. | Potency (EC50, μmol l–1) . | . | . | . | Efficacy (%5-HT effect) . | . | . | . | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Drug . | 5-HT2βPan . | 5-HT2βPro . | 5-HT1αPan . | 5-HT1αPro . | 5-HT2βPan . | 5-HT2βPro . | 5-HT1αPan . | 5-HT1αPro . | ||||||
5-HT | 0.052 | 0.27 | 0.0084 | 0.031 | 100 | 100 | 100 | 100 | ||||||
Dopamine | 310 | 362 | IA | IA | 54 | 19 | IA | IA | ||||||
Octopamine | IA | IA | IA | IA | IA | IA | IA | IA | ||||||
Tyramine | 283 | IA | IA | 30 | 32 | IA | IA | 67 | ||||||
Histamine | IA | IA | IA | IA | IA | IA | IA | IA | ||||||
DOI | 4.5 | IA | Bkd | NS | 32 | IA | Bkd | NS | ||||||
5-CT | 6.1 | 4.6 | 2.2 | NS | 79 | 50 | 100 | NS | ||||||
2-Me-5-HT | 0.78 | 5.2 | Bkd | 0.043 | 96 | 104 | Bkd | 73 | ||||||
MeOTryp | 1.0 | 1.5 | 4.2 | NS | 80 | 29 | 94 | NS | ||||||
N-acetyl-5-HT | IA | IA | IA | NS | IA | IA | IA | NS | ||||||
Quipazine | IA | IA | Bkd | 111 | IA | IA | Bkd | 92 | ||||||
α-Me-HT | 1.5 | 7.3 | 1.1 | 0.22 | 79 | 76 | 120 | 67 | ||||||
8-OH-DPAT | 0.27 | 1.1 | 7.6 | 65 | 77 | 64 | 105 | 68 | ||||||
mCPP | IA | IA | 139 | 109 | IA | IA | 97 | 70 | ||||||
Methysergide | 0.11 | 0.11 | 0.089 | 0.42 | 48 | 19 | 81 | 109 |
. | Potency (EC50, μmol l–1) . | . | . | . | Efficacy (%5-HT effect) . | . | . | . | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Drug . | 5-HT2βPan . | 5-HT2βPro . | 5-HT1αPan . | 5-HT1αPro . | 5-HT2βPan . | 5-HT2βPro . | 5-HT1αPan . | 5-HT1αPro . | ||||||
5-HT | 0.052 | 0.27 | 0.0084 | 0.031 | 100 | 100 | 100 | 100 | ||||||
Dopamine | 310 | 362 | IA | IA | 54 | 19 | IA | IA | ||||||
Octopamine | IA | IA | IA | IA | IA | IA | IA | IA | ||||||
Tyramine | 283 | IA | IA | 30 | 32 | IA | IA | 67 | ||||||
Histamine | IA | IA | IA | IA | IA | IA | IA | IA | ||||||
DOI | 4.5 | IA | Bkd | NS | 32 | IA | Bkd | NS | ||||||
5-CT | 6.1 | 4.6 | 2.2 | NS | 79 | 50 | 100 | NS | ||||||
2-Me-5-HT | 0.78 | 5.2 | Bkd | 0.043 | 96 | 104 | Bkd | 73 | ||||||
MeOTryp | 1.0 | 1.5 | 4.2 | NS | 80 | 29 | 94 | NS | ||||||
N-acetyl-5-HT | IA | IA | IA | NS | IA | IA | IA | NS | ||||||
Quipazine | IA | IA | Bkd | 111 | IA | IA | Bkd | 92 | ||||||
α-Me-HT | 1.5 | 7.3 | 1.1 | 0.22 | 79 | 76 | 120 | 67 | ||||||
8-OH-DPAT | 0.27 | 1.1 | 7.6 | 65 | 77 | 64 | 105 | 68 | ||||||
mCPP | IA | IA | 139 | 109 | IA | IA | 97 | 70 | ||||||
Methysergide | 0.11 | 0.11 | 0.089 | 0.42 | 48 | 19 | 81 | 109 |
EC50 values (potency) and relative efficacy were calculated from dose–response curves for each drug. Efficacy is presented as a given drug's ability to activate the receptor compared to the maximum activation obtained from 5-HT (100%). Drugs that activate one and not the other of 5-HT2β and 5-HT1α for each species are indicated in bold
IA, inactive; Bkd, drug has background activity on non-induced cells and was not tested; NS, curve could not be fit because of complex effects of the drug. N⩾3 separate experiments for each drug
DOI, 2,5-dimethoxy-4-iodoamphetamine; 5-CT, 5-carboxamidotryptamine;2-Me-5-HT, 2-methyl-serotonin; MeOTryp, 5-methoxytryptamine; α-Me-5-HT,α-methyl-serotonin; 8-OH-DPAT,(±)-8-hydroxy-2-(di-n-dipropylamino) tetralin; mCPP,1-(m-chlorophenyl)-piperazine