (0.127) | 4.54 (0.27) |
| M5 | S ⇒ N | 410 | 0.00807 (0.00130) | 0.434 (0.076) | 3.98 (0.27) |
| M5 | VS ⇒ IN | 409–410 | 0.00617 (0.00033) | 0.468 (0.019) | 4.07 (0.21) |
| M5 | D ⇒ A | 414 | 0.00960 (0.00172) | 0.759 (0.055) | 5.00 (0.17) |
| M5 | K ⇒ P | 415 | 0.0106 (0.0008) | 0.803 (0.056) | 5.72 (0.08) |
| M5 | DK ⇒ AP | 414–415 | 0.0104 (0.0014) | 0.681 (0.125) | 4.88 (0.13) |
| M5 | V ⇒ N | 419 | 0.00865 (0.00065) | 0.920 (0.025) | 5.53 (0.06) |
| M5 | L ⇒ V | 421 | 0.00952 (0.00086) | 0.742 (0.058) | 4.91 (0.09) |
| M5 | DE ⇒ GQ | o2 | 0.00439 (.00036) | 0.689 (0.050) | 4.08 (0.06) |
Receptors are described as the parent receptor and the amino acids substituted. The location of the substitution is indicated either as the residue number in the M2 numbering scheme or as o2, meaning that the mutation was within the o2 region of the receptor. Additional detail about the locations of the mutations is presented in Figs. 1, 4, and 6. Data represent the mean (± S.E.) from three or more experiments. wt indicates wild-type; k 0, rate of dissociation of [3H]NMS from the receptor in the absence of gallamine; m and K app are as described inExperimental Procedures.
↵1-a Mean value is the upper constraint on m; no S.E. could be calculated.