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Table 5 Comparison of drug affinities for [ 3 H]clozapine binding sites in rat brain membranes and cloned 5HT 6 receptors

From: Clozapine: Selective Labeling of Sites Resembling 5HT6 Serotonin Receptors May Reflect Psychoactive Profile

  [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
  1. Ki values are means of two to three determinations that varied less than 20%.