Drug | 5-HT2A | W76A | F125L | W200A | W336A | F339L | F340L | F365L | W367A | Y370A | F383A |
---|---|---|---|---|---|---|---|---|---|---|---|
Bufotenine | |||||||||||
K ACT(nm) | 84 ± 2 | 65 ± 26 | 109 ± 128 | 881 ± 832-a | 1838 ± 1792-a | 158 ± 96 | 1,900 ± 1902-a | 585 ± 2712-a | N.D. | 1346 ± 7962-a | 84 ±2 |
V MAX (% 5-HT) | 72 ± 1 | 27 ± 2 | 67 ± 20 | 11 ± 22-a | 16 ± 22-a | 75 ± 14 | 10.5 ± 1.42-a | 30 ± 142-a | 21 ± 2 | 72 ± 2 | |
α-Methyl-serotonin | |||||||||||
K ACT(nm) | 57 ± 14 | 241 ± 632-a | N.D. | 3090 ± 8362-a | N.D. | 311 ± 1332-a | 14,140 ± 68102-a | 3258 ± 9002-a | 117 ± 18 | ||
V MAX (% 5-HT) | 103 ± 13 | 31 ± 122-a | N.D. | 23 ± 52-a | N.D. | 100 ± 12 | 22 ± 182-a | 59 ± 32-a | 100 ± 3 | ||
5-HT | |||||||||||
K ACT (nm) | 47 ± 13 | 91 ± 15 | 249 ± 110 | 2637 ± 4392-a | 716 ± 4032-a | 249 ± 110 | 7,200 ± 20002-a | 118 ± 41 | 7100 ± 31002-a | 14280 ± 9602-a | 43 ± 6 |
V MAX (% 5-HT) | 100 | 31 ± 102-a | 100 ±7 | 3 ± 22-a | 27 ± 22-a | 100 (N = 2) | 18 ± 32-a | 32 ± 22-a | 7 ± 12-a | 9 ± 22-a | 100 ±2 |
DOM | |||||||||||
K ACT (nm) | 42 ± 16 | 166 ± 332-a | N.D. | 180 ± 123 | 28,1000 ± 14,000 | 98 ± 26 | 2360 ± 10752-a | 11,410 ± 5992-a | 67 ± 6 | ||
VMAX (% 5-HT) | 87 ± 4 | 42 ± 32-a | N.D. | 21 ± 22-a | 50 ± 32-a | 56 (N = 2) | 8 ± 12-a | 9 ± 12-a | 81 ± 2 |
Data represent mean ± standard deviation of computer-derived estimates for K act andV max values for experiments that have been replicated at least three times (except where noted).V max values are expressed relative to 5-HT expression of native 5-HT2A receptors. In a typical experiment, basal activity ranged from 200 to 400 cpm, whereas the maximum stimulation elicited by 5-HT was 6,000–10,000 cpm.
N.D., no activation of PI hydrolysis detected (>30% elevation over background).
↵2-a p < 0.05 versus native receptor (F test).