Table 3.
Antagonist profiles of 5-HT2β and 5-HT1α from Panulirus and Procambarus are well conserved
| Drug | Potency (IC50, μmol l−1)
|
Efficacy (% reduction)
|
||||
|---|---|---|---|---|---|---|
| 5-HT2βPan | 5-HT2βPro | 5-HT1αPan | 5-HT1αPro | 5-HT2βPan | 5-HT2βPro | |
| Clozapine | 6.8 | 2.5 | Bkd | Bkd | 79 | 86 |
| Ritanserin | 0.57 | 0.18 | IA | Bkd | 58 | 86 |
| Methiothepin | 0.66 | 0.097 | Bkd | IA | 84 | 88 |
| (+)Butaclamol | 0.14 | 0.017 | IA | Bkd | 48 | 82 |
| Cinanserin | 1.2 | 1.6 | IA | IA | 73 | 88 |
| Gramine | IA | IA | IA | Bkd | IA | IA |
| (−)Butaclamol | IA | IA | IA | IA | IA | IA |
| Ketanserin | IA | IA | IA | IA | IA | IA |
| Spiperone | IA | IA | IA | IA | IA | ND |
| Prazosin | IA | IA | IA | Bkd | IA | IA |
| Atropine | IA | IA | IA | Bkd | IA | IA |
| Chlorpromazine | ND | ND | IA | IA | ND | ND |
| Flupenthixol | ND | ND | IA | Bkd | ND | ND |
| Domperidone | ND | ND | IA | Bkd | ND | ND |
| Fluphenazine | ND | ND | IA | Bkd | ND | ND |
| Haloperidol | ND | ND | IA | IA | ND | ND |
| Metoclopride | ND | ND | IA | IA | ND | ND |
| (−)Sulpiride | ND | ND | IA | Bkd | ND | ND |
| WAY100635 | ND | ND | IA | IA | ND | ND |
| Yohimbine | ND | ND | IA | IA | ND | ND |
| S(−)Propanolol | ND | ND | Bkd | IA | ND | ND |
| SB269970 | ND | ND | IA | IA | ND | ND |
| Metergoline | ND | ND | Bkd | Bkd | ND | ND |
| Cyproheptadine | ND | ND | Bkd | Bkd | ND | ND |
| SB224289 | ND | ND | IA | Bkd | ND | ND |
| BRL15572 | ND | ND | IA | IA | ND | ND |
| TFMPP | ND | ND | IA | IA | ND | ND |
| SCH23390 | ND | ND | Bkd | Bkd | ND | ND |
| S(−)eticlopride | ND | ND | Bkd | Bkd | ND | ND |
IC50 values (potency) and relative efficacy were calculated from dose–response curves for each drug. Efficacy is presented as the percentage reduction of the total effect obtained from 5-HT in the absence of antagonist. Drugs that block one and not the other of 5-HT2β and 5-HT1α for each species are indicated in bold. N≥3 separate experiments for each drug.
IA, inactive; Bkd, drug has background activity on non-induced cells and was not tested on induced cells, ND, not determined.