Antagonist profiles of 5-HT2β and 5-HT1αfrom Panulirus and Procambarus are well conserved
| . | Potency (IC50, μmol l–1) . | . | . | . | Efficacy (% reduction) . | . | ||||
|---|---|---|---|---|---|---|---|---|---|---|
| Drug . | 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 | ||||
| . | Potency (IC50, μmol l–1) . | . | . | . | Efficacy (% reduction) . | . | ||||
|---|---|---|---|---|---|---|---|---|---|---|
| Drug . | 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-HT2βand 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