Table 5 Comparison of drug affinities for [ 3 H]clozapine binding sites in rat brain membranes and cloned 5HT 6 receptors
[3H]Clozapine Ki (nM) | [3H]5HT (nM) | [3H]LSD (nM) | ||
|---|---|---|---|---|
5HT6 Clone | Cortex | 5HT6 Clone | ||
Clozapine | 10 | 10 | 20 | 13 |
Methiothepin | 9 | 7 | 0.4 | 2 |
Lisuride | 20 | 15 | 5 | 8 |
Dihydroergotamine | 25 | 40 | 5 | 13 |
Clomipramine | 150 | 80 | — | 54 |
Lergotrile | 150 | 250 | — | 36 |
Loxapine | 100 | 15 | 56 | 65 |
Nortriptyline | 400 | 30 | — | 148 |
Amitriptyline | 100 | 10 | 82 | 70 |
Fluoxetine | 4,000 | 5,000 | — | 1,700 |
Ritanserin | 1,000 | 150 | 16 | 44 |
Mesulergine | 2,000 | 1,000 | — | 1,700 |
Thioridazine | 300 | 25 | — | — |
Ketanserin | 1,000 | 80 | — | — |
Ergotamine | 10 | 12 | — | — |
Risperidone | >1,000 | 100 | — | — |
Metergoline | 950 | 1,000 | — | — |
Methysergide | 800 | 1,000 | — | — |