Table 2.
Summary of drug action on 5-HT2 receptors.
|
Drug / Receptor |
5-HT2A | 5-HT2B | 5-HT2C | Model (Ref) |
|---|---|---|---|---|
| 2C-B |
partial agonist ∼ 5–10 % (weak response for PLC and PLA2 pathways) |
- |
partial agonist ∼ 40–50 % (PLC and PLA2 pathways) |
CHO cells expressing human 5-HT2A or 5-HT2C receptors [28] |
| 2C-N |
partial agonist ∼ 20 % (PLA2 pathway) |
- | ||
|
2C-D 2C-I |
partial agonist ∼ 15–30 % (PLC and PLA2 pathways) |
- | ||
|
2C-C 2C-D 2C-E 2C‐T‐2 |
full agonist ∼ 65–125 % (PLC and PLA2 pathways) |
- |
full agonist ∼ 80–100 % (PLC pathway) |
HEK cells expressing the corresponding human 5-HT receptors [29] |
| 2C-I |
full agonist ∼ 80 % (PLC pathway) antagonist ∼ 30 % (PLA2 pathway) |
|||
|
25D-NBOMe 25E-NBOMe 25H-NBOMe 25N-NBOMe |
full agonist ∼ 85–95 % (PLC pathway) |
partial agonist ∼ 40–50 % (PLC pathway) |
full agonist ∼ 90–100 % (PLC pathway) |
HEK cells expressing the corresponding human 5-HT receptors [24] |
|
2C‐T‐4 2C‐T‐7 |
partial agonist ∼ 50–60 % |
partial agonist ∼ 45–75 % |
- | HEK 293 cells expressing the corresponding human 5-HT2B receptors; mouse embryonic fibroblasts expressing the human 5-HT2A receptor [27] |
|
2C-B, 2C-C, 2C-D, 2C-E, 2C-I, 2C-N, 2C‐T‐2, 2C‐T‐4, 2C‐T‐7, 25B-NBOMe, 25C-NBOMe, 25D-NBOMe, 25E-NBOMe, 25I-NBOMe, 25N-NBOMe, 25T2-NBOMe, 25T4-NBOMe, 25T7-NBOMe |
partial agonist ∼ 40–90 % |
partial agonist ∼ 45–90 % |
- | NIH-3T3 expressing the human 5-HT2A receptors; HEK293 cells expressing the human 5-HT2B receptors [25] |
|
2C-C 2C-I 25C-NBOMe 25I-NBOMe |
full agonist ∼ 90–110 % |
- |
partial agonist ∼ 30–70 % |
HEK 293 cells expressing the corresponding human 5-HT2A and 5-HT2C receptors [23] |