Table 3
Functional activity of WT, Ser3.36Ala, and Ser5.46Ala 5-HT2A receptors
| EC50 | E
| |||||
|---|---|---|---|---|---|---|
| WT | S3.36A | S5.46A | WT | S3.36A | S5.46A | |
| 5-HT | 440 ± 15 | 5,085 ± 451 | 200 ± 14 | 1 | 1 | 1 |
| N-Me-5-HT | 233 ± 14 | 1,061 ± 140 | 0.21 ± 0.01 | 0.82 ± 0.01 | ||
| N,N-dMe-5-HT | 217 ± 29 | 280 ± 98 | 110 ± 18 | 0.19 ± 0.03 | 0.93 ± 0.07 | 0.41 ± 0.04 |
| 1-N-Me-5-HT | 4,206 ± 176 | 9,929 ± 2,052 | 293 ± 31 | 0.26 ± 0.02 | 0.11 ± 0.02 | 0.61 ± 0.03 |
| 5-MeOT | 199 ± 21 | 3,277 ± 178 | 182 ± 28 | 0.83 ± 0.10 | 1.0 ± 0.04 | 0.86 ± 0.10 |
| N-Me-5-MeOT | 214 ± 33 | 1,037 ± 244 | 0.29 ± 0.01 | 0.86 ± 0.08 | ||
| N,N-dMe-5-MeOT | 249 ± 49 | 504 ± 49 | 282 ± 64 | 0.26 ± 0.03 | 0.76 ± 0.06 | 0.43 ± 0.08 |
| 4-HT | 1,040 ± 321 | 14,801 ± 1,737 | 0.52 ± 0.02 | 0.25 ± 0.03 | ||
| N,N-dMe-4-HT | 366 ± 104 | 495 ± 89 | 0.07 ± 0.01 | 0.59 ± 0.04 | ||
| TRYP | 2,647 ± 578 | 37,230 ± 3,302 | 2,995 ± 925 | 0.43 ± 0.03 | 0.40 ± 0.04 | 0.54 ± 0.08 |
| N-Me-TRYP | 1,736 ± 132 | 5,584 ± 400 | 0.12 ± 0.01 | 0.23 ± 0.04 | ||
| N,N-dMe-TRYP | 888 ± 236 | 1,971 ± 370 | N.D. | 0.05 ± 0.02 | 0.32 ± 0.08 | 0 |
| 1-N-Me-TRYP | 7,629 ± 1,662 | 51,453 ± 14,489 | 1142 ± 311 | 0.08 ± 0.03 | 0.07 ± 0.02 | 0.35 ± 0.03 |
| LSD | 1.4 ± 0.4 | 3.4 ± 0.6 | 4.1 ± 0.9 | 0.11 ± 0.01 | 0.87 ± 0.03 | 0.15 ± 0.01 |
| Lisuride | N.D. | 3.4 ± 1.0 | 0 | 0.32 ± 0.07 | ||
| BOL | N.D. | 1.5 ± 0.2 | 0 | 0.37 ± 0.08 | ||
| Ergonovine | 17 ± 6 | 4.4 ± 0.1 | 19 ± 9 | 0.08 ± 0.01 | 0.79 ± 0.05 | 0.16 ± 0.02 |
| Methysergide | N.D. | 23 ± 3 | N.D. | 0 | 0.08 ± 0.01 | 0 |
| Mesulergine | N.D. | N.D. | 0 | 0 | ||
Values for EC50 and E 
were determined from accumulation of [3H]IP. Data are mean ± S.E. from at least three experiments.
-
N.D., EC50 could not be determined because of low activity